Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders

Trends Pharmacol Sci. 2001 Jul;22(7):331-7. doi: 10.1016/s0165-6147(00)01694-1.

Abstract

Although multiple metabotropic glutamate (mglu) receptor subtypes were cloned in the early 1990s, progress in the characterization of these receptors has been slow because of difficulties in obtaining subtype-selective ligands. However, in the past few years exciting progress has been made on the mglu(5) receptor subtype following the identification of selective non-amino-acid-like ligands that implicate the mglu(5) receptor as a potentially important therapeutic target, particularly for the treatment of pain and anxiety.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation / drug effects
  • Allosteric Regulation / physiology
  • Animals
  • Anxiety / drug therapy*
  • Brain / drug effects
  • Brain / metabolism
  • Central Nervous System Diseases / drug therapy
  • Depression / drug therapy
  • Excitatory Amino Acid Antagonists / chemistry
  • Excitatory Amino Acid Antagonists / pharmacology
  • Excitatory Amino Acid Antagonists / therapeutic use*
  • Humans
  • Neurons, Afferent / drug effects
  • Neurons, Afferent / metabolism
  • Pain / drug therapy*
  • Parkinson Disease / drug therapy*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Pyridines / therapeutic use*
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate / physiology

Substances

  • Excitatory Amino Acid Antagonists
  • Pyridines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate
  • 6-methyl-2-(phenylethynyl)pyridine