盐酸依沙维林

盐酸依沙维林用途

罂粟碱的衍生物盐酸伊沙韦林抑制心脏L型钙通道。盐酸乙威林是一种外周血管扩张剂和解痉药。盐酸乙威林可用于外周血管疾病的研究[1][2][3]。

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盐酸依沙维林名称

[ CAS 号 ]:
985-13-7

[ 中文名 ]:
盐酸依沙维林

[ 英文名 ]:
Isoquinoline,1-[(3,4-diethoxyphenyl)methyl]-6,7-diethoxy-, hydrochloride (1:1)

[英文别名 ]:

Consenil
Balborin
Isovex
Barbonin hydrochloride
Cebral
Ethaquin
Ethylpapaverin hydrochloride

盐酸依沙维林生物活性

[ 描述 ]:

罂粟碱的衍生物盐酸伊沙韦林抑制心脏L型钙通道。盐酸乙威林是一种外周血管扩张剂和解痉药。盐酸乙威林可用于外周血管疾病的研究[1][2][3]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> 神经信号通路 >> 单胺氧化酶

[体外研究]

盐酸乙威林(10μM,PC12细胞) 通过阻断 L型电压敏感钙离子通道来减少儿茶酚胺分泌[2]。盐酸乙威林(12小时)通过抑制第12页细胞中的酪氨酸羟化酶 (第)活性来降低多巴胺含量,国际50为 1.4μM[3]盐酸乙威林抑制小鼠脑中的单胺氧化酶 (毛)(分离自小鼠全脑) 活性,国际50为 25.5μM[6]

[体内研究]

将盐酸乙威林(2-10mg/kg静脉滴注,静脉注射)引起豚鼠耳蜗内电位显着升高[4]。 Ethaverine(1-10mg/kg静脉注射) 抑制麻醉狗的房室传导和心率[5]。动物模型：狗[5]剂量：1和10 mg/kg给药：静脉注射结果：抑制房室传导和心率。

[参考文献]

[1]. Wang Y, et al. Ethaverine, a derivative of papaverine, inhibits cardiac L-type calcium channels. Mol Pharmacol. 1991 Nov;40(5):750-5.

[2]. Suh BC, et al. Inhibition by ethaverine of catecholamine secretion through blocking L-type Ca2+ channels in PC12 cells. Biochem Pharmacol. 1994 Mar 29;47(7):1262-6.

[3]. Shin JS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on dopamine content in PC12 cells. Biol Pharm Bull. 2001 Jan;24(1):103-5.

[4]. Prazma J, et al. Effect of ethaverine hydrochloride on cochlear microcirculation. Arch Otolaryngol. 1981 Apr;107(4):227-9.

[5]. Lacroix P, et al. [Comparative activity of ethaverine and papaverine on chronotropic and dromotropic cardiac functions in the anesthetized dog]. Arch Int Pharmacodyn Ther. 1976 May;221(1):163-76. French.

[6]. Lee SS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on monoamine oxidase activity in mouse brain. Biol Pharm Bull. 2001 Jul;24(7):838-40.

盐酸依沙维林物理化学性质

[ 密度 ]:
1.104g/cm3

[ 沸点 ]:
527.1ºC at 760 mmHg

[ 熔点 ]:
187ºC

[ 分子式 ]:
C₂₄H₃₀ClNO₄

[ 分子量 ]:
431.95200

[ 闪点 ]:
185.9ºC

[ 精确质量 ]:
431.18600

[ PSA ]:
49.81000

[ LogP ]:
6.22240

[ 外观性状 ]:
固体

[ 储存条件 ]:
-20°C，密封，干燥

盐酸依沙维林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NW7524100

CHEMICAL NAME :: Isoquinoline, 1-(3,4-diethoxybenzyl)-6,7-diethoxy-, hydrochloride

CAS REGISTRY NUMBER :: 985-13-7

LAST UPDATED :: 199701

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C24-H29-N-O4.Cl-H

MOLECULAR WEIGHT :: 432.00

WISWESSER LINE NOTATION :: T66 CNJ B1R CO2 DO2& HO2 FO2 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 660 mg/kg

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

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 5,69,1950

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 86 mg/kg

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

REFERENCE :: APFRAD Annales Pharmaceutiques Francaises. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1943- Volume(issue)/page/year: 9,585,1951 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5434 No. of Facilities: 26 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1324 (estimated) No. of Female Employees: 667 (estimated)

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盐酸依沙维林安全信息

[ 危险品运输编码 ]:
UN 3249

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2933499090

盐酸依沙维林海关

[ 海关编码 ]: 2933499090

[ 中文概述 ]:
2933499090. 其他含喹琳或异喹啉环系的化合物〔但未进一步稠合的〕. 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 ]:
2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%