Modulation of GABAA and glycine receptors by chlormethiazole

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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

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Keywords

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

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