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Development of a Second Generation mGlu

Development of a Second Generation mGlu

Cody Wenthur, J. Scott Daniels, Ryan Morrison, Julie L. Engers, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley

PMID: 23885366

Abstract:

Herein we report the discovery and structure activity relationship (SAR) of a novel, second generation metabotropic glutamate receptor 3 (mGlu3) negative allosteric modulator (NAM) probe (ML337) with >50-fold selectivity versus mGlu2 (IC50 >30 μM). The mGlu3 NAM was discovered via an iterative parallel synthesis optimization of the first generation mGlu3 NAM ML289, that was only ~15-fold selective. This mGlu3 NAM (60204017, ML337) displays an IC50 value of 592 nM and is inactive (>30 μM) on mGlu2 (as well as mGlu1,4,5,6,7,8) and clean in a Ricerca ancillary pharmacology panel. ML337 possesses favorable physiochemical properties, a good dystrophia myotonica protein kinase (DMPK) profile and is centrally penetrant. Thus, ML337 is a best-in-class in vitro and in vivo probe for studying non-competitive antagonism of mGlu3.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1382481799	ML289		1382481-79-9	Price

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