Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics

Albert J. Robichaud, Darren W. Engers, Craig W. Lindsley, Corey R. Hopkins

Research output: Contribution to journalReview article

30 Scopus citations

Abstract

This Review describes recent activity in the advancement of ligands for the metabotropic glutamate 4 receptor subtype and their potential utility as central nervous system (CNS) therapeutics. Until recently, there was a paucity of compounds with suitable selectivity and druglike properties to elucidate the value of this target. The search for selective entities has led several groups to the investigation of allosteric modulators as a path to optimization of potential ligands. Recent efforts, discussed here, have afforded a variety of derivatives with improvements in potency, solubility, and pharmacokinetic properties that garner support for continued investigation and optimization.

Original languageEnglish (US)
Pages (from-to)433-449
Number of pages17
JournalACS Chemical Neuroscience
Volume2
Issue number8
DOIs
StatePublished - Aug 17 2011

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Keywords

  • Class C GPCR
  • Metabotropic glutamate receptor 4
  • Parkinson's disease
  • allosteric modulator
  • anxiety
  • cognitive disorders
  • neurodegenerative disorders
  • orthosteric ligand
  • pain
  • psychiatric disorders

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

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