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Chlormethiazole is a potentiator of GABAA receptors.1 It potentiates GABA-induced currents in L-M(TK-) cells expressing α1β1γ2 or α1β2γ2 subunit-containing GABAA receptors with EC50 values of 0.8 and 3.4 µM, respectively. Chlormethiazole protects against seizures induced by maximal electroshock (MES) in mice (ED50 = 130.8 mg/kg).2 It reduces infarct volume in a rat model of focal ischemia induced by permanent middle cerebral artery occlusion (MCAO).3 Formulations containing chlormethiazole have been used in the treatment of acute alcohol withdrawal.
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1. Electrophysiological actions of γ-
2. Anticonvulsant action of chlormethiazole is prevented by subconvulsive amounts of strychnine and aminophylline but not by bicuculline and picrotoxin. Pol. J. Pharmacol. 52(4), 267-273 (2000).
3. The neuroprotective effect of chlormethiazole on ischaemic neuronal damage following permanent middle cerebral artery ischaemia in the rat. Neurodegeneration 4(3), 323-328 (1995).