中文同义词:
5-(2-氯乙基)-4-甲基噻唑;5-(2-氯乙基)-4-甲基噻唑 氯美噻唑;氯美噻唑 1G;氯美噻唑
英文同义词:
5-(2-chloroethyl)-4-methylthiazole;CLOMETHIAZOLE;5-(2-Chlorethyl)-4-methylthiaziole hydrochloride;Chlorethiazole;Clomethiazolum;Distraneurin;5-(2-chloroethyl)-4-methyl-1,3-thiazole;chlormethiazole
相关类别:
GABA/Glycine receptor
储存条件
Inert atmosphere,2-8°C
酸度系数(pKa)
pKa 3.2 (Uncertain)
CAS 数据库
533-45-9(CAS DataBase Reference)
NIST化学物质信息
Clomethiazole(533-45-9)
生物活性
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。
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.
急性毒性
口服-小鼠 LD50: 2110 毫克/公斤;腹腔-小鼠 LD50: 190 毫克/公斤;
可燃性危险特性
可燃, 火场释放有毒氯化物, 氮氧化物, 硫氧化物烟雾