氯苄哌醚联苯酰苯酸盐

中文名称:

氯苄哌醚联苯酰苯酸盐

中文同义词:

氯苄哌醚联苯酰苯酸盐;氯哌斯汀芬地柞酸盐;氯哌斯汀芬地柞酸

英文名称:

o-[(2-hydroxy[1,1-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1)

英文同义词:

o-[(2-hydroxy[1,1-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1);Cloperastine fendizoate;Levocloperastine Fendizoate;Cloperastine Febdizoate;o-[(2-hydroxy[1,1-biphenyl]-4-yl)carbonyl]benzoic acid, compound with 1-[2-(4-chlorobenzhydryloxy)ethyl]piperidine (1:1);1-[2-[(4-Chlorophenyl)phenylmethoxy]ethyl]piperidine Fendizoate;Levocloperastine Fendizoate Racemic Impurity;1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine,2-(4-hydroxy-3-phenylbenzoyl)benzoic acid

CAS号:

85187-37-7

分子式:

C40H38ClNO5

分子量:

648.18642

EINECS号:

286-126-9

相关类别:

医药原料

Mol文件:

85187-37-7.mol

生物活性

Cloperastine fendizoate 抑制 hERG K+ 电流，IC50 为 27 nM，这种作用具有浓度依赖性。

靶点

27 nM (K + currents)

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.