Therapeutic potential of GABA(B) receptor ligands in drug addiction, anxiety, depression and other CNS disorders

Pharmacol Biochem Behav. 2013 Sep:110:174-84. doi: 10.1016/j.pbb.2013.07.003. Epub 2013 Jul 17.

Abstract

Glutamate and γ-aminobutyric acid (GABA) are the major excitatory and inhibitory neurotransmitter systems, respectively in the central nervous system (CNS). Dysregulation, in any of these or both, has been implicated in various CNS disorders. GABA acts via ionotropic (GABA(A) and GABA(C) receptor) and metabotropic (GABA(B)) receptor. Dysregulation of GABAergic signaling and alteration in GABA(B) receptor expression has been implicated in various CNS disorders. Clinically, baclofen-a GABA(B) receptor agonist is available for the treatment of spasticity, dystonia etc., associated with various neurological disorders. Moreover, GABAB receptor ligands has also been suggested to be beneficial in various neuropsychiatric and neurodegenerative disorders. The present review is aimed to discuss the role of GABA(B) receptors and the possible outcomes of GABA(B) receptor modulation in CNS disorders.

Keywords: Addiction; Anxiety; CNS disorders; Depression; GABA; Neurodegenerative disorders.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anxiety / metabolism
  • Anxiety / therapy*
  • Central Nervous System Diseases / metabolism
  • Central Nervous System Diseases / therapy*
  • Depression / metabolism
  • Depression / therapy*
  • GABA Modulators / pharmacology
  • GABA Modulators / therapeutic use*
  • Humans
  • Ligands
  • Protein Conformation
  • Receptors, GABA-B / chemistry
  • Receptors, GABA-B / metabolism*
  • Substance-Related Disorders / metabolism
  • Substance-Related Disorders / therapy*
  • gamma-Aminobutyric Acid / metabolism*

Substances

  • GABA Modulators
  • Ligands
  • Receptors, GABA-B
  • gamma-Aminobutyric Acid