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CAS No.: 533-45-9

Clomethiazole/氯美噻唑 Catalog No. CSN10673

Synonyms: Distraneurin;Chlormethiazole;氯美噻唑

Clomethiazole can act as an agonist of GABAA and modulator of glycine receptor. It is a sedative used in the treatment of alcohol withdrawal.

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技术信息

生物活性

描述Clomethiazole (CMZ), a thiazole derivative, is structurally related to thiamine (vitamin B1). Chlorothiazole inhibits GABA and glycine mediated electrical stimulation of the central nervous system. In vitro, clomethiazole reversibly inhibits human CYP2E1 and decrease CYP2E1-mediated elimination of chlorzoxazone. CYP2A6 and CYP2E1 exhibited IC50 values of 24 µM and 42 µM^[3]. In vivo，with a single dose of CMZ (10, 50, or 100 mg/kg) by intraperitoneal injection, a single-dose CMZ treatment decreased DEN (diethylnitrosamine) clearance (CL), prolonged the t1/2, CMZ significantly inhibits the metabolism of DEN in normal and hepatofibrotic rats^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02374567	Dementia Depr... more >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders Collapse <<	Phase 3	Terminated	-	Germany ... more >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany Collapse <<

参考文献

[1] Chen YY, Zhang CL, et al. Inhibition of cytochrome P4502E1 by chlormethiazole attenuated acute ethanol-induced fatty liver. Chem Biol Interact. 2014 Oct 5;222:18-26.
[2] Stresser DM, Perloff ES, et al. Selective Time- and NADPH-Dependent Inhibition of Human CYP2E1 by Clomethiazole. Drug Metab Dispos. 2016 Aug;44(8):1424-30.
[3] Stresser DM, Perloff ES, Mason AK, et al. Selective Time- and NADPH-Dependent Inhibition of Human CYP2E1 by Clomethiazole. Drug Metab Dispos. 2016;44(8):1424-1430.
[4] Wang G, Xiao K, Gao J, et al. Inhibitory effect of chlormethiazole on the toxicokinetics of diethylnitrosamine in normal and hepatofibrotic rats. Drug Chem Toxicol. 2019;42(6):600-607.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 6.1861 mL
- 30.9306 mL
- 61.8611 mL
- 5 mM
- 1.2372 mL
- 6.1861 mL
- 12.3722 mL
- 10 mM
- 0.6186 mL
- 3.0931 mL
- 6.1861 mL

技术信息

CAS号

533-45-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C6H8ClNS

运输

蓝冰

分子量

161.65

别名

Distraneurin;Chlormethiazole;氯美噻唑;氯甲噻唑

溶解度

DMSO	50.0 mg/mL (309.3 mM)

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