Faculty Appointments
Research Professor of Pharmacology
Professor of Pharmacology, Emeritus
Education
Ph.D., Pharmacology, Vanderbilt University, Nashville, TennesseeB.S., Physiological Psychology/Biology, Lee University, Cleveland, Tennessee
Office Address
23rd Avenue South at Pierce
Nashville, TN 37232-6600
Nashville, TN 37232-6600
Research Description
Dr. Conn is the Lee E. Limbird Professor of Pharmacology at Vanderbilt University and Director of the Vanderbilt Center for Neuroscience Drug Discovery (VCNDD). He received the Ph.D. degree from Vanderbilt in 1986 and pursued postdoctoral studies at Yale University before joining the faculty at Emory University in 1988. Dr. Conn served as head of the Department of Neuroscience at Merck and Company (West Point, PA) from 2000 – 2003 then moved to Vanderbilt as founding director of the VCNDD. Dr. Conn served as Editor in Chief of Molecular Pharmacology, on editorial boards of multiple other journals, and Scientific Advisory Boards of multiple foundations and companies. He has received numerous awards for his translational research. The primary focus of research in the Conn laboratory is to develop a detailed understanding of the cellular mechanisms involved in regulating signaling through identified brain circuits that are impacted in neurological and psychiatric disorders and insights that this may provide for development of novel therapeutic strategies. The primary mission of the VCNDD under Dr. Conn’s leadership is to build on fundamental breakthroughs in neuroscience to develop novel treatment strategies for brain disorders. His lab focuses specific efforts on metabotropic glutamate receptors and muscarinic acetylcholine receptors and the roles of individual receptor subtypes in regulating brain function. He pioneered discovery and characterization of allosteric modulators of G protein-coupled receptors (GPCRs), which represents a fundamentally new area that is impacting all GPCR research. Dr. Conn builds on these advances in to develop novel treatments for schizophrenia, Parkinson’s disease, and other CNS disorders. These efforts have generated multiple drug candidates that are advancing to clinical development at Vanderbilt and in collaboration with pharmaceutical companies, including Johnson and Johnson, Bristol Myers Squibb, AstraZeneca, and others. These represent novel approaches with potential for providing fundamental advances in patient care. Please visit the following websites for more information on research that The Conn Lab and The VCNDD are working on, (Conn Lab URL: https://www.connlab.com/ and The VCNDD URL: http://www.vcndd.org/).
Research Keywords
Cellular/molecular mechanisms of regulation of neuronal function. Novel treatments for CNS disorders. Drug Discovery
Publications
O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ. Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators. Mol. Pharmacol [print-electronic]. 2018 Mar 3/15/2018; PMID: 29545267, PII: mol.117.110114, DOI: 10.1124/mol.117.110114, ISSN: 1521-0111.
Stansley BJ, Conn PJ. The therapeutic potential of metabotropic glutamate receptor modulation for schizophrenia. Curr Opin Pharmacol [print-electronic]. 2018 Feb 2/24/2018; 38: 31-6. PMID: 29486374, PII: S1471-4892(17)30063-2, DOI: 10.1016/j.coph.2018.02.003, ISSN: 1471-4973.
Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology [print-electronic]. 2017 Mar 3/15/2017; 115: 60-72. PMID: 27392634, PMCID: PMC5217481, PII: S0028-3908(16)30287-8, DOI: 10.1016/j.neuropharm.2016.07.001, ISSN: 1873-7064.
Ade KK, Wan Y, Hamann HC, O'Hare JK, Guo W, Quian A, Kumar S, Bhagat S, Rodriguiz RM, Wetsel WC, Conn PJ, Dzirasa K, Huber KM, Calakos N. Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice. Biol. Psychiatry [print-electronic]. 2016 Oct 10/1/2016; 80(7): 522-33. PMID: 27436084, PMCID: PMC5536332, PII: S0006-3223(16)32380-0, DOI: 10.1016/j.biopsych.2016.04.023, ISSN: 1873-2402.
Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Aug 8/1/2016; 26(15): 3822-5. PMID: 27173801, PMCID: PMC5082649, PII: S0960-894X(16)30472-3, DOI: 10.1016/j.bmcl.2016.04.083, ISSN: 1464-3405.
Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ. Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. ACS Chem. Biol [print-electronic]. 2016 Jul 7/15/2016; 11(7): 1870-9. PMID: 27115427, PMCID: PMC4981245, DOI: 10.1021/acschembio.6b00026, ISSN: 1554-8937.
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jul 7/1/2016; 26(13): 2984-7. PMID: 27234146, PMCID: PMC4955388, PII: S0960-894X(16)30514-5, DOI: 10.1016/j.bmcl.2016.05.029, ISSN: 1464-3405.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jul 7/1/2016; 26(13): 3029-33. PMID: 27185330, PMCID: PMC4955361, PII: S0960-894X(16)30490-5, DOI: 10.1016/j.bmcl.2016.05.010, ISSN: 1464-3405.
Balu DT, Li Y, Takagi S, Presti KT, Ramikie TS, Rook JM, Jones CK, Lindsley CW, Conn PJ, Bolshakov VY, Coyle JT. An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia. Neuropsychopharmacology [print-electronic]. 2016 Jul; 41(8): 2052-61. PMID: 26741285, PMCID: PMC4908650, PII: npp20162, DOI: 10.1038/npp.2016.2, ISSN: 1740-634X.
Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jun 6/15/2016; 26(12): 2915-9. PMID: 27131990, PMCID: PMC4899947, PII: S0960-894X(16)30414-0, DOI: 10.1016/j.bmcl.2016.04.041, ISSN: 1464-3405.
Ponnazhagan R, Harms AS, Thome AD, Jurkuvenaite A, Gogliotti R, Niswender CM, Conn PJ, Standaert DG. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol [print-electronic]. 2016 Jun; 11(2): 231-7. PMID: 26872456, PMCID: PMC4848139, PII: 10.1007/s11481-016-9655-z, DOI: 10.1007/s11481-016-9655-z, ISSN: 1557-1904.
Gogliotti RG, Senter RK, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones CK, Lindsley CW, Conn PJ, Niswender CM. MGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome. Hum. Mol. Genet [print-electronic]. 2016 May 5/15/2016; 25(10): 1990-2004. PMID: 26936821, PMCID: PMC5062588, PII: ddw074, DOI: 10.1093/hmg/ddw074, ISSN: 1460-2083.
O'Brien DE, Conn PJ. Neurobiological Insights from mGlu Receptor Allosteric Modulation. Int. J. Neuropsychopharmacol [electronic-print]. 2016 May; 19(5): PMID: 26647381, PMCID: PMC4886670, PII: pyv133, DOI: 10.1093/ijnp/pyv133, ISSN: 1469-5111.
Dean B, Hopper S, Conn PJ, Scarr E. Changes in BQCA Allosteric Modulation of [(3)H]NMS Binding to Human Cortex within Schizophrenia and by Divalent Cations. Neuropsychopharmacology [print-electronic]. 2016 May; 41(6): 1620-8. PMID: 26511338, PMCID: PMC4832025, PII: npp2015330, DOI: 10.1038/npp.2015.330, ISSN: 1740-634X.
Garcia-Barrantes PM, Cho HP, Starr TM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR. Bioorg. Med. Chem. Lett [print-electronic]. 2016 May 5/1/2016; 26(9): 2289-92. PMID: 27013388, PMCID: PMC4833523, PII: S0960-894X(16)30264-5, DOI: 10.1016/j.bmcl.2016.03.044, ISSN: 1464-3405.
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Apr 4/15/2016; 26(8): 1894-900. PMID: 26988308, PMCID: PMC4824313, PII: S0960-894X(16)30246-3, DOI: 10.1016/j.bmcl.2016.03.026, ISSN: 1464-3405.
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Apr 4/15/2016; 26(8): 1869-72. PMID: 26988302, PMCID: PMC4823774, PII: S0960-894X(16)30251-7, DOI: 10.1016/j.bmcl.2016.03.031, ISSN: 1464-3405.
Xiang Z, Conn PJ. Novel PAMs Targeting NMDAR GluN2A Subunit. Neuron. 2016 Mar 3/2/2016; 89(5): 884-6. PMID: 26938436, PMCID: PMC4793964, PII: S0896-6273(16)00142-2, DOI: 10.1016/j.neuron.2016.02.025, ISSN: 1097-4199.
Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, Lindsley CW, Conn PJ, Jones CK. State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects. Neuropharmacology [print-electronic]. 2016 Mar; 102: 244-53. PMID: 26617071, PMCID: PMC4809053, PII: S0028-3908(15)30180-5, DOI: 10.1016/j.neuropharm.2015.11.016, ISSN: 1873-7064.
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW, Jones CK. Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. Neuropsychopharmacology [print-electronic]. 2016 Mar; 41(4): 1166-78. PMID: 26315507, PMCID: PMC4748441, PII: npp2015265, DOI: 10.1038/npp.2015.265, ISSN: 1740-634X.
Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Feb 2/1/2016; 26(3): 751-6. PMID: 26778256, PMCID: PMC4794757, PII: S0960-894X(15)30417-0, DOI: 10.1016/j.bmcl.2015.12.104, ISSN: 1464-3405.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM. Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jan 1/15/2016; 26(2): 429-34. PMID: 26684851, PMCID: PMC4835042, PII: S0960-894X(15)30306-1, DOI: 10.1016/j.bmcl.2015.11.098, ISSN: 1464-3405.
Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ. VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy. J. Pharmacol. Exp. Ther [print-electronic]. 2016 Jan; 356(1): 123-36. PMID: 26503377, PMCID: PMC4702078, PII: jpet.115.226597, DOI: 10.1124/jpet.115.226597, ISSN: 1521-0103.
Ghoshal A, Rook JM, Dickerson JW, Roop GN, Morrison RD, Jalan-Sakrikar N, Lamsal A, Noetzel MJ, Poslusney MS, Wood MR, Melancon BJ, Stauffer SR, Xiang Z, Daniels JS, Niswender CM, Jones CK, Lindsley CW, Conn PJ. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology [print-electronic]. 2016 Jan; 41(2): 598-610. PMID: 26108886, PMCID: PMC5130135, PII: npp2015189, DOI: 10.1038/npp.2015.189, ISSN: 1740-634X.
Senter RK, Ghoshal A, Walker AG, Xiang Z, Niswender CM, Conn PJ. The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies. Curr Neuropharmacol. 2016; 14(5): 455-73. PMID: 27296640, PMCID: PMC4983746, PII: CN-EPUB-66683, ISSN: 1875-6190.
Gogliotti RG, Conn PJ. Pharmacological Treatments for Autism Spectrum Disorder: Will Emerging Approaches Yield New Treatments?. Neuropsychopharmacology. 2016 Jan; 41(1): 376-7. PMID: 26657955, PMCID: PMC4677143, PII: npp2015259, DOI: 10.1038/npp.2015.259, ISSN: 1740-634X.
Garcia RC, Dati LM, Torres LH, da Silva MA, Udo MS, Abdalla FM, da Costa JL, Gorjão R, Afeche SC, Yonamine M, Niswender CM, Conn PJ, Camarini R, Sandoval MR, Marcourakis T. M1 and M3 muscarinic receptors may play a role in the neurotoxicity of anhydroecgonine methyl ester, a cocaine pyrolysis product. Sci Rep. 2015 Dec 12/2/2015; 5: 17555. PMID: 26626425, PMCID: PMC4667193, PII: srep17555, DOI: 10.1038/srep17555, ISSN: 2045-2322.
Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2. J. Med. Chem [print-electronic]. 2015 Nov 11/25/2015; 58(22): 9027-40. PMID: 26524606, PMCID: PMC4817271, DOI: 10.1021/acs.jmedchem.5b01371, ISSN: 1520-4804.
Shen W, Plotkin JL, Francardo V, Ko WK, Xie Z, Li Q, Fieblinger T, Wess J, Neubig RR, Lindsley CW, Conn PJ, Greengard P, Bezard E, Cenci MA, Surmeier DJ. M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia. Neuron. 2015 Nov 11/18/2015; 88(4): 762-73. PMID: 26590347, PMCID: PMC4864040, PII: S0896-6273(15)00933-2, DOI: 10.1016/j.neuron.2015.10.039, ISSN: 1097-4199.
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Nov 11/15/2015; 25(22): 5107-10. PMID: 26476971, PMCID: PMC4758672, PII: S0960-894X(15)30121-9, DOI: 10.1016/j.bmcl.2015.10.013, ISSN: 1464-3405.
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Nov 11/15/2015; 25(22): 5115-20. PMID: 26475522, PMCID: PMC4634704, PII: S0960-894X(15)30118-9, DOI: 10.1016/j.bmcl.2015.10.009, ISSN: 1464-3405.
Pancani T, Foster DJ, Moehle MS, Bichell TJ, Bradley E, Bridges TM, Klar R, Poslusney M, Rook JM, Daniels JS, Niswender CM, Jones CK, Wood MR, Bowman AB, Lindsley CW, Xiang Z, Conn PJ. Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2015 Nov 11/10/2015; 112(45): 14078-83. PMID: 26508634, PMCID: PMC4653197, PII: 1512812112, DOI: 10.1073/pnas.1512812112, ISSN: 1091-6490.
Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS. Tackling reproducibility in academic preclinical drug discovery. Nat Rev Drug Discov [print-electronic]. 2015 Nov; 14(11): 733-4. PMID: 26388229, PII: nrd4737, DOI: 10.1038/nrd4737, ISSN: 1474-1784.
Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS. A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo. Drug Metab. Dispos [print-electronic]. 2015 Nov; 43(11): 1718-26. PMID: 26265743, PMCID: PMC4613951, PII: dmd.115.064006, DOI: 10.1124/dmd.115.064006, ISSN: 1521-009X.
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW. Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics. J. Med. Chem [print-electronic]. 2015 Oct 10/22/2015; 58(20): 7959-71. PMID: 26426481, PMCID: PMC4839290, DOI: 10.1021/acs.jmedchem.5b00727, ISSN: 1520-4804.
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J. Med. Chem [print-electronic]. 2015 Sep 9/24/2015; 58(18): 7485-500. PMID: 26335039, PMCID: PMC4809247, DOI: 10.1021/acs.jmedchem.5b01005, ISSN: 1520-4804.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Sep 9/1/2015; 25(17): 3515-9. PMID: 26183084, PMCID: PMC4535329, PII: S0960-894X(15)00701-5, DOI: 10.1016/j.bmcl.2015.06.096, ISSN: 1464-3405.
Burket JA, Benson AD, Green TL, Rook JM, Lindsley CW, Conn PJ, Deutsch SI. Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism. Prog. Neuropsychopharmacol. Biol. Psychiatry [print-electronic]. 2015 Aug 8/3/2015; 61: 10-7. PMID: 25784602, PII: S0278-5846(15)00052-4, DOI: 10.1016/j.pnpbp.2015.03.003, ISSN: 1878-4216.
Smith E, Chase P, Niswender CM, Utley TJ, Sheffler DJ, Noetzel MJ, Lamsal A, Wood MR, Conn PJ, Lindsley CW, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P. Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4). J Biomol Screen [print-electronic]. 2015 Aug; 20(7): 858-68. PMID: 25877150, PMCID: PMC4659430, PII: 1087057115581770, DOI: 10.1177/1087057115581770, ISSN: 1552-454X.
Iderberg H, Maslava N, Thompson AD, Bubser M, Niswender CM, Hopkins CR, Lindsley CW, Conn PJ, Jones CK, Cenci MA. Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist. Neuropharmacology [print-electronic]. 2015 Aug; 95: 121-9. PMID: 25749357, PMCID: PMC4466038, PII: S0028-3908(15)00079-9, DOI: 10.1016/j.neuropharm.2015.02.023, ISSN: 1873-7064.
Brown JH, Catterall WA, Conn PJ, Cull-Candy SG, Dingledine R, Harden TK, Insel PA, Milligan G, Traynelis SF. The First 50 Years of Molecular Pharmacology. Mol. Pharmacol [print-electronic]. 2015 Jul; 88(1): 139-40. PMID: 25943115, PII: mol.115.099564, DOI: 10.1124/mol.115.099564, ISSN: 1521-0111.
Gregory KJ, Conn PJ. Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation. Mol. Pharmacol [print-electronic]. 2015 Jul; 88(1): 188-202. PMID: 25808929, PMCID: PMC4468636, PII: mol.114.097220, DOI: 10.1124/mol.114.097220, ISSN: 1521-0111.
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015 Jun 6/11/2015; 6(6): 716-20. PMID: 26157544, PMCID: PMC4492464, DOI: 10.1021/acsmedchemlett.5b00181, ISSN: 1948-5875.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA, . Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 2015 Jun 6/4/2015; 161(6): 1252-65. PMID: 26046436, PMCID: PMC4564295, PII: S0092-8674(15)00572-3, DOI: 10.1016/j.cell.2015.05.023, ISSN: 1097-4172.
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ. Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents. Neuron [print-electronic]. 2015 May 5/20/2015; 86(4): 1029-40. PMID: 25937172, PMCID: PMC4443790, PII: S0896-6273(15)00287-1, DOI: 10.1016/j.neuron.2015.03.063, ISSN: 1097-4199.
Klar R, Walker AG, Ghose D, Grueter BA, Engers DW, Hopkins CR, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. J. Neurosci. 2015 May 5/13/2015; 35(19): 7600-15. PMID: 25972184, PMCID: PMC4429158, PII: 35/19/7600, DOI: 10.1523/JNEUROSCI.4543-14.2015, ISSN: 1529-2401.
