氯美噻唑 T14983

Product Introduction
Bioactivity


英文名: Clomethiazole

描述: Clomethiazole (Distraneurin) 是口服GABAA 激动剂，可抑制人肝微粒体中的细胞色素 P450 异构体，CYP2A6 和 CYP2E1。它有抗惊厥作用，具有治疗惊厥性癫痫持续状态的潜力。

体外活性: Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 (IC50: 24 μM and 42 μ), in human liver microsomes. But all other isoforms exhibiting values > 300 μM[2]. Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1]. Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells ( EC50: 0.3 and 1.5 mM) [1]. 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[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 240 mg/mL (1484.69 mM)


关键字: GABA Receptor | inhibit | Clomethiazole | Cytochrome P450 | sedative | anticonvulsant | Gamma-aminobutyric acid Receptor | alcoholism | insomnia | CYPs | Inhibitor | neuroprotective | γ-Aminobutyric acid Receptor

相关产品: Naringin | Ayanin | Cobicistat | Memantine hydrochloride | Curcumenol | Gomisin G | SDZ285428 | TMS | Amentoflavone | Seneciphylline

相关库: Anti-Aging Compound Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途