Modulation of GABAA and glycine receptors by chlormethiazole

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    55 Citations (Scopus)

    Abstract

    The influence of chlormethiazole, on currents evoked by γ-aminobutyric acid (GABA) and glycine, was investigated under voltage-clamp conditions, in bovine chromaffin cells and murine spinal neurones, respectively. Chlormethiazole (30 and 100 μM) dose dependently potentiated currents activated by either inhibitory neurotransmitter. The potentiation of the GABA-evoked response occurred without altering the reversal potential and was not influenced by the benzodiazepine receptor antagonist Ro 15-1788 (300 nM). GABA-gated channels, recorded from outside-out membrane patches, showed increased probability of being in the conducting state in the presence of chlormethiazole. High concentrations of chlormethiazole (3 mM) activated bicuculline (1 μM)-sensitive whole-cell currents with a reversal potential similar to the chloride equilibrium potential. Chlormethiazole potentiates GABA- and glycine-activated currents and at higher doses, directly activates the GABAA receptor.

    Original languageEnglish
    Pages (from-to)239-246
    Number of pages8
    JournalEuropean Journal of Pharmacology
    Volume210
    Issue number3
    DOIs
    Publication statusPublished - 21 Jan 1992

    Keywords

    • Anaesthetics (general)
    • Anticonvulsants
    • Chlormethiazole
    • GABA receptors
    • Glycine receptors
    • Patch-clamp

    ASJC Scopus subject areas

    • Cellular and Molecular Neuroscience
    • Pharmacology

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