Nedelcovych MT, Gould RW, Zhan X, Bubser M, Gong X, Grannan M, Thompson AT, Ivarsson M, Lindsley CW, Conn PJ, Jones CK. A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances. ACS Chem Neurosci [print-electronic]. 2015 Mar 3/18/2015; 6(3): 485-93. PMID: 25581551, PMCID: PMC4403733, DOI: 10.1021/cn500342u, ISSN: 1948-7193.
Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg. Med. Chem. Lett [print-electronic]. 2015 Mar 3/15/2015; 25(6): 1310-7. PMID: 25683622, PMCID: PMC4399811, PII: S0960-894X(15)00050-5, DOI: 10.1016/j.bmcl.2015.01.038, ISSN: 1464-3405.
Walker AG, Wenthur CJ, Xiang Z, Rook JM, Emmitte KA, Niswender CM, Lindsley CW, Conn PJ. Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2015 Jan 1/27/2015; 112(4): 1196-201. PMID: 25583490, PMCID: PMC4313856, PII: 1416196112, DOI: 10.1073/pnas.1416196112, ISSN: 1091-6490.
Ghoshal A, Conn PJ. The hippocampo-prefrontal pathway: a possible therapeutic target for negative and cognitive symptoms of schizophrenia. Future Neurol. 2015; 10(2): 115-28. PMID: 25825588, PMCID: PMC4376007, DOI: 10.2217/FNL.14.63, ISSN: 1479-6708.
Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe. ChemMedChem [print-electronic]. 2014 Aug; 9(8): 1677-82. PMID: 24692176, PMCID: PMC4116439, DOI: 10.1002/cmdc.201402051, ISSN: 1860-7187.
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol. Pharmacol [print-electronic]. 2009 Aug; 76(2): 356-68. PMID: 19407080, PMCID: PMC2713127, PII: mol.109.056531, DOI: 10.1124/mol.109.056531, ISSN: 1521-0111.
Ayala JE, Chen Y, Banko JL, Sheffler DJ, Williams R, Telk AN, Watson NL, Xiang Z, Zhang Y, Jones PJ, Lindsley CW, Olive MF, Conn PJ. MGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology [print-electronic]. 2009 Aug; 34(9): 2057-71. PMID: 19295507, PMCID: PMC2884290, PII: npp200930, DOI: 10.1038/npp.2009.30, ISSN: 1740-634X.
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J. Med. Chem. 2009 Jul 7/23/2009; 52(14): 4115-8. PMID: 19469556, PMCID: PMC2765192, DOI: 10.1021/jm9005065, ISSN: 1520-4804.
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jun 6/15/2009; 19(12): 3209-13. PMID: 19443219, PMCID: PMC3177605, PII: S0960-894X(09)00621-0, DOI: 10.1016/j.bmcl.2009.04.110, ISSN: 1464-3405.
Kennedy JP, Conn PJ, Lindsley CW. A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jun 6/15/2009; 19(12): 3204-8. PMID: 19443215, PII: S0960-894X(09)00618-0, DOI: 10.1016/j.bmcl.2009.04.106, ISSN: 1464-3405.
Kulkarni SS, Zou MF, Cao J, Deschamps JR, Rodriguez AL, Conn PJ, Newman AH. Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. J. Med. Chem. 2009 Jun 6/11/2009; 52(11): 3563-75. PMID: 19445453, PMCID: PMC2894482, DOI: 10.1021/jm900172f, ISSN: 1520-4804.
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J. Med. Chem. 2009 Jun 6/11/2009; 52(11): 3445-8. PMID: 19438238, PMCID: PMC3875304, DOI: 10.1021/jm900286j, ISSN: 1520-4804.
Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. ChemMedChem. 2009 Apr; 4(4): 505-11. PMID: 19197923, PMCID: PMC2865690, DOI: 10.1002/cmdc.200800357, ISSN: 1860-7187.
Conn PJ, Jones CK, Lindsley CW. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol. Sci [print-electronic]. 2009 Mar; 30(3): 148-55. PMID: 19201489, PMCID: PMC2907736, PII: S0165-6147(09)00013-3, DOI: 10.1016/j.tips.2008.12.002, ISSN: 0165-6147.
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol. Pharmacol [print-electronic]. 2009 Mar; 75(3): 577-88. PMID: 19047481, PMCID: PMC2684909, PII: mol.108.052886, DOI: 10.1124/mol.108.052886, ISSN: 1521-0111.
Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Feb 2/1/2009; 19(3): 962-6. PMID: 19097893, PMCID: PMC3787871, PII: S0960-894X(08)01468-6, DOI: 10.1016/j.bmcl.2008.11.104, ISSN: 1464-3405.
Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov. 2009 Jan; 8(1): 41-54. PMID: 19116626, PMCID: PMC2907734, PII: nrd2760, DOI: 10.1038/nrd2760, ISSN: 1474-1784.
Conn PJ, Jones CK. Promise of mGluR2/3 activators in psychiatry. Neuropsychopharmacology. 2009 Jan; 34(1): 248-9. PMID: 19079073, PMCID: PMC2907744, PII: npp2008156, DOI: 10.1038/npp.2008.156, ISSN: 1740-634X.
Conn PJ, Lindsley CW, Jones CK. Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol. Sci [print-electronic]. 2009 Jan; 30(1): 25-31. PMID: 19058862, PMCID: PMC2907735, PII: S0165-6147(08)00247-2, DOI: 10.1016/j.tips.2008.10.006, ISSN: 0165-6147.
Brady AE, Jones CK, Bridges TM, Kennedy JP, Thompson AD, Heiman JU, Breininger ML, Gentry PR, Yin H, Jadhav SB, Shirey JK, Conn PJ, Lindsley CW. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J. Pharmacol. Exp. Ther [print-electronic]. 2008 Dec; 327(3): 941-53. PMID: 18772318, PMCID: PMC2745822, PII: jpet.108.140350, DOI: 10.1124/jpet.108.140350, ISSN: 1521-0103.
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol. Pharmacol [print-electronic]. 2008 Nov; 74(5): 1345-58. PMID: 18664603, PMCID: PMC2574552, PII: mol.108.049551, DOI: 10.1124/mol.108.049551, ISSN: 1521-0111.
Miller NR, Daniels RN, Bridges TM, Brady AE, Conn PJ, Lindsley CW. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5443-7. PMID: 18829311, PMCID: PMC3177607, PII: S0960-894X(08)01088-3, DOI: 10.1016/j.bmcl.2008.09.032, ISSN: 1464-3405.
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW. Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5439-42. PMID: 18805692, PMCID: PMC3177598, PII: S0960-894X(08)01078-0, DOI: 10.1016/j.bmcl.2008.09.023, ISSN: 1464-3405.
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5626-30. PMID: 18793851, PMCID: PMC3182458, PII: S0960-894X(08)01018-4, DOI: 10.1016/j.bmcl.2008.08.087, ISSN: 1464-3405.
Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J. Neurosci. 2008 Oct 10/8/2008; 28(41): 10422-33. PMID: 18842902, PMCID: PMC2577155, PII: 28/41/10422, DOI: 10.1523/JNEUROSCI.1850-08.2008, ISSN: 1529-2401.
Jones PJ, Xiang Z, Conn PJ. Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract-piriform cortex synapse. Neuropharmacology [print-electronic]. 2008 Sep; 55(4): 440-6. PMID: 18625254, PMCID: PMC2644556, PII: S0028-3908(08)00238-4, DOI: 10.1016/j.neuropharm.2008.06.043, ISSN: 0028-3908.
Sheffler DJ, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology [print-electronic]. 2008 Sep; 55(4): 419-27. PMID: 18625258, PMCID: PMC2600811, PII: S0028-3908(08)00245-1, DOI: 10.1016/j.neuropharm.2008.06.047, ISSN: 0028-3908.
Conn PJ, Roth BL. Opportunities and challenges of psychiatric drug discovery: roles for scientists in academic, industry, and government settings. Neuropsychopharmacology [print-electronic]. 2008 Aug; 33(9): 2048-60. PMID: 18216778, PII: 1301638, DOI: 10.1038/sj.npp.1301638, ISSN: 0893-133X.
Sharma S, Rodriguez AL, Conn PJ, Lindsley CW. Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Jul 7/15/2008; 18(14): 4098-101. PMID: 18550372, PMCID: PMC2533619, PII: S0960-894X(08)00599-4, DOI: 10.1016/j.bmcl.2008.05.091, ISSN: 1464-3405.
Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ. Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated. Neuropharmacology [print-electronic]. 2008 Apr; 54(5): 804-14. PMID: 18255102, PMCID: PMC2431171, PII: S0028-3908(07)00397-8, DOI: 10.1016/j.neuropharm.2007.12.009, ISSN: 0028-3908.
Conn PJ, Tamminga C, Schoepp DD, Lindsley C. Schizophrenia: moving beyond monoamine antagonists. Mol. Interv. 2008 Apr; 8(2): 99-107. PMID: 18403654, PII: 8/2/99, DOI: 10.1124/mi.8.2.7, ISSN: 1534-0384.
Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol. Pharmacol [print-electronic]. 2008 Apr; 73(4): 1213-24. PMID: 18171729, PII: mol.107.041053, DOI: 10.1124/mol.107.041053, ISSN: 1521-0111.
Chen Y, Goudet C, Pin JP, Conn PJ. N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol. Pharmacol [print-electronic]. 2008 Mar; 73(3): 909-18. PMID: 18056795, PII: mol.107.040097, DOI: 10.1124/mol.107.040097, ISSN: 1521-0111.
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Feb 2/1/2008; 18(3): 885-90. PMID: 18178088, PMCID: PMC2275053, PII: S0960-894X(07)01510-7, DOI: 10.1016/j.bmcl.2007.12.051, ISSN: 1464-3405.
Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat. Chem. Biol [print-electronic]. 2008 Jan; 4(1): 42-50. PMID: 18059262, PII: nchembio.2007.55, DOI: 10.1038/nchembio.2007.55, ISSN: 1552-4469.
Bikbaev A, Neyman S, Ngomba RT, Conn J, Nicoletti F, Manahan-Vaughan D. MGluR5 mediates the interaction between late-LTP, network activity, and learning. PLoS ONE. 2008; 3((5)): e2155.
Benneyworth MA, Xiang Z, Smith RL, Garcia EE, Conn PJ, Sanders-Bush E. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Mol. Pharmacol [print-electronic]. 2007 Aug; 72(2): 477-84. PMID: 17526600, PII: mol.107.035170, DOI: 10.1124/mol.107.035170, ISSN: 0026-895X.
Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. J. Pharmacol. Exp. Ther [print-electronic]. 2007 Jul; 322(1): 254-64. PMID: 17416742, PII: jpet.106.117093, DOI: 10.1124/jpet.106.117093, ISSN: 0022-3565.
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, Conn PJ. Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol. Pharmacol [print-electronic]. 2007 May; 71(5): 1389-98. PMID: 17303702, PII: mol.106.032425, DOI: 10.1124/mol.106.032425, ISSN: 0026-895X.
Lindsley CW, Weaver D, Jones C, Marnett L, Conn PJ. Preclinical drug discovery research and training at Vanderbilt. ACS Chem. Biol. 2007 Jan 1/23/2007; 2(1): 17-20. PMID: 17243778, DOI: 10.1021/cb6004867, ISSN: 1554-8937.
Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, Tamagnan GD, Conn PJ. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol. Pharmacol [print-electronic]. 2006 Aug; 70(2): 616-26. PMID: 16645124, PII: mol.105.021857, DOI: 10.1124/mol.105.021857, ISSN: 0026-895X.
Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Tsou NN, Duggan ME, Conn PJ, Hartman GD. Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides. ChemMedChem. 2006 Aug; 1(8): 807-11. PMID: 16902933, DOI: 10.1002/cmdc.200600097, ISSN: 1860-7179.
Galici R, Jones CK, Hemstapat K, Nong Y, Echemendia NG, Williams LC, de Paulis T, Conn PJ. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J. Pharmacol. Exp. Ther [print-electronic]. 2006 Jul; 318(1): 173-85. PMID: 16608916, PII: jpet.106.102046, DOI: 10.1124/jpet.106.102046, ISSN: 0022-3565.
de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, Conn PJ. Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J. Med. Chem. 2006 Jun 6/1/2006; 49(11): 3332-44. PMID: 16722652, DOI: 10.1021/jm051252j, ISSN: 0022-2623.
Marino MJ, Conn PJ. Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. Curr Opin Pharmacol [print-electronic]. 2006 Feb; 6(1): 98-102. PMID: 16368268, PII: S1471-4892(05)00183-9, DOI: 10.1016/j.coph.2005.09.006, ISSN: 1471-4892.
Conn PJ, Niswender CM. MGluR7's lucky number. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2006 Jan 1/10/2006; 103(2): 251-2. PMID: 16407154, PMCID: PMC1326193, PII: 0510051103, DOI: 10.1073/pnas.0510051103, ISSN: 0027-8424.
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ. A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol. Pharmacol [print-electronic]. 2005 Dec; 68(6): 1793-802. PMID: 16155210, PII: mol.105.016139, DOI: 10.1124/mol.105.016139, ISSN: 0026-895X.
Zhang Y, Rodriguez AL, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Dec; 315(3): 1212-9. PMID: 16135701, PII: jpet.105.090308, DOI: 10.1124/jpet.105.090308, ISSN: 0022-3565.
Galici R, Echemendia NG, Rodriguez AL, Conn PJ. A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Dec; 315(3): 1181-7. PMID: 16123306, PII: jpet.105.091074, DOI: 10.1124/jpet.105.091074, ISSN: 0022-3565.
Conn PJ, Battaglia G, Marino MJ, Nicoletti F. Metabotropic glutamate receptors in the basal ganglia motor circuit. Nat. Rev. Neurosci. 2005 Oct; 6(10): 787-98. PMID: 16276355, PII: nrn1763, DOI: 10.1038/nrn1763, ISSN: 1471-003X.
Valenti O, Mannaioni G, Seabrook GR, Conn PJ, Marino MJ. Group III metabotropic glutamate-receptor-mediated modulation of excitatory transmission in rodent substantia nigra pars compacta dopamine neurons. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Jun; 313(3): 1296-304. PMID: 15761115, PII: jpet.104.080481, DOI: 10.1124/jpet.104.080481, ISSN: 0022-3565.
Wittmann M, Marino MJ, Henze DA, Seabrook GR, Conn PJ. Clozapine potentiation of N-methyl-D-aspartate receptor currents in the nucleus accumbens: role of NR2B and protein kinase A/Src kinases. J. Pharmacol. Exp. Ther [print-electronic]. 2005 May; 313(2): 594-603. PMID: 15659539, PII: jpet.104.080200, DOI: 10.1124/jpet.104.080200, ISSN: 0022-3565.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Apr; 313(1): 199-206. PMID: 15608073, PII: jpet.104.079244, DOI: 10.1124/jpet.104.079244, ISSN: 0022-3565.
Niswender CM, Jones CK, Conn PJ. New therapeutic frontiers for metabotropic glutamate receptors. Curr Top Med Chem. 2005; 5(9): 847-57. PMID: 16178730, ISSN: 1568-0266.
Alagarsamy S, Saugstad J, Warren L, Mansuy IM, Gereau RW, Conn PJ. NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin. Neuropharmacology. 2005; 49 Suppl 1: 135-45. PMID: 16005030, PMCID: PMC3799794, PII: S0028-3908(05)00188-7, DOI: 10.1016/j.neuropharm.2005.05.005, ISSN: 0028-3908.
Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y. Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology. 2005; 49 Suppl 1: 57-69. PMID: 15993439, PII: S0028-3908(05)00106-1, DOI: 10.1016/j.neuropharm.2005.03.006, ISSN: 0028-3908.
Doherty JJ, Alagarsamy S, Bough KJ, Conn PJ, Dingledine R, Mott DD. Metabotropic glutamate receptors modulate feedback inhibition in a developmentally regulated manner in rat dentate gyrus. J. Physiol. (Lond.) [print-electronic]. 2004 Dec 12/1/2004; 561(Pt 2): 395-401. PMID: 15513941, PMCID: PMC1665349, PII: jphysiol.2004.074930, DOI: 10.1113/jphysiol.2004.074930, ISSN: 0022-3751.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J. Med. Chem. 2004 Nov 11/18/2004; 47(24): 5825-8. PMID: 15537338, DOI: 10.1021/jm049400d, ISSN: 0022-2623.
Campbell UC, Lalwani K, Hernandez L, Kinney GG, Conn PJ, Bristow LJ. The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats. Psychopharmacology (Berl.). 2004 Sep; 175(3): 310-8. PMID: 15024550, DOI: 10.1007/s00213-004-1827-5, ISSN: 0033-3158.
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J. Pharmacol. Exp. Ther [print-electronic]. 2004 May; 309(2): 568-77. PMID: 14747613, PII: jpet.103.061747, DOI: 10.1124/jpet.103.061747, ISSN: 0022-3565.
Marino, M.J., Bradley, S.R. , Awad, H., Wittmann, M., Conn, P.J. Localization and physiological roles of metabotropic glutamate receptors in the indirect pathway of the basal ganglia. Movement Disorders. 2004; in press.
