- 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
- 储运特性
库房低温通风干燥
- 灭火剂
水, 二氧化碳, 泡沫, 沙土
医药
合成路线 1（1. 合成：533-45-9）
产率：98%
合成条件：for 3 h; Reflux
实验步骤：参考实施例18 5-（2-氯乙基）-4-甲基噻唑的制备将2-（4-甲基 - 噻唑-5-基）乙醇18-a（500mg，3.49mmol）加入亚硫酰氯（4ml）中。 将混合物在回流下搅拌3小时。 将混合物浓缩至干，得到浅黄色固体（680mg，收率：98％）。 ESI-MS（m z）：162.0 [M + H] +。
参考文献：
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