Re-exploration of the PHCCC scaffold: Discovery of improved positive allosteric modulators of mGluR4

Richard Williams, Ya Zhou, Colleen M. Niswender, Qingwei Luo, P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins

Research output: Contribution to journalArticle

41 Scopus citations

Abstract

This paper describes a detailed structure-activity relationship (SAR) analysis of the metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulator, (-)-N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC). We have now developed compounds with improved potency and efficacy; in addition, compounds are presented that show selectivity for mGluR4 versus the other mGluR subtypes.

Original languageEnglish (US)
Pages (from-to)411-419
Number of pages9
JournalACS Chemical Neuroscience
Volume1
Issue number6
DOIs
StatePublished - Jun 16 2010

Keywords

  • Allosteric modulation
  • Metabotropic glutamate receptor 4
  • PHCCC
  • Parkinson's disease
  • Positive allosteric modulator
  • SAR
  • Structure-activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

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