Williams JB, Mallorga PJ, Conn PJ, Pettibone DJ, Sur C.. Effects of typical and atypical antipsychotics on human glycine transporters. Schizophrenia Res. 2004; (in press).
Sur C, Mallorga PJ, Wittmann M, Jacobson MA, Pascarella D, Williams JB, Brandish PE, Pettibone DJ, Scolnick EM, Conn PJ. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Nov 11/11/2003; 100(23): 13674-9. PMID: 14595031, PMCID: PMC263872, PII: 1835612100, DOI: 10.1073/pnas.1835612100, ISSN: 0027-8424.
Marino MJ, Williams DL, O'Brien JA, Valenti O, McDonald TP, Clements MK, Wang R, DiLella AG, Hess JF, Kinney GG, Conn PJ. Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Nov 11/11/2003; 100(23): 13668-73. PMID: 14593202, PMCID: PMC263871, PII: 1835724100, DOI: 10.1073/pnas.1835724100, ISSN: 0027-8424.
Williams DL, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ. Difference in mGluR5 interaction between positive allosteric modulators from two structural classes. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 481-4. PMID: 14684495, ISSN: 0077-8923.
Valenti O, Marino MJ, Conn PJ. Modulation of excitatory transmission onto midbrain dopaminergic neurons of the rat by activation of group III metabotropic glutamate receptors. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 479-80. PMID: 14684494, ISSN: 0077-8923.
Marino MJ, Valenti O, O'Brien JA, Williams DL, Conn PJ. Modulation of inhibitory transmission in the rat globus pallidus by activation of mGluR4. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 435-7. PMID: 14684481, ISSN: 0077-8923.
Conn PJ. Physiological roles and therapeutic potential of metabotropic glutamate receptors. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 12-21. PMID: 14684432, ISSN: 0077-8923.
Junge CE, Sugawara T, Mannaioni G, Alagarsamy S, Conn PJ, Brat DJ, Chan PH, Traynelis SF. The contribution of protease-activated receptor 1 to neuronal damage caused by transient focal cerebral ischemia. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Oct 10/28/2003; 100(22): 13019-24. PMID: 14559973, PMCID: PMC240737, PII: 2235594100, DOI: 10.1073/pnas.2235594100, ISSN: 0027-8424.
Mallorga PJ, Williams JB, Jacobson M, Marques R, Chaudhary A, Conn PJ, Pettibone DJ, Sur C. Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine. Neuropharmacology. 2003 Oct; 45(5): 585-93. PMID: 12941372, PII: S0028390803002272, ISSN: 0028-3908.
O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol. Pharmacol. 2003 Sep; 64(3): 731-40. PMID: 12920211, PII: 64/3/731, DOI: 10.1124/mol.64.3.731, ISSN: 0026-895X.
Kinney GG, Sur C, Burno M, Mallorga PJ, Williams JB, Figueroa DJ, Wittmann M, Lemaire W, Conn PJ. The glycine transporter type 1 inhibitor N-[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy)propyl]sarcosine potentiates NMDA receptor-mediated responses in vivo and produces an antipsychotic profile in rodent behavior. J. Neurosci. 2003 Aug 8/20/2003; 23(20): 7586-91. PMID: 12930797, PII: 23/20/7586, ISSN: 1529-2401.
Valenti O, Marino MJ, Wittmann M, Lis E, DiLella AG, Kinney GG, Conn PJ. Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse. J. Neurosci. 2003 Aug 8/6/2003; 23(18): 7218-26. PMID: 12904482, PII: 23/18/7218, ISSN: 1529-2401.
Kinney GG, Burno M, Campbell UC, Hernandez LM, Rodriguez D, Bristow LJ, Conn PJ. Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents. J. Pharmacol. Exp. Ther [print-electronic]. 2003 Jul; 306(1): 116-23. PMID: 12660307, PII: jpet.103.048702, DOI: 10.1124/jpet.103.048702, ISSN: 0022-3565.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003 May; 44(6): 699-706. PMID: 12681368, PII: S0028390803000534, ISSN: 0028-3908.
Marino MJ, Valenti O, Conn PJ. Glutamate receptors and Parkinson's disease: opportunities for intervention. Drugs Aging. 2003; 20(5): 377-97. PMID: 12696997, PII: 2056, ISSN: 1170-229X.
Poisik OV, Mannaioni G, Traynelis S, Smith Y, Conn PJ. Distinct functional roles of the metabotropic glutamate receptors 1 and 5 in the rat globus pallidus. J. Neurosci. 2003 Jan 1/1/2003; 23(1): 122-30. PMID: 12514208, PII: 23/1/122, ISSN: 1529-2401.
Poisik, O., Marino, M.J. and Conn, P.J. Distinct functional roles of the group I metabotropic glutamate receptors 1 and 5 in the rat globus pallidus. J. Neurosci. 2003; 23((1)): 122-30.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003; 44((6)): 699-706.
Marino M, Valenti O, Conn PJ. Glutamate receptors and Parkinson's disease : opportunities for intervention. Drugs Aging. 2003; 20((5)): 377-97.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003; 44((6)): 699-706.
Williams, J., Mallorga, P., Patel, S., Conn, P.J., Pettibone, D., Austin, C. and Sur, C. Development of a scintillation proximity assay for analysis of Na+/Cl- dependent neurotransmitter transporter activity. Analytical Biochem. 2003; 321: 31-7.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors [editorial]. Pharmacol. Biochem. Behav. 2002 Dec; 74(1): 255-6. PMID: 12376174, PII: S009130570200953X, ISSN: 0091-3057.
Peavy RD, Sorensen SD, Conn PJ. Differential regulation of metabotropic glutamate receptor 5-mediated phosphoinositide hydrolysis and extracellular signal-regulated kinase responses by protein kinase C in cultured astrocytes. J. Neurochem. 2002 Oct; 83(1): 110-8. PMID: 12358734, PII: 1113, ISSN: 0022-3042.
Alagarsamy S, Rouse ST, Junge C, Hubert GW, Gutman D, Smith Y, Conn PJ. NMDA-induced phosphorylation and regulation of mGluR5. Pharmacol. Biochem. Behav. 2002 Sep; 73(2): 299-306. PMID: 12117583, PII: S0091305702008262, ISSN: 0091-3057.
Marino MJ, Awad-Granko H, Ciombor KJ, Conn PJ. Haloperidol-induced alteration in the physiological actions of group I mGlus in the subthalamic nucleus and the substantia nigra pars reticulata. Neuropharmacology. 2002 Aug; 43(2): 147-59. PMID: 12213269, PII: S0028390802000977, ISSN: 0028-3908.
Wittmann M, Marino MJ, Conn PJ. Dopamine modulates the function of group II and group III metabotropic glutamate receptors in the substantia nigra pars reticulata. J. Pharmacol. Exp. Ther. 2002 Aug; 302(2): 433-41. PMID: 12130700, DOI: 10.1124/jpet.102.033266, ISSN: 0022-3565.
Besong G, Battaglia G, D'Onofrio M, Di Marco R, Ngomba RT, Storto M, Castiglione M, Mangano K, Busceti CL, Nicoletti FR, Bacon K, Tusche M, Valenti O, Conn PJ, Bruno V, Nicoletti F. Activation of group III metabotropic glutamate receptors inhibits the production of RANTES in glial cell cultures. J. Neurosci. 2002 Jul 7/1/2002; 22(13): 5403-11. PMID: 12097492, PII: 22/13/5403, DOI: 20026585, ISSN: 1529-2401.
Sorensen SD, Macek TA, Cai Z, Saugstad JA, Conn PJ. Dissociation of protein kinase-mediated regulation of metabotropic glutamate receptor 7 (mGluR7) interactions with calmodulin and regulation of mGluR7 function. Mol. Pharmacol. 2002 Jun; 61(6): 1303-12. PMID: 12021391, ISSN: 0026-895X.
Scotland RS, Morales-Ruiz M, Chen Y, Yu J, Rudic RD, Fulton D, Gratton JP, Sessa WC. Functional reconstitution of endothelial nitric oxide synthase reveals the importance of serine 1179 in endothelium-dependent vasomotion. Circ. Res. 2002 May 5/3/2002; 90(8): 904-10. PMID: 11988492, ISSN: 1524-4571.
Fontana J, Fulton D, Chen Y, Fairchild TA, McCabe TJ, Fujita N, Tsuruo T, Sessa WC. Domain mapping studies reveal that the M domain of hsp90 serves as a molecular scaffold to regulate Akt-dependent phosphorylation of endothelial nitric oxide synthase and NO release. Circ. Res. 2002 May 5/3/2002; 90(8): 866-73. PMID: 11988487, ISSN: 1524-4571.
Valenti O, Conn PJ, Marino MJ. Distinct physiological roles of the Gq-coupled metabotropic glutamate receptors Co-expressed in the same neuronal populations. J. Cell. Physiol. 2002 May; 191(2): 125-37. PMID: 12064455, DOI: 10.1002/jcp.10081, ISSN: 0021-9541.
Saugstad JA, Yang S, Pohl J, Hall RA, Conn PJ. Interaction between metabotropic glutamate receptor 7 and alpha tubulin. J. Neurochem. 2002 Mar; 80(6): 980-8. PMID: 11953448, PMCID: PMC2925652, ISSN: 0022-3042.
Marino MJ, Conn PJ. Direct and indirect modulation of the N-methyl D-aspartate receptor. Curr Drug Targets CNS Neurol Disord. 2002 Feb; 1(1): 1-16. PMID: 12769631, ISSN: 1568-007X.
Marino MJ, Awad H, Poisik O, Wittmann M, Conn PJ. Localization and physiological roles of metabotropic glutamate receptors in the direct and indirect pathways of the basal ganglia. Amino Acids. 2002; 23(1-3): 185-91. PMID: 12373536, DOI: 10.1007/s00726-001-0127-1, ISSN: 0939-4451.
Sorensen SD, Macek TA, Cai Z, Saugstad JA, Conn PJ. Dissociation of protein kinase-mediated regulation of metabotropic glutamate receptor 7 (mGluR7) interactions with calmodulin and regulation of mGluR7 function. Mol Pharmacol. 2002; 61((6)): 1303-12.
Peavy RD, Chang MS, Sanders-Bush E, Conn PJ. Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor. J Neurosci. 2002; 21((24)): 9619-28.
Marino MJ, Conn PJ. Direct and indirect modulation of the N-Methyl D-Aspartate receptor. Curr Drug Target CNS Neurol Disord. 2002; 1((1)): 1.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors. Pharmacol Biochem Behav. 2002; 74((1)): 255-6.
Marino MJ, Conn P.J. Modulation of the Basal Ganglia by metabotropic glutamate receptors: potential for novel therapeutics. Curr Drug Target CNS Neurol Disord. 2002; 1((3)): 239-50.
Peavy RD, Chang MS, Sanders-Bush E, Conn PJ. Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor. J. Neurosci. 2001 Dec 12/15/2001; 21(24): 9619-28. PMID: 11739572, PII: 21/24/9619, ISSN: 1529-2401.
Marino MJ, Wittmann M, Bradley SR, Hubert GW, Smith Y, Conn PJ. Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata. J. Neurosci. 2001 Sep 9/15/2001; 21(18): 7001-12. PMID: 11549710, PII: 21/18/7001, ISSN: 1529-2401.
Zheng F, Erreger K, Low CM, Banke T, Lee CJ, Conn PJ, Traynelis SF. Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A. Nat. Neurosci. 2001 Sep; 4(9): 894-901. PMID: 11528420, PII: nn0901-894, DOI: 10.1038/nn0901-894, ISSN: 1097-6256.
Mannaioni G, Marino MJ, Valenti O, Traynelis SF, Conn PJ. Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function. J. Neurosci. 2001 Aug 8/15/2001; 21(16): 5925-34. PMID: 11487615, PII: 21/16/5925, ISSN: 1529-2401.
Cai Z, Saugstad JA, Sorensen SD, Ciombor KJ, Zhang C, Schaffhauser H, Hubalek F, Pohl J, Duvoisin RM, Conn PJ. Cyclic AMP-dependent protein kinase phosphorylates group III metabotropic glutamate receptors and inhibits their function as presynaptic receptors. J. Neurochem. 2001 Aug; 78(4): 756-66. PMID: 11520896, PMCID: PMC3799790, ISSN: 0022-3042.
Awad-Granko H, Conn PJ. Activation of groups I or III metabotropic glutamate receptors inhibits excitatory transmission in the rat subthalamic nucleus. Neuropharmacology. 2001 Jul; 41(1): 32-41. PMID: 11445183, PII: S0028390801000478, ISSN: 0028-3908.
Alagarsamy S, Sorensen SD, Conn PJ. Coordinate regulation of metabotropic glutamate receptors. Curr. Opin. Neurobiol. 2001 Jun; 11(3): 357-62. PMID: 11399435, PII: S0959-4388(00)00219-1, ISSN: 0959-4388.
Wittmann M, Marino MJ, Bradley SR, Conn PJ. Activation of group III mGluRs inhibits GABAergic and glutamatergic transmission in the substantia nigra pars reticulata. J. Neurophysiol. 2001 May; 85(5): 1960-8. PMID: 11353013, ISSN: 0022-3077.
De Blasi A, Conn PJ, Pin J, Nicoletti F. Molecular determinants of metabotropic glutamate receptor signaling. Trends Pharmacol. Sci. 2001 Mar; 22(3): 114-20. PMID: 11239574, PII: S0165614700016357, ISSN: 0165-6147.
Wittmann M, Hubert GW, Smith Y, Conn PJ. Activation of metabotropic glutamate receptor 1 inhibits glutamatergic transmission in the substantia nigra pars reticulata. Neuroscience. 2001; 105(4): 881-9. PMID: 11530226, PII: S0306452201002548, ISSN: 0306-4522.
Marino MJ, Wittmann M, Bradley SR, Hubert GW, Smith Y, Conn PJ. Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata. J Neurosci. 2001; 21((18)): 7001-12.
Zheng F, Erreger K, Low CM, Banke T, Lee CJ, Conn PJ, Traynelis SF. Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A. Nat Neurosci. 2001; 4((9)): 894-901.
Prince HC, Tzingounis AV, Levey AI, Conn PJ. Functional downregulation of GluR2 in piriform cortex of kindled animals. Synapse. 2000 Dec 12/15/2000; 38(4): 489-98. PMID: 11044897, PII: 10.1002/1098-2396(20001215)38:4<489::AID-SYN15>3.0.CO;2-N, DOI: 10.1002/1098-2396(20001215)38:4<489::AID-SYN15>3.0.CO;2-N, ISSN: 0887-4476.
Rouse ST, Marino MJ, Bradley SR, Awad H, Wittmann M, Conn PJ. Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders. Pharmacol. Ther. 2000 Dec; 88(3): 427-35. PMID: 11337032, PII: S016372580000098X, ISSN: 0163-7258.
Awad H, Hubert GW, Smith Y, Levey AI, Conn PJ. Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus. J. Neurosci. 2000 Nov 11/1/2000; 20(21): 7871-9. PMID: 11050106, PII: 20/21/7871, ISSN: 1529-2401.
Schaffhauser H, Cai Z, Hubalek F, Macek TA, Pohl J, Murphy TJ, Conn PJ. CAMP-dependent protein kinase inhibits mGluR2 coupling to G-proteins by direct receptor phosphorylation. J. Neurosci. 2000 Aug 8/1/2000; 20(15): 5663-70. PMID: 10908604, PII: 20/15/5663, ISSN: 0270-6474.
Bradley SR, Marino MJ, Wittmann M, Rouse ST, Awad H, Levey AI, Conn PJ. Activation of group II metabotropic glutamate receptors inhibits synaptic excitation of the substantia Nigra pars reticulata. J. Neurosci. 2000 May 5/1/2000; 20(9): 3085-94. PMID: 10777772, ISSN: 1529-2401.
Dingledine R, Conn PJ. Peripheral glutamate receptors: molecular biology and role in taste sensation. J. Nutr. 2000 Apr; 130(4S Suppl): 1039S-42S. PMID: 10736377, ISSN: 0022-3166.
Rouse ST, Hamilton SE, Potter LT, Nathanson NM, Conn PJ. Muscarinic-induced modulation of potassium conductances is unchanged in mouse hippocampal pyramidal cells that lack functional M1 receptors. Neurosci. Lett. 2000 Jan 1/7/2000; 278(1-2): 61-4. PMID: 10643801, PII: S0304-3940(99)00914-3, ISSN: 0304-3940.
Lie AA, Becker A, Behle K, Beck H, Malitschek B, Conn PJ, Kuhn R, Nitsch R, Plaschke M, Schramm J, Elger CE, Wiestler OD, Blümcke I. Up-regulation of the metabotropic glutamate receptor mGluR4 in hippocampal neurons with reduced seizure vulnerability. Ann. Neurol. 2000 Jan; 47(1): 26-35. PMID: 10632098, ISSN: 0364-5134.
Kosinski CM, Risso Bradley S, Conn PJ, Levey AI, Landwehrmeyer GB, Penney JB, Young AB, Standaert DG. Localization of metabotropic glutamate receptor 7 mRNA and mGluR7a protein in the rat basal ganglia. J. Comp. Neurol. 1999 Dec 12/13/1999; 415(2): 266-84. PMID: 10545164, PII: 10.1002/(SICI)1096-9861(19991213)415:2<266::AID-CNE9>3.0.CO;2-7, ISSN: 0021-9967.
