Function and modulation of δ-containing GABAA receptors

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

    Research output: Contribution to journalArticlepeer-review

    45 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 2009

    Keywords

    • Neurosteroids
    • Tonic inhibition
    • Tracazolate
    • αβδ GABA receptors

    ASJC Scopus subject areas

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

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