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Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.

Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
J Med Chem. 2011 54 (4): 1106-10

PMID: 21247167 · PMCID: PMC3166797 · DOI:10.1021/jm101271s

Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu(4). Compounds from the series show submicromolar potency at both human and rat mGlu(4). In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.

MeSH Terms (14)

Allosteric Regulation Animals Brain Central Nervous System CHO Cells Cricetinae Cricetulus Humans Magnetic Resonance Spectroscopy Mass Spectrometry Picolines Rats Receptors, Metabotropic Glutamate Structure-Activity Relationship

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