Alagarsamy S, Rouse ST, Gereau RW, Heinemann SF, Smith Y, Conn PJ. Activation of N-methyl-D-aspartate receptors reverses desensitization of metabotropic glutamate receptor, mGluR5, in native and recombinant systems. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 526-30. PMID: 10414329, ISSN: 0077-8923.
Macek TA, Schaffhauser H, Conn PJ. Activation of PKC disrupts presynaptic inhibition by group II and group III metabotropic glutamate receptors and uncouples the receptor from GTP-binding proteins. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 554-7. PMID: 10414335, ISSN: 0077-8923.
Bradley SR, Standaert DG, Levey AI, Conn PJ. Distribution of group III mGluRs in rat basal ganglia with subtype-specific antibodies. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 531-4. PMID: 10414330, ISSN: 0077-8923.
Bradley SR, Standaert DG, Rhodes KJ, Rees HD, Testa CM, Levey AI, Conn PJ. Immunohistochemical localization of subtype 4a metabotropic glutamate receptors in the rat and mouse basal ganglia. J. Comp. Neurol. 1999 Apr 4/28/1999; 407(1): 33-46. PMID: 10213186, PII: 10.1002/(SICI)1096-9861(19990428)407:1<33::AID-CNE3>3.0.CO;2-G, ISSN: 0021-9967.
Alagarsamy S, Marino MJ, Rouse ST, Gereau RW, Heinemann SF, Conn PJ. Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems. Nat. Neurosci. 1999 Mar; 2(3): 234-40. PMID: 10195215, DOI: 10.1038/6338, ISSN: 1097-6256.
Hay M, McKenzie H, Lindsley K, Dietz N, Bradley SR, Conn PJ, Hasser EM. Heterogeneity of metabotropic glutamate receptors in autonomic cell groups of the medulla oblongata of the rat. J. Comp. Neurol. 1999 Jan 1/25/1999; 403(4): 486-501. PMID: 9888314, PII: 10.1002/(SICI)1096-9861(19990125)403:4<486::AID-CNE5>3.0.CO;2-9, ISSN: 0021-9967.
Paradee W, Melikian HE, Rasmussen DL, Kenneson A, Conn PJ, Warren ST. Fragile X mouse: strain effects of knockout phenotype and evidence suggesting deficient amygdala function. Neuroscience. 1999; 94(1): 185-92. PMID: 10613508, PII: S0306-4522(99)00285-7, ISSN: 0306-4522.
Rouse ST, Marino MJ, Potter LT, Conn PJ, Levey AI. Muscarinic receptor subtypes involved in hippocampal circuits. Life Sci. 1999; 64(6-7): 501-9. PMID: 10069516, ISSN: 0024-3205.
Khawaja XZ, Liang JJ, Saugstad JA, Jones PG, Harnish S, Conn PJ, Cockett MI. Immunohistochemical distribution of RGS7 protein and cellular selectivity in colocalizing with Galphaq proteins in the adult rat brain. J. Neurochem. 1999 Jan; 72(1): 174-84. PMID: 9886068, ISSN: 0022-3042.
Marino MJ, Rouse ST, Levey AI, Potter LT, Conn PJ. Activation of the genetically defined m1 muscarinic receptor potentiates N-methyl-D-aspartate (NMDA) receptor currents in hippocampal pyramidal cells. Proc. Natl. Acad. Sci. U.S.A. 1998 Sep 9/15/1998; 95(19): 11465-70. PMID: 9736760, PMCID: PMC21666, ISSN: 0027-8424.
Macek TA, Schaffhauser H, Conn PJ. Protein kinase C and A3 adenosine receptor activation inhibit presynaptic metabotropic glutamate receptor (mGluR) function and uncouple mGluRs from GTP-binding proteins. J. Neurosci. 1998 Aug 8/15/1998; 18(16): 6138-46. PMID: 9698308, ISSN: 0270-6474.
Bradley SR, Rees HD, Yi H, Levey AI, Conn PJ. Distribution and developmental regulation of metabotropic glutamate receptor 7a in rat brain. J. Neurochem. 1998 Aug; 71(2): 636-45. PMID: 9681454, ISSN: 0022-3042.
Peavy RD, Conn PJ. Phosphorylation of mitogen-activated protein kinase in cultured rat cortical glia by stimulation of metabotropic glutamate receptors. J. Neurochem. 1998 Aug; 71(2): 603-12. PMID: 9681450, ISSN: 0022-3042.
Zheng F, Gingrich MB, Traynelis SF, Conn PJ. Tyrosine kinase potentiates NMDA receptor currents by reducing tonic zinc inhibition. Nat. Neurosci. 1998 Jul; 1(3): 185-91. PMID: 10195142, PII: 634, DOI: 10.1038/634, ISSN: 1097-6256.
Saugstad JA, Marino MJ, Folk JA, Hepler JR, Conn PJ. RGS4 inhibits signaling by group I metabotropic glutamate receptors. J. Neurosci. 1998 Feb 2/1/1998; 18(3): 905-13. PMID: 9437012, ISSN: 0270-6474.
Chung DS, Traynelis SF, Murphy TJ, Conn PJ. 4-Methylhomoibotenic acid activates a novel metabotropic glutamate receptor coupled to phosphoinositide hydrolysis. J. Pharmacol. Exp. Ther. 1997 Nov; 283(2): 742-9. PMID: 9353394, ISSN: 0022-3565.
Chen YT, Henk MJ, Carney KJ, Wong WD, Rothenberger DA, Zheng T, Feygin M, Madoff RD. Prognostic significance of tumor markers in colorectal cancer patients: DNA index, S-phase fraction, p53 expression, and Ki-67 index. J. Gastrointest. Surg. 1997 May; 1(3): 266-72; discussion 273. PMID: 9834357, PII: S1091-255X(97)80119-9, ISSN: 1091-255X.
Miller HP, Levey AI, Rothstein JD, Tzingounis AV, Conn PJ. Alterations in glutamate transporter protein levels in kindling-induced epilepsy. J. Neurochem. 1997 Apr; 68(4): 1564-70. PMID: 9084427, ISSN: 0022-3042.
Conn PJ, Pin JP. Pharmacology and functions of metabotropic glutamate receptors. Annu. Rev. Pharmacol. Toxicol. 1997; 37: 205-37. PMID: 9131252, DOI: 10.1146/annurev.pharmtox.37.1.205, ISSN: 0362-1642.
Macek TA, Winder DG, Gereau RW, Ladd CO, Conn PJ. Differential involvement of group II and group III mGluRs as autoreceptors at lateral and medial perforant path synapses. J. Neurophysiol. 1996 Dec; 76(6): 3798-806. PMID: 8985877, ISSN: 0022-3077.
Winder DG, Conn PJ. Roles of metabotropic glutamate receptors in glial function and glial-neuronal communication. J. Neurosci. Res. 1996 Oct 10/15/1996; 46(2): 131-7. PMID: 8915890, PII: 10.1002/(SICI)1097-4547(19961015)46:2<131::AID-JNR1>3.0.CO;2-I, DOI: 10.1002/(SICI)1097-4547(19961015)46:2<131::AID-JNR1>3.0.CO;2-I, ISSN: 0360-4012.
Winder DG, Ritch PS, Gereau RW, Conn PJ. Novel glial-neuronal signalling by coactivation of metabotropic glutamate and beta-adrenergic receptors in rat hippocampus. J. Physiol. (Lond.). 1996 Aug 8/1/1996; 494 ( Pt 3): 743-55. PMID: 8865071, PMCID: PMC1160674, ISSN: 0022-3751.
Bradley SR, Levey AI, Hersch SM, Conn PJ. Immunocytochemical localization of group III metabotropic glutamate receptors in the hippocampus with subtype-specific antibodies. J. Neurosci. 1996 Mar 3/15/1996; 16(6): 2044-56. PMID: 8604049, ISSN: 0270-6474.
Gereau RW, Conn PJ. Multiple presynaptic metabotropic glutamate receptors modulate excitatory and inhibitory synaptic transmission in hippocampal area CA1. J. Neurosci. 1995 Oct; 15(10): 6879-89. PMID: 7472445, ISSN: 0270-6474.
Gereau RW, Conn PJ. Roles of specific metabotropic glutamate receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability. J. Neurophysiol. 1995 Jul; 74(1): 122-9. PMID: 7472317, ISSN: 0022-3077.
Gereau RW, Winder DG, Conn PJ. Pharmacological differentiation of the effects of co-activation of beta-adrenergic and metabotropic glutamate receptors in rat hippocampus. Neurosci. Lett. 1995 Feb 2/17/1995; 186(2-3): 119-22. PMID: 7777178, ISSN: 0304-3940.
Winder DG, Conn PJ. Metabotropic glutamate receptor (mGluR)-mediated potentiation of cyclic AMP responses does not require phosphoinositide hydrolysis: mediation by a group II-like mGluR. J. Neurochem. 1995 Feb; 64(2): 592-9. PMID: 7830052, ISSN: 0022-3042.
Prince HK, Conn PJ, Blackstone CD, Huganir RL, Levey AI. Down-regulation of AMPA receptor subunit GluR2 in amygdaloid kindling. J. Neurochem. 1995 Jan; 64(1): 462-5. PMID: 7798948, ISSN: 0022-3042.
Desai MA, McBain CJ, Kauer JA, Conn PJ. Metabotropic glutamate receptor-induced disinhibition is mediated by reduced transmission at excitatory synapses onto interneurons and inhibitory synapses onto pyramidal cells. Neurosci. Lett. 1994 Nov 11/7/1994; 181(1-2): 78-82. PMID: 7898776, ISSN: 0304-3940.
Gereau RW, Conn PJ. Presynaptic enhancement of excitatory synaptic transmission by beta-adrenergic receptor activation. J. Neurophysiol. 1994 Sep; 72(3): 1438-42. PMID: 7807226, ISSN: 0022-3077.
Chung DS, Winder DG, Conn PJ. 4-Bromohomoibotenic acid selectively activates a 1-aminocyclopentane-1S,3R-dicarboxylic acid-insensitive metabotropic glutamate receptor coupled to phosphoinositide hydrolysis in rat cortical slices. J. Neurochem. 1994 Jul; 63(1): 133-9. PMID: 8207423, ISSN: 0022-3042.
Boss V, Nutt KM, Conn PJ. L-cysteine sulfinic acid as an endogenous agonist of a novel metabotropic receptor coupled to stimulation of phospholipase D activity. Mol. Pharmacol. 1994 Jun; 45(6): 1177-82. PMID: 8022410, ISSN: 0026-895X.
Gereau RW, Conn PJ. Potentiation of cAMP responses by metabotropic glutamate receptors depresses excitatory synaptic transmission by a kinase-independent mechanism. Neuron. 1994 May; 12(5): 1121-9. PMID: 8185947, PII: 0896-6273(94)90319-0, ISSN: 0896-6273.
Gereau RW, Conn PJ. A cyclic AMP-dependent form of associative synaptic plasticity induced by coactivation of beta-adrenergic receptors and metabotropic glutamate receptors in rat hippocampus. J. Neurosci. 1994 May; 14(5 Pt 2): 3310-8. PMID: 8182474, ISSN: 0270-6474.
Winder DG, Smith T, Conn PJ. Pharmacological differentiation of metabotropic glutamate receptors coupled to potentiation of cyclic adenosine monophosphate responses and phosphoinositide hydrolysis. J. Pharmacol. Exp. Ther. 1993 Aug; 266(2): 518-25. PMID: 8394908, ISSN: 0022-3565.
Winder DG, Conn PJ. Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to endogenous adenosine. J. Neurosci. 1993 Jan; 13(1): 38-44. PMID: 8380851, ISSN: 0270-6474.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors in brain function and pathology. Trends Pharmacol. Sci. 1993 Jan; 14(1): 13-20. PMID: 7680175, ISSN: 0165-6147.
Boss V, Conn PJ. Metabotropic excitatory amino acid receptor activation stimulates phospholipase D in hippocampal slices. J. Neurochem. 1992 Dec; 59(6): 2340-3. PMID: 1431912, ISSN: 0022-3042.
Chen SJ, Desai MA, Klann E, Winder DG, Sweatt JD, Conn PJ. Amygdala kindling alters protein kinase C activity in dentate gyrus. J. Neurochem. 1992 Nov; 59(5): 1761-9. PMID: 1402921, ISSN: 0022-3042.
Desai MA, Smith TS, Conn PJ. Multiple metabotropic glutamate receptors regulate hippocampal function. Synapse. 1992 Nov; 12(3): 206-13. PMID: 1336225, DOI: 10.1002/syn.890120305, ISSN: 0887-4476.
Boss V, Desai MA, Smith TS, Conn PJ. Trans-ACPD-induced phosphoinositide hydrolysis and modulation of hippocampal pyramidal cell excitability do not undergo parallel developmental regulation. Brain Res. 1992 Oct 10/30/1992; 594(2): 181-8. PMID: 1360322, PII: 0006-8993(92)91124-W, ISSN: 0006-8993.
Winder DG, Conn PJ. Activation of metabotropic glutamate receptors in the hippocampus increases cyclic AMP accumulation. J. Neurochem. 1992 Jul; 59(1): 375-8. PMID: 1351930, ISSN: 0022-3042.
Desai MA, Conn PJ. Excitatory effects of ACPD receptor activation in the hippocampus are mediated by direct effects on pyramidal cells and blockade of synaptic inhibition. J. Neurophysiol. 1991 Jul; 66(1): 40-52. PMID: 1655995, ISSN: 0022-3077.
Desai MA, Conn PJ. Selective activation of phosphoinositide hydrolysis by a rigid analogue of glutamate. Neurosci. Lett. 1990 Feb 2/5/1990; 109(1-2): 157-62. PMID: 1969130, PII: 0304-3940(90)90555-N, ISSN: 0304-3940.
Conn PJ, Strong JA, Kaczmarek LK. Inhibitors of protein kinase C prevent enhancement of calcium current and action potentials in peptidergic neurons of Aplysia. J. Neurosci. 1989 Feb; 9(2): 480-7. PMID: 2918372, ISSN: 0270-6474.
Conn PJ, Strong JA, Azhderian EM, Nairn AC, Greengard P, Kaczmarek LK. Protein kinase inhibitors selectively block phorbol ester- or forskolin-induced changes in excitability of Aplysia neurons. J. Neurosci. 1989 Feb; 9(2): 473-9. PMID: 2537389, ISSN: 0270-6474.
Conn PJ, Kaczmarek LK. The bag cell neurons of Aplysia. A model for the study of the molecular mechanisms involved in the control of prolonged animal behaviors. Mol. Neurobiol. 1989; 3(4): 237-73. PMID: 2698177, DOI: 10.1007/BF02740607, ISSN: 0893-7648.
Conn PJ, Sanders-Bush E. Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors. J. Pharmacol. Exp. Ther. 1987 Aug; 242(2): 552-7. PMID: 3039120, ISSN: 0022-3565.
Conn PJ, Janowsky A, Sanders-Bush E. Denervation supersensitivity of 5-HT-1c receptors in rat choroid plexus. Brain Res. 1987 Jan 1/6/1987; 400(2): 396-8. PMID: 3815085, PII: 0006-8993(87)90641-X, ISSN: 0006-8993.
Conn PJ, Sanders-Bush E. Central serotonin receptors: effector systems, physiological roles and regulation. Psychopharmacology (Berl.). 1987; 92(3): 267-77. PMID: 2819915, ISSN: 0033-3158.
Conn PJ, Sanders-Bush E. Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site. J. Neurosci. 1986 Dec; 6(12): 3669-75. PMID: 3025382, ISSN: 0270-6474.
Conn PJ, Sanders-Bush E. Agonist-induced phosphoinositide hydrolysis in choroid plexus. J. Neurochem. 1986 Dec; 47(6): 1754-60. PMID: 3021903, ISSN: 0022-3042.
Conn PJ, Sanders-Bush E, Hoffman BJ, Hartig PR. A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover. Proc. Natl. Acad. Sci. U.S.A. 1986 Jun; 83(11): 4086-8. PMID: 2940597, PMCID: PMC323671, ISSN: 0027-8424.
Conn PJ, Sanders-Bush E. Biochemical characterization of serotonin stimulated phosphoinositide turnover. Life Sci. 1986 Feb 2/17/1986; 38(7): 663-9. PMID: 3003490, ISSN: 0024-3205.
Sanders-Bush E, Conn PJ. Effector systems coupled to serotonin receptors in brain: serotonin stimulated phosphoinositide hydrolysis. Psychopharmacol Bull. 1986; 22(3): 829-36. PMID: 3025911, ISSN: 0048-5764.
Conn PJ, Sanders-Bush E. Serotonin-stimulated phosphoinositide turnover: mediation by the S2 binding site in rat cerebral cortex but not in subcortical regions. J. Pharmacol. Exp. Ther. 1985 Jul; 234(1): 195-203. PMID: 2989504, ISSN: 0022-3565.
Conn PJ, Sanders-Bush E. Selective 5HT-2 antagonists inhibit serotonin stimulated phosphatidylinositol metabolism in cerebral cortex. Neuropharmacology. 1984 Aug; 23(8): 993-6. PMID: 6483122, ISSN: 0028-3908.
Stansley BJ, Conn PJ. The therapeutic potential of metabotropic glutamate receptor modulation for schizophrenia. Curr Opin Pharmacol [print-electronic]. 2018 Feb 2/24/2018; 38: 31-6. PMID: 29486374, PII: S1471-4892(17)30063-2, DOI: 10.1016/j.coph.2018.02.003, ISSN: 1471-4973.
Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology [print-electronic]. 2017 Mar 3/15/2017; 115: 60-72. PMID: 27392634, PMCID: PMC5217481, PII: S0028-3908(16)30287-8, DOI: 10.1016/j.neuropharm.2016.07.001, ISSN: 1873-7064.
Ade KK, Wan Y, Hamann HC, O'Hare JK, Guo W, Quian A, Kumar S, Bhagat S, Rodriguiz RM, Wetsel WC, Conn PJ, Dzirasa K, Huber KM, Calakos N. Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice. Biol. Psychiatry [print-electronic]. 2016 Oct 10/1/2016; 80(7): 522-33. PMID: 27436084, PMCID: PMC5536332, PII: S0006-3223(16)32380-0, DOI: 10.1016/j.biopsych.2016.04.023, ISSN: 1873-2402.
Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Aug 8/1/2016; 26(15): 3822-5. PMID: 27173801, PMCID: PMC5082649, PII: S0960-894X(16)30472-3, DOI: 10.1016/j.bmcl.2016.04.083, ISSN: 1464-3405.
Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ. Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. ACS Chem. Biol [print-electronic]. 2016 Jul 7/15/2016; 11(7): 1870-9. PMID: 27115427, PMCID: PMC4981245, DOI: 10.1021/acschembio.6b00026, ISSN: 1554-8937.
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jul 7/1/2016; 26(13): 2984-7. PMID: 27234146, PMCID: PMC4955388, PII: S0960-894X(16)30514-5, DOI: 10.1016/j.bmcl.2016.05.029, ISSN: 1464-3405.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jul 7/1/2016; 26(13): 3029-33. PMID: 27185330, PMCID: PMC4955361, PII: S0960-894X(16)30490-5, DOI: 10.1016/j.bmcl.2016.05.010, ISSN: 1464-3405.
Balu DT, Li Y, Takagi S, Presti KT, Ramikie TS, Rook JM, Jones CK, Lindsley CW, Conn PJ, Bolshakov VY, Coyle JT. An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia. Neuropsychopharmacology [print-electronic]. 2016 Jul; 41(8): 2052-61. PMID: 26741285, PMCID: PMC4908650, PII: npp20162, DOI: 10.1038/npp.2016.2, ISSN: 1740-634X.
Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jun 6/15/2016; 26(12): 2915-9. PMID: 27131990, PMCID: PMC4899947, PII: S0960-894X(16)30414-0, DOI: 10.1016/j.bmcl.2016.04.041, ISSN: 1464-3405.
Ponnazhagan R, Harms AS, Thome AD, Jurkuvenaite A, Gogliotti R, Niswender CM, Conn PJ, Standaert DG. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol [print-electronic]. 2016 Jun; 11(2): 231-7. PMID: 26872456, PMCID: PMC4848139, PII: 10.1007/s11481-016-9655-z, DOI: 10.1007/s11481-016-9655-z, ISSN: 1557-1904.
Gogliotti RG, Senter RK, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones CK, Lindsley CW, Conn PJ, Niswender CM. MGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome. Hum. Mol. Genet [print-electronic]. 2016 May 5/15/2016; 25(10): 1990-2004. PMID: 26936821, PMCID: PMC5062588, PII: ddw074, DOI: 10.1093/hmg/ddw074, ISSN: 1460-2083.
O'Brien DE, Conn PJ. Neurobiological Insights from mGlu Receptor Allosteric Modulation. Int. J. Neuropsychopharmacol [electronic-print]. 2016 May; 19(5): PMID: 26647381, PMCID: PMC4886670, PII: pyv133, DOI: 10.1093/ijnp/pyv133, ISSN: 1469-5111.
Dean B, Hopper S, Conn PJ, Scarr E. Changes in BQCA Allosteric Modulation of [(3)H]NMS Binding to Human Cortex within Schizophrenia and by Divalent Cations. Neuropsychopharmacology [print-electronic]. 2016 May; 41(6): 1620-8. PMID: 26511338, PMCID: PMC4832025, PII: npp2015330, DOI: 10.1038/npp.2015.330, ISSN: 1740-634X.
Garcia-Barrantes PM, Cho HP, Starr TM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR. Bioorg. Med. Chem. Lett [print-electronic]. 2016 May 5/1/2016; 26(9): 2289-92. PMID: 27013388, PMCID: PMC4833523, PII: S0960-894X(16)30264-5, DOI: 10.1016/j.bmcl.2016.03.044, ISSN: 1464-3405.
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Apr 4/15/2016; 26(8): 1894-900. PMID: 26988308, PMCID: PMC4824313, PII: S0960-894X(16)30246-3, DOI: 10.1016/j.bmcl.2016.03.026, ISSN: 1464-3405.
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Apr 4/15/2016; 26(8): 1869-72. PMID: 26988302, PMCID: PMC4823774, PII: S0960-894X(16)30251-7, DOI: 10.1016/j.bmcl.2016.03.031, ISSN: 1464-3405.
Xiang Z, Conn PJ. Novel PAMs Targeting NMDAR GluN2A Subunit. Neuron. 2016 Mar 3/2/2016; 89(5): 884-6. PMID: 26938436, PMCID: PMC4793964, PII: S0896-6273(16)00142-2, DOI: 10.1016/j.neuron.2016.02.025, ISSN: 1097-4199.
Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, Lindsley CW, Conn PJ, Jones CK. State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects. Neuropharmacology [print-electronic]. 2016 Mar; 102: 244-53. PMID: 26617071, PMCID: PMC4809053, PII: S0028-3908(15)30180-5, DOI: 10.1016/j.neuropharm.2015.11.016, ISSN: 1873-7064.
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW, Jones CK. Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. Neuropsychopharmacology [print-electronic]. 2016 Mar; 41(4): 1166-78. PMID: 26315507, PMCID: PMC4748441, PII: npp2015265, DOI: 10.1038/npp.2015.265, ISSN: 1740-634X.
Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Feb 2/1/2016; 26(3): 751-6. PMID: 26778256, PMCID: PMC4794757, PII: S0960-894X(15)30417-0, DOI: 10.1016/j.bmcl.2015.12.104, ISSN: 1464-3405.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM. Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. Bioorg. Med. Chem. Lett [print-electronic]. 2016 Jan 1/15/2016; 26(2): 429-34. PMID: 26684851, PMCID: PMC4835042, PII: S0960-894X(15)30306-1, DOI: 10.1016/j.bmcl.2015.11.098, ISSN: 1464-3405.
Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ. VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy. J. Pharmacol. Exp. Ther [print-electronic]. 2016 Jan; 356(1): 123-36. PMID: 26503377, PMCID: PMC4702078, PII: jpet.115.226597, DOI: 10.1124/jpet.115.226597, ISSN: 1521-0103.
Ghoshal A, Rook JM, Dickerson JW, Roop GN, Morrison RD, Jalan-Sakrikar N, Lamsal A, Noetzel MJ, Poslusney MS, Wood MR, Melancon BJ, Stauffer SR, Xiang Z, Daniels JS, Niswender CM, Jones CK, Lindsley CW, Conn PJ. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology [print-electronic]. 2016 Jan; 41(2): 598-610. PMID: 26108886, PMCID: PMC5130135, PII: npp2015189, DOI: 10.1038/npp.2015.189, ISSN: 1740-634X.
Senter RK, Ghoshal A, Walker AG, Xiang Z, Niswender CM, Conn PJ. The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies. Curr Neuropharmacol. 2016; 14(5): 455-73. PMID: 27296640, PMCID: PMC4983746, PII: CN-EPUB-66683, ISSN: 1875-6190.
Gogliotti RG, Conn PJ. Pharmacological Treatments for Autism Spectrum Disorder: Will Emerging Approaches Yield New Treatments?. Neuropsychopharmacology. 2016 Jan; 41(1): 376-7. PMID: 26657955, PMCID: PMC4677143, PII: npp2015259, DOI: 10.1038/npp.2015.259, ISSN: 1740-634X.
Garcia RC, Dati LM, Torres LH, da Silva MA, Udo MS, Abdalla FM, da Costa JL, Gorjão R, Afeche SC, Yonamine M, Niswender CM, Conn PJ, Camarini R, Sandoval MR, Marcourakis T. M1 and M3 muscarinic receptors may play a role in the neurotoxicity of anhydroecgonine methyl ester, a cocaine pyrolysis product. Sci Rep. 2015 Dec 12/2/2015; 5: 17555. PMID: 26626425, PMCID: PMC4667193, PII: srep17555, DOI: 10.1038/srep17555, ISSN: 2045-2322.
Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2. J. Med. Chem [print-electronic]. 2015 Nov 11/25/2015; 58(22): 9027-40. PMID: 26524606, PMCID: PMC4817271, DOI: 10.1021/acs.jmedchem.5b01371, ISSN: 1520-4804.
Shen W, Plotkin JL, Francardo V, Ko WK, Xie Z, Li Q, Fieblinger T, Wess J, Neubig RR, Lindsley CW, Conn PJ, Greengard P, Bezard E, Cenci MA, Surmeier DJ. M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia. Neuron. 2015 Nov 11/18/2015; 88(4): 762-73. PMID: 26590347, PMCID: PMC4864040, PII: S0896-6273(15)00933-2, DOI: 10.1016/j.neuron.2015.10.039, ISSN: 1097-4199.
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Nov 11/15/2015; 25(22): 5107-10. PMID: 26476971, PMCID: PMC4758672, PII: S0960-894X(15)30121-9, DOI: 10.1016/j.bmcl.2015.10.013, ISSN: 1464-3405.
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Nov 11/15/2015; 25(22): 5115-20. PMID: 26475522, PMCID: PMC4634704, PII: S0960-894X(15)30118-9, DOI: 10.1016/j.bmcl.2015.10.009, ISSN: 1464-3405.
Pancani T, Foster DJ, Moehle MS, Bichell TJ, Bradley E, Bridges TM, Klar R, Poslusney M, Rook JM, Daniels JS, Niswender CM, Jones CK, Wood MR, Bowman AB, Lindsley CW, Xiang Z, Conn PJ. Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2015 Nov 11/10/2015; 112(45): 14078-83. PMID: 26508634, PMCID: PMC4653197, PII: 1512812112, DOI: 10.1073/pnas.1512812112, ISSN: 1091-6490.
Frye SV, Arkin MR, Arrowsmith CH, Conn PJ, Glicksman MA, Hull-Ryde EA, Slusher BS. Tackling reproducibility in academic preclinical drug discovery. Nat Rev Drug Discov [print-electronic]. 2015 Nov; 14(11): 733-4. PMID: 26388229, PII: nrd4737, DOI: 10.1038/nrd4737, ISSN: 1474-1784.
Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS. A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo. Drug Metab. Dispos [print-electronic]. 2015 Nov; 43(11): 1718-26. PMID: 26265743, PMCID: PMC4613951, PII: dmd.115.064006, DOI: 10.1124/dmd.115.064006, ISSN: 1521-009X.
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW. Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics. J. Med. Chem [print-electronic]. 2015 Oct 10/22/2015; 58(20): 7959-71. PMID: 26426481, PMCID: PMC4839290, DOI: 10.1021/acs.jmedchem.5b00727, ISSN: 1520-4804.
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J. Med. Chem [print-electronic]. 2015 Sep 9/24/2015; 58(18): 7485-500. PMID: 26335039, PMCID: PMC4809247, DOI: 10.1021/acs.jmedchem.5b01005, ISSN: 1520-4804.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound. Bioorg. Med. Chem. Lett [print-electronic]. 2015 Sep 9/1/2015; 25(17): 3515-9. PMID: 26183084, PMCID: PMC4535329, PII: S0960-894X(15)00701-5, DOI: 10.1016/j.bmcl.2015.06.096, ISSN: 1464-3405.
Burket JA, Benson AD, Green TL, Rook JM, Lindsley CW, Conn PJ, Deutsch SI. Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism. Prog. Neuropsychopharmacol. Biol. Psychiatry [print-electronic]. 2015 Aug 8/3/2015; 61: 10-7. PMID: 25784602, PII: S0278-5846(15)00052-4, DOI: 10.1016/j.pnpbp.2015.03.003, ISSN: 1878-4216.
Smith E, Chase P, Niswender CM, Utley TJ, Sheffler DJ, Noetzel MJ, Lamsal A, Wood MR, Conn PJ, Lindsley CW, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P. Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4). J Biomol Screen [print-electronic]. 2015 Aug; 20(7): 858-68. PMID: 25877150, PMCID: PMC4659430, PII: 1087057115581770, DOI: 10.1177/1087057115581770, ISSN: 1552-454X.
Iderberg H, Maslava N, Thompson AD, Bubser M, Niswender CM, Hopkins CR, Lindsley CW, Conn PJ, Jones CK, Cenci MA. Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist. Neuropharmacology [print-electronic]. 2015 Aug; 95: 121-9. PMID: 25749357, PMCID: PMC4466038, PII: S0028-3908(15)00079-9, DOI: 10.1016/j.neuropharm.2015.02.023, ISSN: 1873-7064.
Brown JH, Catterall WA, Conn PJ, Cull-Candy SG, Dingledine R, Harden TK, Insel PA, Milligan G, Traynelis SF. The First 50 Years of Molecular Pharmacology. Mol. Pharmacol [print-electronic]. 2015 Jul; 88(1): 139-40. PMID: 25943115, PII: mol.115.099564, DOI: 10.1124/mol.115.099564, ISSN: 1521-0111.
Gregory KJ, Conn PJ. Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation. Mol. Pharmacol [print-electronic]. 2015 Jul; 88(1): 188-202. PMID: 25808929, PMCID: PMC4468636, PII: mol.114.097220, DOI: 10.1124/mol.114.097220, ISSN: 1521-0111.
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015 Jun 6/11/2015; 6(6): 716-20. PMID: 26157544, PMCID: PMC4492464, DOI: 10.1021/acsmedchemlett.5b00181, ISSN: 1948-5875.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA, . Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 2015 Jun 6/4/2015; 161(6): 1252-65. PMID: 26046436, PMCID: PMC4564295, PII: S0092-8674(15)00572-3, DOI: 10.1016/j.cell.2015.05.023, ISSN: 1097-4172.
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ. Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents. Neuron [print-electronic]. 2015 May 5/20/2015; 86(4): 1029-40. PMID: 25937172, PMCID: PMC4443790, PII: S0896-6273(15)00287-1, DOI: 10.1016/j.neuron.2015.03.063, ISSN: 1097-4199.
Klar R, Walker AG, Ghose D, Grueter BA, Engers DW, Hopkins CR, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. J. Neurosci. 2015 May 5/13/2015; 35(19): 7600-15. PMID: 25972184, PMCID: PMC4429158, PII: 35/19/7600, DOI: 10.1523/JNEUROSCI.4543-14.2015, ISSN: 1529-2401.
Nedelcovych MT, Gould RW, Zhan X, Bubser M, Gong X, Grannan M, Thompson AT, Ivarsson M, Lindsley CW, Conn PJ, Jones CK. A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances. ACS Chem Neurosci [print-electronic]. 2015 Mar 3/18/2015; 6(3): 485-93. PMID: 25581551, PMCID: PMC4403733, DOI: 10.1021/cn500342u, ISSN: 1948-7193.
Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg. Med. Chem. Lett [print-electronic]. 2015 Mar 3/15/2015; 25(6): 1310-7. PMID: 25683622, PMCID: PMC4399811, PII: S0960-894X(15)00050-5, DOI: 10.1016/j.bmcl.2015.01.038, ISSN: 1464-3405.
Walker AG, Wenthur CJ, Xiang Z, Rook JM, Emmitte KA, Niswender CM, Lindsley CW, Conn PJ. Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2015 Jan 1/27/2015; 112(4): 1196-201. PMID: 25583490, PMCID: PMC4313856, PII: 1416196112, DOI: 10.1073/pnas.1416196112, ISSN: 1091-6490.
Ghoshal A, Conn PJ. The hippocampo-prefrontal pathway: a possible therapeutic target for negative and cognitive symptoms of schizophrenia. Future Neurol. 2015; 10(2): 115-28. PMID: 25825588, PMCID: PMC4376007, DOI: 10.2217/FNL.14.63, ISSN: 1479-6708.
Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe. ChemMedChem [print-electronic]. 2014 Aug; 9(8): 1677-82. PMID: 24692176, PMCID: PMC4116439, DOI: 10.1002/cmdc.201402051, ISSN: 1860-7187.
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol. Pharmacol [print-electronic]. 2009 Aug; 76(2): 356-68. PMID: 19407080, PMCID: PMC2713127, PII: mol.109.056531, DOI: 10.1124/mol.109.056531, ISSN: 1521-0111.
Ayala JE, Chen Y, Banko JL, Sheffler DJ, Williams R, Telk AN, Watson NL, Xiang Z, Zhang Y, Jones PJ, Lindsley CW, Olive MF, Conn PJ. MGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology [print-electronic]. 2009 Aug; 34(9): 2057-71. PMID: 19295507, PMCID: PMC2884290, PII: npp200930, DOI: 10.1038/npp.2009.30, ISSN: 1740-634X.
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J. Med. Chem. 2009 Jul 7/23/2009; 52(14): 4115-8. PMID: 19469556, PMCID: PMC2765192, DOI: 10.1021/jm9005065, ISSN: 1520-4804.
