GABAB receptors

Pharmacol Ther. 1995;67(2):187-246. doi: 10.1016/0163-7258(95)00016-a.

Abstract

GABAB receptors are a distinct subclass of receptors for the major inhibitory transmitter 4-aminobutanoic acid (GABA) that mediate depression of synaptic transmission and contribute to the inhibition controlling neuronal excitability. The development of specific agonists and antagonists for these receptors has led to a better understanding of their physiology and pharmacology, highlighting their diverse coupling to different intracellular effectors through Gi/G(o) proteins. This review emphasises our current knowledge of the neurophysiology and neurochemistry of GABAB receptors, including their heterogeneity, as well as the therapeutic potential of drugs acting at these sites.

Publication types

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

MeSH terms

  • Baclofen / metabolism
  • Baclofen / pharmacology
  • Binding, Competitive
  • Cations, Divalent / pharmacology
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism*
  • Central Nervous System Diseases / drug therapy
  • GABA Agonists / metabolism
  • GABA Agonists / pharmacology*
  • GABA Agonists / therapeutic use
  • GABA Antagonists / metabolism
  • GABA Antagonists / pharmacology*
  • GABA Antagonists / therapeutic use
  • GTP-Binding Proteins / metabolism
  • Humans
  • Neurophysiology
  • Radioligand Assay
  • Receptors, GABA-B / chemistry
  • Receptors, GABA-B / drug effects
  • Receptors, GABA-B / metabolism*
  • Structure-Activity Relationship

Substances

  • Cations, Divalent
  • GABA Agonists
  • GABA Antagonists
  • Receptors, GABA-B
  • GTP-Binding Proteins
  • Baclofen