Neurosteroid modulation of native and recombinant GABAA receptors

Jeremy J. Lambert, Delia Belelli, Claire Hill-Venning, Helen Callachan, John A. Peters

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    89 Citations (Scopus)

    Abstract

    1. The pioneering work of Hans Selye over 50 years ago demonstrated that certain steroid metabolites can produce a rapid depression of central nervous system activity. 2. Research during the last 10 years has established that such effects are mediated by a nongenomic and specific interaction of these steroids with the brain's major inhibitory receptor, the GABAA receptor. 3. Here we describe the molecular mechanism of action of such steroids and review attempts to define the steroid binding site on the receptor protein. The therapeutic potential of such neurosteroids is discussed.

    Original languageEnglish
    Pages (from-to)155-174
    Number of pages20
    JournalCellular and Molecular Neurobiology
    Volume16
    Issue number2
    DOIs
    Publication statusPublished - Apr 1996

    Keywords

    • Anesthetic
    • GABA receptor
    • Ligand-gated ion channel
    • Neurosteroids
    • Neurotransmitter receptor
    • Nongenomic steroid effects
    • Pregnane steroids
    • Whole-cell patch-clamp
    • Xenopus laevis oocyte

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