GABAB receptor: a site of therapeutic benefit

Curr Opin Pharmacol. 2006 Feb;6(1):37-43. doi: 10.1016/j.coph.2005.10.002. Epub 2005 Dec 19.

Abstract

Although the presence of functional GABAB receptors in mammalian brain has been known for more than 20 years, there is still only one therapeutic agent in use, baclofen, which mediates its effects directly via this receptor. However, activation of this receptor can produce numerous effects that might be amenable to drug development. Evidence from preclinical studies also suggests that antagonism of the GABAB receptor produces beneficial clinical effects.

Publication types

  • Review

MeSH terms

  • Animals
  • Baclofen / pharmacology*
  • Baclofen / therapeutic use
  • Brain / drug effects
  • Brain / metabolism
  • Clinical Trials as Topic
  • Cognition / drug effects
  • Drug Evaluation, Preclinical
  • Epilepsy, Absence / drug therapy
  • Epilepsy, Absence / metabolism
  • GABA Agonists / pharmacology*
  • GABA Agonists / therapeutic use
  • GABA Antagonists / pharmacology
  • GABA Antagonists / therapeutic use
  • Humans
  • Muscle Spasticity / drug therapy
  • Muscle Spasticity / metabolism
  • Organophosphorus Compounds / pharmacology
  • Organophosphorus Compounds / therapeutic use
  • Pain / drug therapy
  • Pain / metabolism
  • Receptors, GABA-B / classification
  • Receptors, GABA-B / drug effects*
  • Receptors, GABA-B / metabolism
  • Substance-Related Disorders / drug therapy
  • Substance-Related Disorders / metabolism

Substances

  • GABA Agonists
  • GABA Antagonists
  • Organophosphorus Compounds
  • Receptors, GABA-B
  • (3-aminopropyl)(n-butyl)phosphinic acid
  • Baclofen