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咳平盐酸盐

咳平盐酸盐用途

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

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咳平盐酸盐名称

[ CAS 号 ]:
14984-68-0

[ 中文名 ]:
咳平盐酸盐

[ 英文名 ]:
Cloperastine hydrochloride

[中文别名 ]:

[英文别名 ]:

MFCD00079012
Cloperastine hydrochloride
EINECS 239-067-8

咳平盐酸盐生物活性

[ 描述 ]:

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

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

27 nM (K+ currents)[1]

[体外研究]

氯吡拉汀以浓度依赖的方式抑制hERG K+电流,IC50值为27nm[1]。在镇咳药物中,具有镇咳和抗水肿活性的氯吡拉汀也能松弛支气管肌肉。氯吡拉汀是一种具有中枢镇咳作用的药物,同时具有与可待因相似的抗组胺和罂粟碱活性,但没有麻醉作用[2]。

[体内研究]

在麻醉豚鼠中,治疗剂量为1mg/kg的氯吡拉汀可延长QT间期和单相动作电位(MAP)持续时间,但不影响PR间期或QRS宽度[1]。盐酸氯吡拉汀在大鼠和小鼠经腹腔途径给药时表现出相对较低的急性毒性,口服给药时表现出轻微毒性,两种给药途径大鼠和小鼠的半数致死量分别超过1000和2000毫克/千克[2]。

[参考文献]

[1]. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165-75.

[2]. Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.

咳平盐酸盐物理化学性质

[ 沸点 ]:
84°C 35mm

[ 分子式 ]:
C₂₀H₂₅Cl₂NO

[ 分子量 ]:
366.325

[ 闪点 ]:
210.2ºC

[ 精确质量 ]:
365.131317

[ PSA ]:
12.47000

[ LogP ]:
5.67180

[ 蒸汽压 ]:
2.15E-07mmHg at 25°C

[ 折射率 ]:
1.414

咳平盐酸盐MSDS

详细MSDS(安全技术说明书)

咳平盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM6491500

CHEMICAL NAME :: Piperidine, 1-(2-((p-chloro-alpha-phenylbenzyl)oxy)ethyl)-, hydrochloride

CAS REGISTRY NUMBER :: 14984-68-0

LAST UPDATED :: 199706

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C20-H24-Cl-N-O.Cl-H

MOLECULAR WEIGHT :: 366.36

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 :: 1986 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 553 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 122,384,1983

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1300 mg/kg

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

REFERENCE :: YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 80,1759,1960

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咳平盐酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
TM6491500

[ 海关编码 ]:
2933399090

咳平盐酸盐海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

咳平盐酸盐文献

[Novel antidepressant-like action of drugs possessing GIRK channel blocking action in rats].

Yakugaku Zasshi 130(5) , 699-705, (2010)

We have previously found that antitussive drugs inhibit G protein-coupled inwardly rectifying potassium (GIRK) channel currents in brain neurons. Potassium efflux through GIRK channels causes membrane...

Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs.

J. Pharmacol. Sci. 120(3) , 165-75, (2012)

Cloperastine is an antitussive drug, which can be received as an over-the-counter cold medicine. The chemical structure of cloperastine is quite similar to that of the antihistamine drug diphenhydrami...

Levocloperastine in the treatment of chronic nonproductive cough: comparative efficacy versus standard antitussive agents.

Drugs Exp. Clin. Res. 30(4) , 133-41, (2004)

The medical and social impact of cough is substantial. Current antitussive agents at effective doses have adverse events such as drowsiness, nausea and constipation that limit their use. There is also...

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