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jun 6/15/2009; 19(12): 3209-13. PMID: 19443219, PMCID: PMC3177605, PII: S0960-894X(09)00621-0, DOI: 10.1016/j.bmcl.2009.04.110, ISSN: 1464-3405.
Kennedy JP, Conn PJ, Lindsley CW. A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Jun 6/15/2009; 19(12): 3204-8. PMID: 19443215, PII: S0960-894X(09)00618-0, DOI: 10.1016/j.bmcl.2009.04.106, ISSN: 1464-3405.
Kulkarni SS, Zou MF, Cao J, Deschamps JR, Rodriguez AL, Conn PJ, Newman AH. Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. J. Med. Chem. 2009 Jun 6/11/2009; 52(11): 3563-75. PMID: 19445453, PMCID: PMC2894482, DOI: 10.1021/jm900172f, ISSN: 1520-4804.
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J. Med. Chem. 2009 Jun 6/11/2009; 52(11): 3445-8. PMID: 19438238, PMCID: PMC3875304, DOI: 10.1021/jm900286j, ISSN: 1520-4804.
Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. ChemMedChem. 2009 Apr; 4(4): 505-11. PMID: 19197923, PMCID: PMC2865690, DOI: 10.1002/cmdc.200800357, ISSN: 1860-7187.
Conn PJ, Jones CK, Lindsley CW. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol. Sci [print-electronic]. 2009 Mar; 30(3): 148-55. PMID: 19201489, PMCID: PMC2907736, PII: S0165-6147(09)00013-3, DOI: 10.1016/j.tips.2008.12.002, ISSN: 0165-6147.
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol. Pharmacol [print-electronic]. 2009 Mar; 75(3): 577-88. PMID: 19047481, PMCID: PMC2684909, PII: mol.108.052886, DOI: 10.1124/mol.108.052886, ISSN: 1521-0111.
Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorg. Med. Chem. Lett [print-electronic]. 2009 Feb 2/1/2009; 19(3): 962-6. PMID: 19097893, PMCID: PMC3787871, PII: S0960-894X(08)01468-6, DOI: 10.1016/j.bmcl.2008.11.104, ISSN: 1464-3405.
Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov. 2009 Jan; 8(1): 41-54. PMID: 19116626, PMCID: PMC2907734, PII: nrd2760, DOI: 10.1038/nrd2760, ISSN: 1474-1784.
Conn PJ, Jones CK. Promise of mGluR2/3 activators in psychiatry. Neuropsychopharmacology. 2009 Jan; 34(1): 248-9. PMID: 19079073, PMCID: PMC2907744, PII: npp2008156, DOI: 10.1038/npp.2008.156, ISSN: 1740-634X.
Conn PJ, Lindsley CW, Jones CK. Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol. Sci [print-electronic]. 2009 Jan; 30(1): 25-31. PMID: 19058862, PMCID: PMC2907735, PII: S0165-6147(08)00247-2, DOI: 10.1016/j.tips.2008.10.006, ISSN: 0165-6147.
Brady AE, Jones CK, Bridges TM, Kennedy JP, Thompson AD, Heiman JU, Breininger ML, Gentry PR, Yin H, Jadhav SB, Shirey JK, Conn PJ, Lindsley CW. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J. Pharmacol. Exp. Ther [print-electronic]. 2008 Dec; 327(3): 941-53. PMID: 18772318, PMCID: PMC2745822, PII: jpet.108.140350, DOI: 10.1124/jpet.108.140350, ISSN: 1521-0103.
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol. Pharmacol [print-electronic]. 2008 Nov; 74(5): 1345-58. PMID: 18664603, PMCID: PMC2574552, PII: mol.108.049551, DOI: 10.1124/mol.108.049551, ISSN: 1521-0111.
Miller NR, Daniels RN, Bridges TM, Brady AE, Conn PJ, Lindsley CW. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5443-7. PMID: 18829311, PMCID: PMC3177607, PII: S0960-894X(08)01088-3, DOI: 10.1016/j.bmcl.2008.09.032, ISSN: 1464-3405.
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW. Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5439-42. PMID: 18805692, PMCID: PMC3177598, PII: S0960-894X(08)01078-0, DOI: 10.1016/j.bmcl.2008.09.023, ISSN: 1464-3405.
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Oct 10/15/2008; 18(20): 5626-30. PMID: 18793851, PMCID: PMC3182458, PII: S0960-894X(08)01018-4, DOI: 10.1016/j.bmcl.2008.08.087, ISSN: 1464-3405.
Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J. Neurosci. 2008 Oct 10/8/2008; 28(41): 10422-33. PMID: 18842902, PMCID: PMC2577155, PII: 28/41/10422, DOI: 10.1523/JNEUROSCI.1850-08.2008, ISSN: 1529-2401.
Jones PJ, Xiang Z, Conn PJ. Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract-piriform cortex synapse. Neuropharmacology [print-electronic]. 2008 Sep; 55(4): 440-6. PMID: 18625254, PMCID: PMC2644556, PII: S0028-3908(08)00238-4, DOI: 10.1016/j.neuropharm.2008.06.043, ISSN: 0028-3908.
Sheffler DJ, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology [print-electronic]. 2008 Sep; 55(4): 419-27. PMID: 18625258, PMCID: PMC2600811, PII: S0028-3908(08)00245-1, DOI: 10.1016/j.neuropharm.2008.06.047, ISSN: 0028-3908.
Conn PJ, Roth BL. Opportunities and challenges of psychiatric drug discovery: roles for scientists in academic, industry, and government settings. Neuropsychopharmacology [print-electronic]. 2008 Aug; 33(9): 2048-60. PMID: 18216778, PII: 1301638, DOI: 10.1038/sj.npp.1301638, ISSN: 0893-133X.
Sharma S, Rodriguez AL, Conn PJ, Lindsley CW. Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Jul 7/15/2008; 18(14): 4098-101. PMID: 18550372, PMCID: PMC2533619, PII: S0960-894X(08)00599-4, DOI: 10.1016/j.bmcl.2008.05.091, ISSN: 1464-3405.
Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ. Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated. Neuropharmacology [print-electronic]. 2008 Apr; 54(5): 804-14. PMID: 18255102, PMCID: PMC2431171, PII: S0028-3908(07)00397-8, DOI: 10.1016/j.neuropharm.2007.12.009, ISSN: 0028-3908.
Conn PJ, Tamminga C, Schoepp DD, Lindsley C. Schizophrenia: moving beyond monoamine antagonists. Mol. Interv. 2008 Apr; 8(2): 99-107. PMID: 18403654, PII: 8/2/99, DOI: 10.1124/mi.8.2.7, ISSN: 1534-0384.
Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol. Pharmacol [print-electronic]. 2008 Apr; 73(4): 1213-24. PMID: 18171729, PII: mol.107.041053, DOI: 10.1124/mol.107.041053, ISSN: 1521-0111.
Chen Y, Goudet C, Pin JP, Conn PJ. N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol. Pharmacol [print-electronic]. 2008 Mar; 73(3): 909-18. PMID: 18056795, PII: mol.107.040097, DOI: 10.1124/mol.107.040097, ISSN: 1521-0111.
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg. Med. Chem. Lett [print-electronic]. 2008 Feb 2/1/2008; 18(3): 885-90. PMID: 18178088, PMCID: PMC2275053, PII: S0960-894X(07)01510-7, DOI: 10.1016/j.bmcl.2007.12.051, ISSN: 1464-3405.
Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat. Chem. Biol [print-electronic]. 2008 Jan; 4(1): 42-50. PMID: 18059262, PII: nchembio.2007.55, DOI: 10.1038/nchembio.2007.55, ISSN: 1552-4469.
Bikbaev A, Neyman S, Ngomba RT, Conn J, Nicoletti F, Manahan-Vaughan D. MGluR5 mediates the interaction between late-LTP, network activity, and learning. PLoS ONE. 2008; 3((5)): e2155.
Benneyworth MA, Xiang Z, Smith RL, Garcia EE, Conn PJ, Sanders-Bush E. A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis. Mol. Pharmacol [print-electronic]. 2007 Aug; 72(2): 477-84. PMID: 17526600, PII: mol.107.035170, DOI: 10.1124/mol.107.035170, ISSN: 0026-895X.
Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. J. Pharmacol. Exp. Ther [print-electronic]. 2007 Jul; 322(1): 254-64. PMID: 17416742, PII: jpet.106.117093, DOI: 10.1124/jpet.106.117093, ISSN: 0022-3565.
Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, Conn PJ. Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol. Pharmacol [print-electronic]. 2007 May; 71(5): 1389-98. PMID: 17303702, PII: mol.106.032425, DOI: 10.1124/mol.106.032425, ISSN: 0026-895X.
Lindsley CW, Weaver D, Jones C, Marnett L, Conn PJ. Preclinical drug discovery research and training at Vanderbilt. ACS Chem. Biol. 2007 Jan 1/23/2007; 2(1): 17-20. PMID: 17243778, DOI: 10.1021/cb6004867, ISSN: 1554-8937.
Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, Tamagnan GD, Conn PJ. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol. Pharmacol [print-electronic]. 2006 Aug; 70(2): 616-26. PMID: 16645124, PII: mol.105.021857, DOI: 10.1124/mol.105.021857, ISSN: 0026-895X.
Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Tsou NN, Duggan ME, Conn PJ, Hartman GD. Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides. ChemMedChem. 2006 Aug; 1(8): 807-11. PMID: 16902933, DOI: 10.1002/cmdc.200600097, ISSN: 1860-7179.
Galici R, Jones CK, Hemstapat K, Nong Y, Echemendia NG, Williams LC, de Paulis T, Conn PJ. Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J. Pharmacol. Exp. Ther [print-electronic]. 2006 Jul; 318(1): 173-85. PMID: 16608916, PII: jpet.106.102046, DOI: 10.1124/jpet.106.102046, ISSN: 0022-3565.
de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, Conn PJ. Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J. Med. Chem. 2006 Jun 6/1/2006; 49(11): 3332-44. PMID: 16722652, DOI: 10.1021/jm051252j, ISSN: 0022-2623.
Marino MJ, Conn PJ. Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. Curr Opin Pharmacol [print-electronic]. 2006 Feb; 6(1): 98-102. PMID: 16368268, PII: S1471-4892(05)00183-9, DOI: 10.1016/j.coph.2005.09.006, ISSN: 1471-4892.
Conn PJ, Niswender CM. MGluR7's lucky number. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2006 Jan 1/10/2006; 103(2): 251-2. PMID: 16407154, PMCID: PMC1326193, PII: 0510051103, DOI: 10.1073/pnas.0510051103, ISSN: 0027-8424.
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ. A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol. Pharmacol [print-electronic]. 2005 Dec; 68(6): 1793-802. PMID: 16155210, PII: mol.105.016139, DOI: 10.1124/mol.105.016139, ISSN: 0026-895X.
Zhang Y, Rodriguez AL, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Dec; 315(3): 1212-9. PMID: 16135701, PII: jpet.105.090308, DOI: 10.1124/jpet.105.090308, ISSN: 0022-3565.
Galici R, Echemendia NG, Rodriguez AL, Conn PJ. A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Dec; 315(3): 1181-7. PMID: 16123306, PII: jpet.105.091074, DOI: 10.1124/jpet.105.091074, ISSN: 0022-3565.
Conn PJ, Battaglia G, Marino MJ, Nicoletti F. Metabotropic glutamate receptors in the basal ganglia motor circuit. Nat. Rev. Neurosci. 2005 Oct; 6(10): 787-98. PMID: 16276355, PII: nrn1763, DOI: 10.1038/nrn1763, ISSN: 1471-003X.
Valenti O, Mannaioni G, Seabrook GR, Conn PJ, Marino MJ. Group III metabotropic glutamate-receptor-mediated modulation of excitatory transmission in rodent substantia nigra pars compacta dopamine neurons. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Jun; 313(3): 1296-304. PMID: 15761115, PII: jpet.104.080481, DOI: 10.1124/jpet.104.080481, ISSN: 0022-3565.
Wittmann M, Marino MJ, Henze DA, Seabrook GR, Conn PJ. Clozapine potentiation of N-methyl-D-aspartate receptor currents in the nucleus accumbens: role of NR2B and protein kinase A/Src kinases. J. Pharmacol. Exp. Ther [print-electronic]. 2005 May; 313(2): 594-603. PMID: 15659539, PII: jpet.104.080200, DOI: 10.1124/jpet.104.080200, ISSN: 0022-3565.
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J. Pharmacol. Exp. Ther [print-electronic]. 2005 Apr; 313(1): 199-206. PMID: 15608073, PII: jpet.104.079244, DOI: 10.1124/jpet.104.079244, ISSN: 0022-3565.
Niswender CM, Jones CK, Conn PJ. New therapeutic frontiers for metabotropic glutamate receptors. Curr Top Med Chem. 2005; 5(9): 847-57. PMID: 16178730, ISSN: 1568-0266.
Alagarsamy S, Saugstad J, Warren L, Mansuy IM, Gereau RW, Conn PJ. NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin. Neuropharmacology. 2005; 49 Suppl 1: 135-45. PMID: 16005030, PMCID: PMC3799794, PII: S0028-3908(05)00188-7, DOI: 10.1016/j.neuropharm.2005.05.005, ISSN: 0028-3908.
Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y. Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology. 2005; 49 Suppl 1: 57-69. PMID: 15993439, PII: S0028-3908(05)00106-1, DOI: 10.1016/j.neuropharm.2005.03.006, ISSN: 0028-3908.
Doherty JJ, Alagarsamy S, Bough KJ, Conn PJ, Dingledine R, Mott DD. Metabotropic glutamate receptors modulate feedback inhibition in a developmentally regulated manner in rat dentate gyrus. J. Physiol. (Lond.) [print-electronic]. 2004 Dec 12/1/2004; 561(Pt 2): 395-401. PMID: 15513941, PMCID: PMC1665349, PII: jphysiol.2004.074930, DOI: 10.1113/jphysiol.2004.074930, ISSN: 0022-3751.
Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR. Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J. Med. Chem. 2004 Nov 11/18/2004; 47(24): 5825-8. PMID: 15537338, DOI: 10.1021/jm049400d, ISSN: 0022-2623.
Campbell UC, Lalwani K, Hernandez L, Kinney GG, Conn PJ, Bristow LJ. The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats. Psychopharmacology (Berl.). 2004 Sep; 175(3): 310-8. PMID: 15024550, DOI: 10.1007/s00213-004-1827-5, ISSN: 0033-3158.
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J. Pharmacol. Exp. Ther [print-electronic]. 2004 May; 309(2): 568-77. PMID: 14747613, PII: jpet.103.061747, DOI: 10.1124/jpet.103.061747, ISSN: 0022-3565.
Marino, M.J., Bradley, S.R. , Awad, H., Wittmann, M., Conn, P.J. Localization and physiological roles of metabotropic glutamate receptors in the indirect pathway of the basal ganglia. Movement Disorders. 2004; in press.
Williams JB, Mallorga PJ, Conn PJ, Pettibone DJ, Sur C.. Effects of typical and atypical antipsychotics on human glycine transporters. Schizophrenia Res. 2004; (in press).
Sur C, Mallorga PJ, Wittmann M, Jacobson MA, Pascarella D, Williams JB, Brandish PE, Pettibone DJ, Scolnick EM, Conn PJ. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Nov 11/11/2003; 100(23): 13674-9. PMID: 14595031, PMCID: PMC263872, PII: 1835612100, DOI: 10.1073/pnas.1835612100, ISSN: 0027-8424.
Marino MJ, Williams DL, O'Brien JA, Valenti O, McDonald TP, Clements MK, Wang R, DiLella AG, Hess JF, Kinney GG, Conn PJ. Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Nov 11/11/2003; 100(23): 13668-73. PMID: 14593202, PMCID: PMC263871, PII: 1835724100, DOI: 10.1073/pnas.1835724100, ISSN: 0027-8424.
Williams DL, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ. Difference in mGluR5 interaction between positive allosteric modulators from two structural classes. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 481-4. PMID: 14684495, ISSN: 0077-8923.
Valenti O, Marino MJ, Conn PJ. Modulation of excitatory transmission onto midbrain dopaminergic neurons of the rat by activation of group III metabotropic glutamate receptors. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 479-80. PMID: 14684494, ISSN: 0077-8923.
Marino MJ, Valenti O, O'Brien JA, Williams DL, Conn PJ. Modulation of inhibitory transmission in the rat globus pallidus by activation of mGluR4. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 435-7. PMID: 14684481, ISSN: 0077-8923.
Conn PJ. Physiological roles and therapeutic potential of metabotropic glutamate receptors. Ann. N. Y. Acad. Sci. 2003 Nov; 1003: 12-21. PMID: 14684432, ISSN: 0077-8923.
Junge CE, Sugawara T, Mannaioni G, Alagarsamy S, Conn PJ, Brat DJ, Chan PH, Traynelis SF. The contribution of protease-activated receptor 1 to neuronal damage caused by transient focal cerebral ischemia. Proc. Natl. Acad. Sci. U.S.A [print-electronic]. 2003 Oct 10/28/2003; 100(22): 13019-24. PMID: 14559973, PMCID: PMC240737, PII: 2235594100, DOI: 10.1073/pnas.2235594100, ISSN: 0027-8424.
