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

  • J Med Chem. 2009 Jul 23;52(14):4115-8. doi: 10.1021/jm9005065.
Darren W Engers  1 ,  Colleen M Niswender ,  C David Weaver ,  Satyawan Jadhav ,  Usha N Menon ,  Rocio Zamorano ,  P Jeffrey Conn ,  Craig W Lindsley ,  Corey R Hopkins
Affiliations
  • 1. Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA.
PMID: 19469556 DOI: 10.1021/jm9005065
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.

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