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CAS No.: 14984-68-0

咳平盐酸盐 Catalog No. CSN23548

Synonyms: HT-11 hydrochloride;Cloperastine HCl

Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.

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技术信息

生物活性

描述Cloperastine (HCl), a centrally acting antitussive, ameliorated depression-like and anxiety-like behaviors in rodents at antitussive-effective doses. Cloperastine at 10 and 30 mg/kg ameliorated DES-induced impairment of passive avoidance responses. In addition, cloperastine affected the levels of 5-HT1A receptors, GIRK and BDNF in the hippocampus of DES-exposed mice^[3]. Cloperastine inhibited the hERG K⁺ currents in a concentration-dependent manner with an IC₅₀ value of 0.027 μM, whose potency was 100 times greater than that of diphenhydramine (IC50 = 2.7 μM). In the anesthetized guinea pigs, cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and MAP (monophasic action potential) duration without affecting PR interval or QRS width^[1]. Dextromethorphan (20 mg/kg) and cloperastine (2.5 and 5.0 mg/kg) at antitussive effective doses significantly increased bladder capacity and micturition latency. Unlike dextromethorphan, cloperastine ameliorated decreases in flow rate and increases in urethral resistance caused by cerebral infarction^[4].
参考文献

[1] Takahara A, Fujiwara K, Ohtsuki A, Oka T, Namekata I, Tanaka H. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165‐175
[2] Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.
[3] Soeda F, Hirakawa E, Inoue M, Shirasaki T, Takahama K. Cloperastine rescues impairment of passive avoidance response in mice prenatally exposed to diethylstilbestrol. Environ Toxicol. 2014;29(2):216‐225
[4] Yamamoto G, Soeda F, Shirasaki T, Takahama K. Ameliorating effects of cloperastine on dysfunction of the urinary bladder caused by cerebral infarction in conscious rats. Can J Physiol Pharmacol. 2009;87(11):893‐899

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7298 mL
- 13.6491 mL
- 27.2982 mL
- 5 mM
- 0.5460 mL
- 2.7298 mL
- 5.4596 mL
- 10 mM
- 0.2730 mL
- 1.3649 mL
- 2.7298 mL

技术信息

CAS号

14984-68-0

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H25Cl2NO

运输

蓝冰

分子量

366.32

别名

HT-11 hydrochloride;Cloperastine HCl

溶解度

DMSO	73.0 mg/mL (199.3 mM)

动物实验配方

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咳平盐酸盐 Catalog No. CSN23548

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