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

Darren W. Engers, Colleen M. Niswender, C. David Weaver, Satyawan Jadhav, Usha N. Menon, Rocio Zamorano, P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins

Research output: Contribution to journalArticle

60 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)4115-4118
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number14
StatePublished - Jul 23 2009


ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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