氯美噻唑

氯美噻唑用途

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,具有治疗惊厥性癫痫的潜力。

氯美噻唑名称

[ CAS 号 ]:
533-45-9

[ 中文名 ]:
氯美噻唑

[ 英文名 ]:
Clomethiazole

[中文别名 ]:

5-(2-氯乙基)-4-甲基噻唑

[英文别名 ]:

Clomethiazole
Emineurina
Clomethiazol
Chlormethiazole
MFCD00868012
Distraneurin
Clometiazole
Chlormethiazol
Clomethiazolum
EINECS 208-565-7

氯美噻唑生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[体外研究]

在没有GABA的情况下,氯噻唑(1mm)对α1/β1/γ2或α1/β2/γ2亚基的细胞产生大的全细胞电流[1]。氯噻唑激活α1/β1/γ2-和α1/β2/γ2-细胞中的GABAA电流,EC50值分别为0.3和1.5mm[1]。低浓度的氯噻唑(30μm)也能增强GABA在两种细胞类型中的作用,相当于效力的3倍增加,最大电流增加到1.8倍(1)。氯噻唑抑制人肝微粒体中细胞色素P450亚型CYP2A6和CYP2E1的IC50值分别为24μM和42μM,同时所有其他亚型的IC50值均大于300μM[2]。

[参考文献]

[1]. Nelson RM, et al.Electrophysiological actions of gamma-aminobutyric acid and clomethiazole on recombinant GABA(A) receptors.Eur J Pharmacol. 2002 Oct 11;452(3):255-62.

[2]. Stresser DM, et al. Selective Time- and NADPH-Dependent Inhibition of Human CYP2E1 by Clomethiazole.Drug Metab Dispos. 2016 Aug;44(8):1424-30

氯美噻唑物理化学性质

[ 密度 ]:
1.218 g/cm3

[ 沸点 ]:
245.8ºC at 760 mmHg

[ 分子式 ]:
C₆H₈ClNS

[ 分子量 ]:
198.11300

[ 闪点 ]:
102.4ºC

[ 精确质量 ]:
196.98300

[ PSA ]:
41.13000

[ LogP ]:
3.03480

[ 储存条件 ]:
库房低温通风干燥

氯美噻唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ3850000

CHEMICAL NAME :: Thiazole, 5-(2-chloroethyl)-4-methyl-

CAS REGISTRY NUMBER :: 533-45-9

BEILSTEIN REFERENCE NO. :: 0114244

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C6-H8-Cl-N-S

MOLECULAR WEIGHT :: 161.66

WISWESSER LINE NOTATION :: T5N CSJ D2G E1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2110 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 7,167,1964

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 190 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: APSXAS Acta Pharmaceutica Suecica. (Apotekarsocieteten-Farmacevtiska Foereningen, Box 1136, S-111, 81 Stockholm, Sweden) V.1- 1964- Volume(issue)/page/year: 8,39,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 94 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: APSXAS Acta Pharmaceutica Suecica. (Apotekarsocieteten-Farmacevtiska Foereningen, Box 1136, S-111, 81 Stockholm, Sweden) V.1- 1964- Volume(issue)/page/year: 7,423,1970

氯美噻唑安全信息

[ 海关编码 ]:
2934100090

氯美噻唑合成路线

详细合成路线

氯美噻唑上下游产品

氯美噻唑上游产品

氯美噻唑下游产品

氯美噻唑海关

[ 海关编码 ]: 2934100090

[ 中文概述 ]:
2934100090. 结构上含有一个非稠合噻唑环的化合物(不论是否氢化). 增值税率:17.0%. 退税率:9.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%