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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).

ABSTRACT: We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.

SUBMITTER: Engers DW

PROVIDER: S-EPMC2765192 | biostudies-literature | 2009 Jul

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).

Engers Darren W DW Niswender Colleen M CM Weaver C David CD Jadhav Satyawan S Menon Usha N UN Zamorano Rocio R Conn P Jeffrey PJ Lindsley Craig W CW Hopkins Corey R CR

Journal of medicinal chemistry 20090701 14

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field. ...[more]

PMID: 19469556

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