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ACS Chem Neurosci. 2011 Aug 17;2(8):433-49. doi: 10.1021/cn200043e. Epub 2011 Jun 14.

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

Author information

1
Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, USA. AJR@Lundbeck.com

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.

KEYWORDS:

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

PMID:
22860170
PMCID:
PMC3369748
DOI:
10.1021/cn200043e
[Indexed for MEDLINE]
Free PMC Article
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