中文名 | 氯美噻唑 |
英文名 | Clomethiazole |
别名 | 氯美噻唑 氯甲基噻唑 5-(2-氯乙基)-4-甲基噻唑 5-(2-氯乙基)-4-甲基噻唑 氯美噻唑 |
英文别名 | Distraneurin Clomethiazole CLOMETHIAZOLE Chlorethiazole Clomethiazolum chlormethiazole 5-(2-chloroethyl)-4-methylthiazole 5-(2-chloroethyl)-4-methyl-1,3-thiazole 5-(2-Chlorethyl)-4-methylthiaziole hydrochloride |
CAS | 533-45-9 |
EINECS | 208-565-7 |
化学式 | C6H8ClNS |
分子量 | 161.65 |
密度 | d425 1.233 |
熔点 | 127-128 °C |
沸点 | bp7 92° |
溶解度 | 氯仿 (微溶) 、甲醇 (微溶) |
折射率 | 1.6000 (estimate) |
酸度系数 | pKa 3.2 (Uncertain) |
存储条件 | Inert atmosphere,2-8°C |
外观 | 滑油 |
颜色 | Pale Yellow |
MDL号 | MFCD00868012 |
体外研究 | 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. |
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