Mallorga PJ, Williams JB, Jacobson M, Marques R, Chaudhary A, Conn PJ, Pettibone DJ, Sur C. Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine. Neuropharmacology. 2003 Oct; 45(5): 585-93. PMID: 12941372, PII: S0028390803002272, ISSN: 0028-3908.
O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol. Pharmacol. 2003 Sep; 64(3): 731-40. PMID: 12920211, PII: 64/3/731, DOI: 10.1124/mol.64.3.731, ISSN: 0026-895X.
Kinney GG, Sur C, Burno M, Mallorga PJ, Williams JB, Figueroa DJ, Wittmann M, Lemaire W, Conn PJ. The glycine transporter type 1 inhibitor N-[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy)propyl]sarcosine potentiates NMDA receptor-mediated responses in vivo and produces an antipsychotic profile in rodent behavior. J. Neurosci. 2003 Aug 8/20/2003; 23(20): 7586-91. PMID: 12930797, PII: 23/20/7586, ISSN: 1529-2401.
Valenti O, Marino MJ, Wittmann M, Lis E, DiLella AG, Kinney GG, Conn PJ. Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse. J. Neurosci. 2003 Aug 8/6/2003; 23(18): 7218-26. PMID: 12904482, PII: 23/18/7218, ISSN: 1529-2401.
Kinney GG, Burno M, Campbell UC, Hernandez LM, Rodriguez D, Bristow LJ, Conn PJ. Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents. J. Pharmacol. Exp. Ther [print-electronic]. 2003 Jul; 306(1): 116-23. PMID: 12660307, PII: jpet.103.048702, DOI: 10.1124/jpet.103.048702, ISSN: 0022-3565.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003 May; 44(6): 699-706. PMID: 12681368, PII: S0028390803000534, ISSN: 0028-3908.
Marino MJ, Valenti O, Conn PJ. Glutamate receptors and Parkinson's disease: opportunities for intervention. Drugs Aging. 2003; 20(5): 377-97. PMID: 12696997, PII: 2056, ISSN: 1170-229X.
Poisik OV, Mannaioni G, Traynelis S, Smith Y, Conn PJ. Distinct functional roles of the metabotropic glutamate receptors 1 and 5 in the rat globus pallidus. J. Neurosci. 2003 Jan 1/1/2003; 23(1): 122-30. PMID: 12514208, PII: 23/1/122, ISSN: 1529-2401.
Poisik, O., Marino, M.J. and Conn, P.J. Distinct functional roles of the group I metabotropic glutamate receptors 1 and 5 in the rat globus pallidus. J. Neurosci. 2003; 23((1)): 122-30.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003; 44((6)): 699-706.
Marino M, Valenti O, Conn PJ. Glutamate receptors and Parkinson's disease : opportunities for intervention. Drugs Aging. 2003; 20((5)): 377-97.
Sorensen SD, Conn PJ. G protein-coupled receptor kinases regulate metabotropic glutamate receptor 5 function and expression. Neuropharmacology. 2003; 44((6)): 699-706.
Williams, J., Mallorga, P., Patel, S., Conn, P.J., Pettibone, D., Austin, C. and Sur, C. Development of a scintillation proximity assay for analysis of Na+/Cl- dependent neurotransmitter transporter activity. Analytical Biochem. 2003; 321: 31-7.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors [editorial]. Pharmacol. Biochem. Behav. 2002 Dec; 74(1): 255-6. PMID: 12376174, PII: S009130570200953X, ISSN: 0091-3057.
Peavy RD, Sorensen SD, Conn PJ. Differential regulation of metabotropic glutamate receptor 5-mediated phosphoinositide hydrolysis and extracellular signal-regulated kinase responses by protein kinase C in cultured astrocytes. J. Neurochem. 2002 Oct; 83(1): 110-8. PMID: 12358734, PII: 1113, ISSN: 0022-3042.
Alagarsamy S, Rouse ST, Junge C, Hubert GW, Gutman D, Smith Y, Conn PJ. NMDA-induced phosphorylation and regulation of mGluR5. Pharmacol. Biochem. Behav. 2002 Sep; 73(2): 299-306. PMID: 12117583, PII: S0091305702008262, ISSN: 0091-3057.
Marino MJ, Awad-Granko H, Ciombor KJ, Conn PJ. Haloperidol-induced alteration in the physiological actions of group I mGlus in the subthalamic nucleus and the substantia nigra pars reticulata. Neuropharmacology. 2002 Aug; 43(2): 147-59. PMID: 12213269, PII: S0028390802000977, ISSN: 0028-3908.
Wittmann M, Marino MJ, Conn PJ. Dopamine modulates the function of group II and group III metabotropic glutamate receptors in the substantia nigra pars reticulata. J. Pharmacol. Exp. Ther. 2002 Aug; 302(2): 433-41. PMID: 12130700, DOI: 10.1124/jpet.102.033266, ISSN: 0022-3565.
Besong G, Battaglia G, D'Onofrio M, Di Marco R, Ngomba RT, Storto M, Castiglione M, Mangano K, Busceti CL, Nicoletti FR, Bacon K, Tusche M, Valenti O, Conn PJ, Bruno V, Nicoletti F. Activation of group III metabotropic glutamate receptors inhibits the production of RANTES in glial cell cultures. J. Neurosci. 2002 Jul 7/1/2002; 22(13): 5403-11. PMID: 12097492, PII: 22/13/5403, DOI: 20026585, ISSN: 1529-2401.
Sorensen SD, Macek TA, Cai Z, Saugstad JA, Conn PJ. Dissociation of protein kinase-mediated regulation of metabotropic glutamate receptor 7 (mGluR7) interactions with calmodulin and regulation of mGluR7 function. Mol. Pharmacol. 2002 Jun; 61(6): 1303-12. PMID: 12021391, ISSN: 0026-895X.
Scotland RS, Morales-Ruiz M, Chen Y, Yu J, Rudic RD, Fulton D, Gratton JP, Sessa WC. Functional reconstitution of endothelial nitric oxide synthase reveals the importance of serine 1179 in endothelium-dependent vasomotion. Circ. Res. 2002 May 5/3/2002; 90(8): 904-10. PMID: 11988492, ISSN: 1524-4571.
Fontana J, Fulton D, Chen Y, Fairchild TA, McCabe TJ, Fujita N, Tsuruo T, Sessa WC. Domain mapping studies reveal that the M domain of hsp90 serves as a molecular scaffold to regulate Akt-dependent phosphorylation of endothelial nitric oxide synthase and NO release. Circ. Res. 2002 May 5/3/2002; 90(8): 866-73. PMID: 11988487, ISSN: 1524-4571.
Valenti O, Conn PJ, Marino MJ. Distinct physiological roles of the Gq-coupled metabotropic glutamate receptors Co-expressed in the same neuronal populations. J. Cell. Physiol. 2002 May; 191(2): 125-37. PMID: 12064455, DOI: 10.1002/jcp.10081, ISSN: 0021-9541.
Saugstad JA, Yang S, Pohl J, Hall RA, Conn PJ. Interaction between metabotropic glutamate receptor 7 and alpha tubulin. J. Neurochem. 2002 Mar; 80(6): 980-8. PMID: 11953448, PMCID: PMC2925652, ISSN: 0022-3042.
Marino MJ, Conn PJ. Direct and indirect modulation of the N-methyl D-aspartate receptor. Curr Drug Targets CNS Neurol Disord. 2002 Feb; 1(1): 1-16. PMID: 12769631, ISSN: 1568-007X.
Marino MJ, Awad H, Poisik O, Wittmann M, Conn PJ. Localization and physiological roles of metabotropic glutamate receptors in the direct and indirect pathways of the basal ganglia. Amino Acids. 2002; 23(1-3): 185-91. PMID: 12373536, DOI: 10.1007/s00726-001-0127-1, ISSN: 0939-4451.
Sorensen SD, Macek TA, Cai Z, Saugstad JA, Conn PJ. Dissociation of protein kinase-mediated regulation of metabotropic glutamate receptor 7 (mGluR7) interactions with calmodulin and regulation of mGluR7 function. Mol Pharmacol. 2002; 61((6)): 1303-12.
Peavy RD, Chang MS, Sanders-Bush E, Conn PJ. Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor. J Neurosci. 2002; 21((24)): 9619-28.
Marino MJ, Conn PJ. Direct and indirect modulation of the N-Methyl D-Aspartate receptor. Curr Drug Target CNS Neurol Disord. 2002; 1((1)): 1.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors. Pharmacol Biochem Behav. 2002; 74((1)): 255-6.
Marino MJ, Conn P.J. Modulation of the Basal Ganglia by metabotropic glutamate receptors: potential for novel therapeutics. Curr Drug Target CNS Neurol Disord. 2002; 1((3)): 239-50.
Peavy RD, Chang MS, Sanders-Bush E, Conn PJ. Metabotropic glutamate receptor 5-induced phosphorylation of extracellular signal-regulated kinase in astrocytes depends on transactivation of the epidermal growth factor receptor. J. Neurosci. 2001 Dec 12/15/2001; 21(24): 9619-28. PMID: 11739572, PII: 21/24/9619, ISSN: 1529-2401.
Marino MJ, Wittmann M, Bradley SR, Hubert GW, Smith Y, Conn PJ. Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata. J. Neurosci. 2001 Sep 9/15/2001; 21(18): 7001-12. PMID: 11549710, PII: 21/18/7001, ISSN: 1529-2401.
Zheng F, Erreger K, Low CM, Banke T, Lee CJ, Conn PJ, Traynelis SF. Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A. Nat. Neurosci. 2001 Sep; 4(9): 894-901. PMID: 11528420, PII: nn0901-894, DOI: 10.1038/nn0901-894, ISSN: 1097-6256.
Mannaioni G, Marino MJ, Valenti O, Traynelis SF, Conn PJ. Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function. J. Neurosci. 2001 Aug 8/15/2001; 21(16): 5925-34. PMID: 11487615, PII: 21/16/5925, ISSN: 1529-2401.
Cai Z, Saugstad JA, Sorensen SD, Ciombor KJ, Zhang C, Schaffhauser H, Hubalek F, Pohl J, Duvoisin RM, Conn PJ. Cyclic AMP-dependent protein kinase phosphorylates group III metabotropic glutamate receptors and inhibits their function as presynaptic receptors. J. Neurochem. 2001 Aug; 78(4): 756-66. PMID: 11520896, PMCID: PMC3799790, ISSN: 0022-3042.
Awad-Granko H, Conn PJ. Activation of groups I or III metabotropic glutamate receptors inhibits excitatory transmission in the rat subthalamic nucleus. Neuropharmacology. 2001 Jul; 41(1): 32-41. PMID: 11445183, PII: S0028390801000478, ISSN: 0028-3908.
Alagarsamy S, Sorensen SD, Conn PJ. Coordinate regulation of metabotropic glutamate receptors. Curr. Opin. Neurobiol. 2001 Jun; 11(3): 357-62. PMID: 11399435, PII: S0959-4388(00)00219-1, ISSN: 0959-4388.
Wittmann M, Marino MJ, Bradley SR, Conn PJ. Activation of group III mGluRs inhibits GABAergic and glutamatergic transmission in the substantia nigra pars reticulata. J. Neurophysiol. 2001 May; 85(5): 1960-8. PMID: 11353013, ISSN: 0022-3077.
De Blasi A, Conn PJ, Pin J, Nicoletti F. Molecular determinants of metabotropic glutamate receptor signaling. Trends Pharmacol. Sci. 2001 Mar; 22(3): 114-20. PMID: 11239574, PII: S0165614700016357, ISSN: 0165-6147.
Wittmann M, Hubert GW, Smith Y, Conn PJ. Activation of metabotropic glutamate receptor 1 inhibits glutamatergic transmission in the substantia nigra pars reticulata. Neuroscience. 2001; 105(4): 881-9. PMID: 11530226, PII: S0306452201002548, ISSN: 0306-4522.
Marino MJ, Wittmann M, Bradley SR, Hubert GW, Smith Y, Conn PJ. Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata. J Neurosci. 2001; 21((18)): 7001-12.
Zheng F, Erreger K, Low CM, Banke T, Lee CJ, Conn PJ, Traynelis SF. Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A. Nat Neurosci. 2001; 4((9)): 894-901.
Prince HC, Tzingounis AV, Levey AI, Conn PJ. Functional downregulation of GluR2 in piriform cortex of kindled animals. Synapse. 2000 Dec 12/15/2000; 38(4): 489-98. PMID: 11044897, PII: 10.1002/1098-2396(20001215)38:4<489::AID-SYN15>3.0.CO;2-N, DOI: 10.1002/1098-2396(20001215)38:4<489::AID-SYN15>3.0.CO;2-N, ISSN: 0887-4476.
Rouse ST, Marino MJ, Bradley SR, Awad H, Wittmann M, Conn PJ. Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders. Pharmacol. Ther. 2000 Dec; 88(3): 427-35. PMID: 11337032, PII: S016372580000098X, ISSN: 0163-7258.
Awad H, Hubert GW, Smith Y, Levey AI, Conn PJ. Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus. J. Neurosci. 2000 Nov 11/1/2000; 20(21): 7871-9. PMID: 11050106, PII: 20/21/7871, ISSN: 1529-2401.
Schaffhauser H, Cai Z, Hubalek F, Macek TA, Pohl J, Murphy TJ, Conn PJ. CAMP-dependent protein kinase inhibits mGluR2 coupling to G-proteins by direct receptor phosphorylation. J. Neurosci. 2000 Aug 8/1/2000; 20(15): 5663-70. PMID: 10908604, PII: 20/15/5663, ISSN: 0270-6474.
Bradley SR, Marino MJ, Wittmann M, Rouse ST, Awad H, Levey AI, Conn PJ. Activation of group II metabotropic glutamate receptors inhibits synaptic excitation of the substantia Nigra pars reticulata. J. Neurosci. 2000 May 5/1/2000; 20(9): 3085-94. PMID: 10777772, ISSN: 1529-2401.
Dingledine R, Conn PJ. Peripheral glutamate receptors: molecular biology and role in taste sensation. J. Nutr. 2000 Apr; 130(4S Suppl): 1039S-42S. PMID: 10736377, ISSN: 0022-3166.
Rouse ST, Hamilton SE, Potter LT, Nathanson NM, Conn PJ. Muscarinic-induced modulation of potassium conductances is unchanged in mouse hippocampal pyramidal cells that lack functional M1 receptors. Neurosci. Lett. 2000 Jan 1/7/2000; 278(1-2): 61-4. PMID: 10643801, PII: S0304-3940(99)00914-3, ISSN: 0304-3940.
Lie AA, Becker A, Behle K, Beck H, Malitschek B, Conn PJ, Kuhn R, Nitsch R, Plaschke M, Schramm J, Elger CE, Wiestler OD, Blümcke I. Up-regulation of the metabotropic glutamate receptor mGluR4 in hippocampal neurons with reduced seizure vulnerability. Ann. Neurol. 2000 Jan; 47(1): 26-35. PMID: 10632098, ISSN: 0364-5134.
Kosinski CM, Risso Bradley S, Conn PJ, Levey AI, Landwehrmeyer GB, Penney JB, Young AB, Standaert DG. Localization of metabotropic glutamate receptor 7 mRNA and mGluR7a protein in the rat basal ganglia. J. Comp. Neurol. 1999 Dec 12/13/1999; 415(2): 266-84. PMID: 10545164, PII: 10.1002/(SICI)1096-9861(19991213)415:2<266::AID-CNE9>3.0.CO;2-7, ISSN: 0021-9967.
Alagarsamy S, Rouse ST, Gereau RW, Heinemann SF, Smith Y, Conn PJ. Activation of N-methyl-D-aspartate receptors reverses desensitization of metabotropic glutamate receptor, mGluR5, in native and recombinant systems. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 526-30. PMID: 10414329, ISSN: 0077-8923.
Macek TA, Schaffhauser H, Conn PJ. Activation of PKC disrupts presynaptic inhibition by group II and group III metabotropic glutamate receptors and uncouples the receptor from GTP-binding proteins. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 554-7. PMID: 10414335, ISSN: 0077-8923.
Bradley SR, Standaert DG, Levey AI, Conn PJ. Distribution of group III mGluRs in rat basal ganglia with subtype-specific antibodies. Ann. N. Y. Acad. Sci. 1999 Apr 4/30/1999; 868: 531-4. PMID: 10414330, ISSN: 0077-8923.
Bradley SR, Standaert DG, Rhodes KJ, Rees HD, Testa CM, Levey AI, Conn PJ. Immunohistochemical localization of subtype 4a metabotropic glutamate receptors in the rat and mouse basal ganglia. J. Comp. Neurol. 1999 Apr 4/28/1999; 407(1): 33-46. PMID: 10213186, PII: 10.1002/(SICI)1096-9861(19990428)407:1<33::AID-CNE3>3.0.CO;2-G, ISSN: 0021-9967.
Alagarsamy S, Marino MJ, Rouse ST, Gereau RW, Heinemann SF, Conn PJ. Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems. Nat. Neurosci. 1999 Mar; 2(3): 234-40. PMID: 10195215, DOI: 10.1038/6338, ISSN: 1097-6256.
Hay M, McKenzie H, Lindsley K, Dietz N, Bradley SR, Conn PJ, Hasser EM. Heterogeneity of metabotropic glutamate receptors in autonomic cell groups of the medulla oblongata of the rat. J. Comp. Neurol. 1999 Jan 1/25/1999; 403(4): 486-501. PMID: 9888314, PII: 10.1002/(SICI)1096-9861(19990125)403:4<486::AID-CNE5>3.0.CO;2-9, ISSN: 0021-9967.
