Function and modulation of δ-containing GABAA receptors

Nadezhda N. Zheleznova, Anna Sedelnikova, David S. Weiss

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

αβδ-Containing GABAA receptors are (1) localized to extra- and perisynaptic membranes, (2) exhibit a high sensitivity to GABA, (3) show little desensitization, and (4) are believed to be one of the primary mediators of tonic inhibition in the central nervous system. This type of signaling appears to play a key role in controlling cell excitability. This review article briefly summarizes recent knowledge on tonic GABA-mediated inhibition. We will also consider the mechanism of action of many clinically important drugs such as anxiolytics, anticonvulsants, and sedative/hypnotics and their effects on δ-containing GABA receptor activation. We will conclude that αβδ-containing GABAA receptors exhibit a relatively low efficacy that can be potentiated by endogenous modulators and anxiolytic agents. This scenario enables these particular GABA receptor combinations, upon neurosteroid exposure for example, to impart a profound effect on excitability in the central nervous system.

Original languageEnglish (US)
Pages (from-to)S67-S73
JournalPsychoneuroendocrinology
Volume34
Issue numberSUPPL. 1
DOIs
StatePublished - Dec 1 2009

Keywords

  • Neurosteroids
  • Tonic inhibition
  • Tracazolate
  • αβδ GABA receptors

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology
  • Endocrine and Autonomic Systems
  • Psychiatry and Mental health
  • Biological Psychiatry

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