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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
Bioorg Med Chem Lett. 2012 22 (24): 7388-92

PMID: 23142615 · PMCID: PMC3539767 · DOI:10.1016/j.bmcl.2012.10.068

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.

Copyright © 2012 Elsevier Ltd. All rights reserved.

MeSH Terms (14)

Allosteric Regulation Animals Binding Sites Dose-Response Relationship, Drug Drug Discovery Glycine Humans Models, Molecular Molecular Structure Rats Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate Structure-Activity Relationship Sulfonamides

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