GABA B receptor coupling to G-proteins and ion channels

Claire L. Padgett, Paul A. Slesinger

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

176 Scopus citations


GABA B receptors have been found to play a key role in regulating membrane excitability and synaptic transmission in the brain. The GABA B receptor is a G-protein coupled receptor (GPCR) that associates with a subset of G-proteins (pertussis toxin sensitive Gi/o family), that in turn regulate specific ion channels and trigger cAMP cascades. In this review, we describe the relationships between the GABA B receptor, its effectors and associated proteins that mediate GABA B receptor function within the brain. We discuss a unique feature of the GABA B receptor, the requirement for heterodimerization to produce functional receptors, as well as an increasing body of evidence that suggests GABA B receptors comprise a macromolecular signaling heterocomplex, critical for efficient targeting and function of the receptors. Within this complex, GABA B receptors associate specifically with Gi/o G-proteins that regulate voltage-gated Ca 2+ (Ca V ) channels, G-protein activated inwardly rectifying K + (GIRK) channels, and adenylyl cyclase. Numerous studies have revealed that lipid rafts, scaffold proteins, targeting motifs in the receptor, and regulators of G-protein signaling (RGS) proteins also contribute to the function of GABA B receptors and affect cellular processes such as receptor trafficking and activity-dependent desensitization. This complex regulation of GABA B receptors in the brain may provide opportunities for new ways to regulate GABA-dependent inhibition in normal and diseased states of the nervous system.

Original languageEnglish
Title of host publicationAdvances in Pharmacology
PublisherAcademic Press Inc.
Number of pages25
StatePublished - 2010
Externally publishedYes

Publication series

NameAdvances in Pharmacology
ISSN (Print)1054-3589


  • Desensitization
  • GIRK
  • Heterodimer
  • Pertussis toxin


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