533-45-9

基本信息
氯美噻唑
CLOMETHIAZOLE
chlormethiazole
ChlormethiazoleHCl
CHLORMETHIAZOLE HYDROCHLORIDE (5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE)
5-(2-Chlorethyl)-4-methylthiaziole hydrochloride
Chlorethiazole
Clomethiazolum
Distraneurin
物理化学性质
制备方法

137-00-8

533-45-9
以4-甲基-5-羟乙基噻唑为原料合成5-(2-氯乙基)-4-甲基噻唑的一般步骤如下:参照实施例18,将2-(4-甲基噻唑-5-基)乙醇(500 mg,3.49 mmol)溶于亚硫酰氯(4 mL)中。将反应混合物在回流条件下搅拌3小时。反应完成后,将混合物浓缩至干,得到浅黄色固体产物(680 mg,收率:98%)。产物经ESI-MS分析,显示m/z:162.0 [M + H]+。
参考文献:
[1] Patent: US2017/158680, 2017, A1. Location in patent: Paragraph 0385
[2] Journal of the American Chemical Society, 2001, vol. 123, # 6, p. 1017 - 1022
[3] Pharmaceutical Chemistry Journal, 1999, vol. 33, # 12, p. 658 - 660
[4] Journal of the American Chemical Society, 1982, vol. 104, # 18, p. 4934 - 4943
[5] Bioorganic and Medicinal Chemistry, 2016, vol. 24, # 22, p. 5988 - 6003
533-45-9(安全特性,毒性,储运)
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2025/05/22 | HY-129105 | 氯美噻唑 Clomethiazole | 533-45-9 | 100mg | 500元 |
2025/05/22 | HY-129105 | 氯美噻唑 Clomethiazole | 533-45-9 | 10mM * 1mLin DMSO | 550元 |
常见问题列表
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 EC 50 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 IC 50 values of 24 µM and 42 µM, respectively, in human liver microsomes, meanwhile all other isoforms exhibiting values > 300 µM.