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Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Rodriguez AL, et al. Among authors: vinson pn. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7388-92. doi: 10.1016/j.bmcl.2012.10.068. Epub 2012 Oct 23. Bioorg Med Chem Lett. 2012. PMID: 23142615 Free PMC article.
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Rodriguez AL, Grier MD, Jones CK, Herman EJ, Kane AS, Smith RL, Williams R, Zhou Y, Marlo JE, Days EL, Blatt TN, Jadhav S, Menon UN, Vinson PN, Rook JM, Stauffer SR, Niswender CM, Lindsley CW, Weaver CD, Conn PJ. Rodriguez AL, et al. Among authors: vinson pn. Mol Pharmacol. 2010 Dec;78(6):1105-23. doi: 10.1124/mol.110.067207. Epub 2010 Oct 5. Mol Pharmacol. 2010. PMID: 20923853 Free PMC article.
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.
Noetzel MJ, Rook JM, Vinson PN, Cho HP, Days E, Zhou Y, Rodriguez AL, Lavreysen H, Stauffer SR, Niswender CM, Xiang Z, Daniels JS, Jones CK, Lindsley CW, Weaver CD, Conn PJ. Noetzel MJ, et al. Among authors: vinson pn. Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21. Mol Pharmacol. 2012. PMID: 22021324 Free PMC article.
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.
Utley T, Haddenham D, Salovich JM, Zamorano R, Vinson PN, Lindsley CW, Hopkins CR, Niswender CM. Utley T, et al. Among authors: vinson pn. Bioorg Med Chem Lett. 2011 Dec 1;21(23):6955-9. doi: 10.1016/j.bmcl.2011.09.131. Epub 2011 Oct 8. Bioorg Med Chem Lett. 2011. PMID: 22030026 Free PMC article.
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW. Sheffler DJ, et al. Among authors: vinson pn. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3921-5. doi: 10.1016/j.bmcl.2012.04.112. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22607673 Free PMC article.
Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats.
D'Amore V, Santolini I, van Rijn CM, Biagioni F, Molinaro G, Prete A, Conn PJ, Lindsley CW, Zhou Y, Vinson PN, Rodriguez AL, Jones CK, Stauffer SR, Nicoletti F, van Luijtelaar G, Ngomba RT. D'Amore V, et al. Among authors: vinson pn. Neuropharmacology. 2013 Mar;66:330-8. doi: 10.1016/j.neuropharm.2012.05.044. Epub 2012 Jun 15. Neuropharmacology. 2013. PMID: 22705340 Free PMC article.
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.
Salovich JM, Vinson PN, Sheffler DJ, Lamsal A, Utley TJ, Blobaum AL, Bridges TM, Le U, Jones CK, Wood MR, Daniels JS, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR. Salovich JM, et al. Among authors: vinson pn. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5084-8. doi: 10.1016/j.bmcl.2012.05.109. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22738637 Free PMC article.
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.
Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ. Gregory KJ, et al. Among authors: vinson pn. Mol Pharmacol. 2012 Nov;82(5):860-75. doi: 10.1124/mol.112.080531. Epub 2012 Aug 3. Mol Pharmacol. 2012. PMID: 22863693 Free PMC article.
48 results