盐酸氯普噻吨

盐酸氯普噻吨用途

Chlorprothixene hydrochloride 是一种多巴胺 (dopamine) 和组胺 (histamine) 受体拮抗剂,高亲和力地结合人 D1,D2,D3,D5,H1 受体,Ki 分别为 18 nM,2.96 nM,4.56 nM,9 nM 和 3.75 nM。具有抗精神病作用。

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盐酸氯普噻吨名称

[ CAS 号 ]:
6469-93-8

[ 中文名 ]:
盐酸氯普噻吨

[ 英文名 ]:
Chlorprothixene hydrochloride

[中文别名 ]:

氯噻酮相关物质B

[英文别名 ]:

Chlorprothixene hydrochloride

盐酸氯普噻吨生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Human D1 Receptor:18 nM (Ki)

Human D2 Receptor:2.96 nM (Ki)

Human D3 Receptor:4.56 nM (Ki)

Human D5 Receptor:9 nM (Ki)

Human H1 Receptor:3.75 nM (Ki)

[体外研究]

5-HT7、5-HT6和5-HT2的PKI分别为8.3、8.5和9.4,氯普罗噻吩与5-HT受体结合[2]。

[参考文献]

[1]. Y von Coburg, et al. Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42.

[2]. B L Roth, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.

盐酸氯普噻吨物理化学性质

[ 沸点 ]:
461.8ºC at 760 mmHg

[ 熔点 ]:
221ºC

[ 分子式 ]:
C₁₈H₁₉Cl₂NS

[ 分子量 ]:
352.32100

[ 闪点 ]:
233.1ºC

[ 精确质量 ]:
351.06200

[ PSA ]:
28.54000

[ LogP ]:
5.99000

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in water and in alcohol, slightly soluble in methylene chloride.

盐酸氯普噻吨MSDS

详细MSDS(安全技术说明书)

盐酸氯普噻吨毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XO0610000

CHEMICAL NAME :: Thioxanthene, 2-chloro-9-(3-(dimethylamino)propylidene)-, hydrochloride, (Z)-

CAS REGISTRY NUMBER :: 6469-93-8

LAST UPDATED :: 199709

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C18-H18-Cl-N-S.Cl-H

MOLECULAR WEIGHT :: 352.34

WISWESSER LINE NOTATION :: T C666 BS IYJ FG IU3N1&1 &GH -Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 25 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 242 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 45,3166,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 98 mg/kg

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

REFERENCE :: CKFRAY Ceskoslovenska Farmacie. (PNS-Ustredni Expedice a Dovoz Tisku, Kafkova 19, 160 00 Prague 6, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 15,526,1966

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,65,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Behavioral - somnolence (general depressed activity) Behavioral - excitement

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 144,481,1963

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盐酸氯普噻吨安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
UN 2811 6

[ WGK德国 ]:
3

[ RTECS号 ]:
XO0610000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

盐酸氯普噻吨文献

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J. Neurophysiol. 114 , 1321-30, (2015)

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Biologically active conformers of phenothiazines and thioxanthenes. Further evidence for a ligand model of dopamine D2 receptor antagonists.

J. Med. Chem. 36 , 2219-2227, (1993)

Conformational analyses have been performed on several phenothiazine and thioxanthene dopamine antagonists using the MM2-87 program and parameter set. The compounds that were examined are thioridazine...

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