Modulation of GABAA and glycine receptors by chlormethiazole.
Eur J Pharmacol
; 210(3): 239-46, 1992 Jan 21.
Article
en En
| MEDLINE
| ID: mdl-1319334
The influence of chlormethiazole, on currents evoked by gamma-aminobutyric acid (GABA) and glycine, was investigated under voltage-clamp conditions, in bovine chromaffin cells and murine spinal neurones, respectively. Chlormethiazole (30 and 100 microM) 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 microM)-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.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Clormetiazol
/
Receptores de GABA-A
Límite:
Animals
Idioma:
En
Revista:
Eur J Pharmacol
Año:
1992
Tipo del documento:
Article