Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu4) with CNS exposure in rats
Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu4. Compounds from the series show submicromolar potency at both human and rat mGlu4. In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.
Engers, Darren W.,Field, Julie R.,Le, Uyen,Zhou, Ya,Bolinger, Julie D.,Zamorano, Rocio,Blobaum, Anna L.,Jones, Carrie K.,Jadhav, Satyawan,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
p. 1106 - 1110
(2011/04/26)
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