Paradee W, Melikian HE, Rasmussen DL, Kenneson A, Conn PJ, Warren ST. Fragile X mouse: strain effects of knockout phenotype and evidence suggesting deficient amygdala function. Neuroscience. 1999; 94(1): 185-92. PMID: 10613508, PII: S0306-4522(99)00285-7, ISSN: 0306-4522.
Rouse ST, Marino MJ, Potter LT, Conn PJ, Levey AI. Muscarinic receptor subtypes involved in hippocampal circuits. Life Sci. 1999; 64(6-7): 501-9. PMID: 10069516, ISSN: 0024-3205.
Khawaja XZ, Liang JJ, Saugstad JA, Jones PG, Harnish S, Conn PJ, Cockett MI. Immunohistochemical distribution of RGS7 protein and cellular selectivity in colocalizing with Galphaq proteins in the adult rat brain. J. Neurochem. 1999 Jan; 72(1): 174-84. PMID: 9886068, ISSN: 0022-3042.
Marino MJ, Rouse ST, Levey AI, Potter LT, Conn PJ. Activation of the genetically defined m1 muscarinic receptor potentiates N-methyl-D-aspartate (NMDA) receptor currents in hippocampal pyramidal cells. Proc. Natl. Acad. Sci. U.S.A. 1998 Sep 9/15/1998; 95(19): 11465-70. PMID: 9736760, PMCID: PMC21666, ISSN: 0027-8424.
Macek TA, Schaffhauser H, Conn PJ. Protein kinase C and A3 adenosine receptor activation inhibit presynaptic metabotropic glutamate receptor (mGluR) function and uncouple mGluRs from GTP-binding proteins. J. Neurosci. 1998 Aug 8/15/1998; 18(16): 6138-46. PMID: 9698308, ISSN: 0270-6474.
Bradley SR, Rees HD, Yi H, Levey AI, Conn PJ. Distribution and developmental regulation of metabotropic glutamate receptor 7a in rat brain. J. Neurochem. 1998 Aug; 71(2): 636-45. PMID: 9681454, ISSN: 0022-3042.
Peavy RD, Conn PJ. Phosphorylation of mitogen-activated protein kinase in cultured rat cortical glia by stimulation of metabotropic glutamate receptors. J. Neurochem. 1998 Aug; 71(2): 603-12. PMID: 9681450, ISSN: 0022-3042.
Zheng F, Gingrich MB, Traynelis SF, Conn PJ. Tyrosine kinase potentiates NMDA receptor currents by reducing tonic zinc inhibition. Nat. Neurosci. 1998 Jul; 1(3): 185-91. PMID: 10195142, PII: 634, DOI: 10.1038/634, ISSN: 1097-6256.
Saugstad JA, Marino MJ, Folk JA, Hepler JR, Conn PJ. RGS4 inhibits signaling by group I metabotropic glutamate receptors. J. Neurosci. 1998 Feb 2/1/1998; 18(3): 905-13. PMID: 9437012, ISSN: 0270-6474.
Chung DS, Traynelis SF, Murphy TJ, Conn PJ. 4-Methylhomoibotenic acid activates a novel metabotropic glutamate receptor coupled to phosphoinositide hydrolysis. J. Pharmacol. Exp. Ther. 1997 Nov; 283(2): 742-9. PMID: 9353394, ISSN: 0022-3565.
Chen YT, Henk MJ, Carney KJ, Wong WD, Rothenberger DA, Zheng T, Feygin M, Madoff RD. Prognostic significance of tumor markers in colorectal cancer patients: DNA index, S-phase fraction, p53 expression, and Ki-67 index. J. Gastrointest. Surg. 1997 May; 1(3): 266-72; discussion 273. PMID: 9834357, PII: S1091-255X(97)80119-9, ISSN: 1091-255X.
Miller HP, Levey AI, Rothstein JD, Tzingounis AV, Conn PJ. Alterations in glutamate transporter protein levels in kindling-induced epilepsy. J. Neurochem. 1997 Apr; 68(4): 1564-70. PMID: 9084427, ISSN: 0022-3042.
Conn PJ, Pin JP. Pharmacology and functions of metabotropic glutamate receptors. Annu. Rev. Pharmacol. Toxicol. 1997; 37: 205-37. PMID: 9131252, DOI: 10.1146/annurev.pharmtox.37.1.205, ISSN: 0362-1642.
Macek TA, Winder DG, Gereau RW, Ladd CO, Conn PJ. Differential involvement of group II and group III mGluRs as autoreceptors at lateral and medial perforant path synapses. J. Neurophysiol. 1996 Dec; 76(6): 3798-806. PMID: 8985877, ISSN: 0022-3077.
Winder DG, Conn PJ. Roles of metabotropic glutamate receptors in glial function and glial-neuronal communication. J. Neurosci. Res. 1996 Oct 10/15/1996; 46(2): 131-7. PMID: 8915890, PII: 10.1002/(SICI)1097-4547(19961015)46:2<131::AID-JNR1>3.0.CO;2-I, DOI: 10.1002/(SICI)1097-4547(19961015)46:2<131::AID-JNR1>3.0.CO;2-I, ISSN: 0360-4012.
Winder DG, Ritch PS, Gereau RW, Conn PJ. Novel glial-neuronal signalling by coactivation of metabotropic glutamate and beta-adrenergic receptors in rat hippocampus. J. Physiol. (Lond.). 1996 Aug 8/1/1996; 494 ( Pt 3): 743-55. PMID: 8865071, PMCID: PMC1160674, ISSN: 0022-3751.
Bradley SR, Levey AI, Hersch SM, Conn PJ. Immunocytochemical localization of group III metabotropic glutamate receptors in the hippocampus with subtype-specific antibodies. J. Neurosci. 1996 Mar 3/15/1996; 16(6): 2044-56. PMID: 8604049, ISSN: 0270-6474.
Gereau RW, Conn PJ. Multiple presynaptic metabotropic glutamate receptors modulate excitatory and inhibitory synaptic transmission in hippocampal area CA1. J. Neurosci. 1995 Oct; 15(10): 6879-89. PMID: 7472445, ISSN: 0270-6474.
Gereau RW, Conn PJ. Roles of specific metabotropic glutamate receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability. J. Neurophysiol. 1995 Jul; 74(1): 122-9. PMID: 7472317, ISSN: 0022-3077.
Gereau RW, Winder DG, Conn PJ. Pharmacological differentiation of the effects of co-activation of beta-adrenergic and metabotropic glutamate receptors in rat hippocampus. Neurosci. Lett. 1995 Feb 2/17/1995; 186(2-3): 119-22. PMID: 7777178, ISSN: 0304-3940.
Winder DG, Conn PJ. Metabotropic glutamate receptor (mGluR)-mediated potentiation of cyclic AMP responses does not require phosphoinositide hydrolysis: mediation by a group II-like mGluR. J. Neurochem. 1995 Feb; 64(2): 592-9. PMID: 7830052, ISSN: 0022-3042.
Prince HK, Conn PJ, Blackstone CD, Huganir RL, Levey AI. Down-regulation of AMPA receptor subunit GluR2 in amygdaloid kindling. J. Neurochem. 1995 Jan; 64(1): 462-5. PMID: 7798948, ISSN: 0022-3042.
Desai MA, McBain CJ, Kauer JA, Conn PJ. Metabotropic glutamate receptor-induced disinhibition is mediated by reduced transmission at excitatory synapses onto interneurons and inhibitory synapses onto pyramidal cells. Neurosci. Lett. 1994 Nov 11/7/1994; 181(1-2): 78-82. PMID: 7898776, ISSN: 0304-3940.
Gereau RW, Conn PJ. Presynaptic enhancement of excitatory synaptic transmission by beta-adrenergic receptor activation. J. Neurophysiol. 1994 Sep; 72(3): 1438-42. PMID: 7807226, ISSN: 0022-3077.
Chung DS, Winder DG, Conn PJ. 4-Bromohomoibotenic acid selectively activates a 1-aminocyclopentane-1S,3R-dicarboxylic acid-insensitive metabotropic glutamate receptor coupled to phosphoinositide hydrolysis in rat cortical slices. J. Neurochem. 1994 Jul; 63(1): 133-9. PMID: 8207423, ISSN: 0022-3042.
Boss V, Nutt KM, Conn PJ. L-cysteine sulfinic acid as an endogenous agonist of a novel metabotropic receptor coupled to stimulation of phospholipase D activity. Mol. Pharmacol. 1994 Jun; 45(6): 1177-82. PMID: 8022410, ISSN: 0026-895X.
Gereau RW, Conn PJ. Potentiation of cAMP responses by metabotropic glutamate receptors depresses excitatory synaptic transmission by a kinase-independent mechanism. Neuron. 1994 May; 12(5): 1121-9. PMID: 8185947, PII: 0896-6273(94)90319-0, ISSN: 0896-6273.
Gereau RW, Conn PJ. A cyclic AMP-dependent form of associative synaptic plasticity induced by coactivation of beta-adrenergic receptors and metabotropic glutamate receptors in rat hippocampus. J. Neurosci. 1994 May; 14(5 Pt 2): 3310-8. PMID: 8182474, ISSN: 0270-6474.
Winder DG, Smith T, Conn PJ. Pharmacological differentiation of metabotropic glutamate receptors coupled to potentiation of cyclic adenosine monophosphate responses and phosphoinositide hydrolysis. J. Pharmacol. Exp. Ther. 1993 Aug; 266(2): 518-25. PMID: 8394908, ISSN: 0022-3565.
Winder DG, Conn PJ. Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to endogenous adenosine. J. Neurosci. 1993 Jan; 13(1): 38-44. PMID: 8380851, ISSN: 0270-6474.
Schoepp DD, Conn PJ. Metabotropic glutamate receptors in brain function and pathology. Trends Pharmacol. Sci. 1993 Jan; 14(1): 13-20. PMID: 7680175, ISSN: 0165-6147.
Boss V, Conn PJ. Metabotropic excitatory amino acid receptor activation stimulates phospholipase D in hippocampal slices. J. Neurochem. 1992 Dec; 59(6): 2340-3. PMID: 1431912, ISSN: 0022-3042.
Chen SJ, Desai MA, Klann E, Winder DG, Sweatt JD, Conn PJ. Amygdala kindling alters protein kinase C activity in dentate gyrus. J. Neurochem. 1992 Nov; 59(5): 1761-9. PMID: 1402921, ISSN: 0022-3042.
Desai MA, Smith TS, Conn PJ. Multiple metabotropic glutamate receptors regulate hippocampal function. Synapse. 1992 Nov; 12(3): 206-13. PMID: 1336225, DOI: 10.1002/syn.890120305, ISSN: 0887-4476.
Boss V, Desai MA, Smith TS, Conn PJ. Trans-ACPD-induced phosphoinositide hydrolysis and modulation of hippocampal pyramidal cell excitability do not undergo parallel developmental regulation. Brain Res. 1992 Oct 10/30/1992; 594(2): 181-8. PMID: 1360322, PII: 0006-8993(92)91124-W, ISSN: 0006-8993.
Winder DG, Conn PJ. Activation of metabotropic glutamate receptors in the hippocampus increases cyclic AMP accumulation. J. Neurochem. 1992 Jul; 59(1): 375-8. PMID: 1351930, ISSN: 0022-3042.
Desai MA, Conn PJ. Excitatory effects of ACPD receptor activation in the hippocampus are mediated by direct effects on pyramidal cells and blockade of synaptic inhibition. J. Neurophysiol. 1991 Jul; 66(1): 40-52. PMID: 1655995, ISSN: 0022-3077.
Desai MA, Conn PJ. Selective activation of phosphoinositide hydrolysis by a rigid analogue of glutamate. Neurosci. Lett. 1990 Feb 2/5/1990; 109(1-2): 157-62. PMID: 1969130, PII: 0304-3940(90)90555-N, ISSN: 0304-3940.
Conn PJ, Strong JA, Kaczmarek LK. Inhibitors of protein kinase C prevent enhancement of calcium current and action potentials in peptidergic neurons of Aplysia. J. Neurosci. 1989 Feb; 9(2): 480-7. PMID: 2918372, ISSN: 0270-6474.
Conn PJ, Strong JA, Azhderian EM, Nairn AC, Greengard P, Kaczmarek LK. Protein kinase inhibitors selectively block phorbol ester- or forskolin-induced changes in excitability of Aplysia neurons. J. Neurosci. 1989 Feb; 9(2): 473-9. PMID: 2537389, ISSN: 0270-6474.
Conn PJ, Kaczmarek LK. The bag cell neurons of Aplysia. A model for the study of the molecular mechanisms involved in the control of prolonged animal behaviors. Mol. Neurobiol. 1989; 3(4): 237-73. PMID: 2698177, DOI: 10.1007/BF02740607, ISSN: 0893-7648.
Conn PJ, Sanders-Bush E. Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors. J. Pharmacol. Exp. Ther. 1987 Aug; 242(2): 552-7. PMID: 3039120, ISSN: 0022-3565.
Conn PJ, Janowsky A, Sanders-Bush E. Denervation supersensitivity of 5-HT-1c receptors in rat choroid plexus. Brain Res. 1987 Jan 1/6/1987; 400(2): 396-8. PMID: 3815085, PII: 0006-8993(87)90641-X, ISSN: 0006-8993.
Conn PJ, Sanders-Bush E. Central serotonin receptors: effector systems, physiological roles and regulation. Psychopharmacology (Berl.). 1987; 92(3): 267-77. PMID: 2819915, ISSN: 0033-3158.
Conn PJ, Sanders-Bush E. Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site. J. Neurosci. 1986 Dec; 6(12): 3669-75. PMID: 3025382, ISSN: 0270-6474.
Conn PJ, Sanders-Bush E. Agonist-induced phosphoinositide hydrolysis in choroid plexus. J. Neurochem. 1986 Dec; 47(6): 1754-60. PMID: 3021903, ISSN: 0022-3042.
Conn PJ, Sanders-Bush E, Hoffman BJ, Hartig PR. A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover. Proc. Natl. Acad. Sci. U.S.A. 1986 Jun; 83(11): 4086-8. PMID: 2940597, PMCID: PMC323671, ISSN: 0027-8424.
Conn PJ, Sanders-Bush E. Biochemical characterization of serotonin stimulated phosphoinositide turnover. Life Sci. 1986 Feb 2/17/1986; 38(7): 663-9. PMID: 3003490, ISSN: 0024-3205.
Sanders-Bush E, Conn PJ. Effector systems coupled to serotonin receptors in brain: serotonin stimulated phosphoinositide hydrolysis. Psychopharmacol Bull. 1986; 22(3): 829-36. PMID: 3025911, ISSN: 0048-5764.
Conn PJ, Sanders-Bush E. Serotonin-stimulated phosphoinositide turnover: mediation by the S2 binding site in rat cerebral cortex but not in subcortical regions. J. Pharmacol. Exp. Ther. 1985 Jul; 234(1): 195-203. PMID: 2989504, ISSN: 0022-3565.
Conn PJ, Sanders-Bush E. Selective 5HT-2 antagonists inhibit serotonin stimulated phosphatidylinositol metabolism in cerebral cortex. Neuropharmacology. 1984 Aug; 23(8): 993-6. PMID: 6483122, ISSN: 0028-3908.
Available Postdoctoral Position Details
Posted: 9/18/2009
Postdoctoral position in cellular/molecular neurobiology is available at Vanderbilt University Medical Center. The successful candidate will join a research group that employs a highly multidisciplinary approach to explore the cellular and molecular mechanisms involved in neuromodulation and regulation of animal behavior. The laboratory uses a combination of biochemical, molecular biological, imaging, electrophysiological and behavioral techniques to study regulation of neuronal function by metabotropic glutamate receptors and other G-protein-linked receptors. Also, we have a strong interest in relating cellular and molecular changes to disorders of the central nervous system, including Parkinson|s disease and Schizophrenia.
Research Faculty positions also available for outstanding candidates.
Send curriculum vita, three references, and statement of research interests to:
Dr. P. Jeffrey Conn,
Professor
Director, Program in Translational Neuropharmacology
Department of Pharmacology
Vanderbilt University Medical Center
23rd Avenue South at Pierce
452-B Preston Research Building
Nashville, TN 37232-6600
E-mail: jeff.conn@vanderbilt.edu
Postdoctoral position in cellular/molecular neurobiology is available at Vanderbilt University Medical Center. The successful candidate will join a research group that employs a highly multidisciplinary approach to explore the cellular and molecular mechanisms involved in neuromodulation and regulation of animal behavior. The laboratory uses a combination of biochemical, molecular biological, imaging, electrophysiological and behavioral techniques to study regulation of neuronal function by metabotropic glutamate receptors and other G-protein-linked receptors. Also, we have a strong interest in relating cellular and molecular changes to disorders of the central nervous system, including Parkinson|s disease and Schizophrenia.
Research Faculty positions also available for outstanding candidates.
Send curriculum vita, three references, and statement of research interests to:
Dr. P. Jeffrey Conn,
Professor
Director, Program in Translational Neuropharmacology
Department of Pharmacology
Vanderbilt University Medical Center
23rd Avenue South at Pierce
452-B Preston Research Building
Nashville, TN 37232-6600
E-mail: jeff.conn@vanderbilt.edu