中文名 | 氯哌斯汀芬地柞酸盐 |
英文名 | o-[(2'-hydroxy[1,1'-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1) |
别名 | 氯哌酮芬地唑 氯哌斯汀芬地柞酸 氯哌斯汀芬地柞酸盐 氯苄哌醚联苯酰苯酸盐 化合物 T13619 1-(2-((4-氯苯基)(苯基)甲氧基)乙基)哌啶 2-(6-羟基-[1,1'-联苯]-3-羰基)苯甲酸盐 |
英文别名 | Cloperastine Febdizoate Cloperastine fendizoate Levocloperastine Fendizoate Levocloperastine Fendizoate Racemic Impurity 1-[2-[(4-Chlorophenyl)phenylmethoxy]ethyl]piperidine Fendizoate 1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,2-(4-hydroxy-3-phenylbenzoyl)benzoic acid |
CAS | 85187-37-7 |
EINECS | 286-126-9 |
化学式 | C40H38ClNO5 |
分子量 | 648.18642 |
InChI | InChI=1/C20H24ClNO.C20H14O4/c21-19-11-9-18(10-12-19)20(17-7-3-1-4-8-17)23-16-15-22-13-5-2-6-14-22;21-18-11-10-14(12-17(18)13-6-2-1-3-7-13)19(22)15-8-4-5-9-16(15)20(23)24/h1,3-4,7-12,20H,2,5-6,13-16H2;1-12,21H,(H,23,24) |
熔点 | 185-187°C |
沸点 | 593.9°C at 760 mmHg |
闪点 | 327°C |
蒸汽压 | 5.95E-15mmHg at 25°C |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
存储条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | Cloperastine inhibits the hERG K + currents in a concentrationdependent manner with IC 50 value of 27±3 nM. Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects. |
体内研究 | In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasic action potential (MAP) duration without affecting PR interval or QRS width. Cloperastine hydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats and mice, and shows minor toxicity by the oral route when administered as Cloperastine fendizoate, the LD 50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.543 ml | 7.714 ml | 15.428 ml |
5 mM | 0.309 ml | 1.543 ml | 3.086 ml |
10 mM | 0.154 ml | 0.771 ml | 1.543 ml |
5 mM | 0.031 ml | 0.154 ml | 0.309 ml |
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