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Clomethiazole
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Clomethiazole
CAS No. : 533-45-9
MCE 站:Clomethiazole
产品活性:Chlormethiazole 是一种有效的口服 GABAA 激动剂。 Chlormethiazole 还可以抑制人肝微粒体中的细胞色素 P450 亚型: CYP2A6 和 CYP2E1。Chlormethiazole 有抗惊厥作用,具有研究惊厥性癫痫的潜力。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling | Metabolic Enzyme/Protease
作用靶点:GABA Receptor | Cytochrome P450
In Vitro: Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents.Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells, with EC50 values of 0.3 and 1.5 mM, respectively.Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current.Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 with IC50 values of 24 ?M and 42 ?M, respectively, in human liver microsomes, meanwhile all other isoforms exhibiting values > 300 ?M.
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