盐酸苄普地尔

盐酸苄普地尔用途

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) 是非选择性的,长效的钙离子通道 (Ca+ channel) 拮抗剂,钠离子、钾离子通道 (Na+, K+ channel) 抑制剂,具有抗心绞痛和抗 I 型心律失常作用。Bepridil hydrochloride hydrate 也是心脏 Na+/Ca2+ 交换 (NCX1) 抑制剂。Bepridil hydrochloride hydrate 可用于心血管疾病的研究。

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盐酸苄普地尔名称

[ CAS 号 ]:
74764-40-2

[ 中文名 ]:
盐酸苄普地尔

[ 英文名 ]:
Bepridil hydrochloride

[中文别名 ]:

苄普地尔盐酸盐

[英文别名 ]:

MFCD00065498
Unii-4W2p15D93m
l)-,monohydrochloride,monohydrate
angopril

盐酸苄普地尔生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 心血管疾病

[ 靶点 ]

Ca2+

[体外研究]

盐酸贝普地尔对犬冠状动脉血管平滑肌钙依赖性动作电位的阻断作用[2]。盐酸贝普地尔分别用0.5μM和30μM的ic50阻断培养心室细胞的Ca电流和Na电流[4]。盐酸贝普地尔在E4031(5μM)阻断IKr的情况下,以浓度依赖性的方式降低IKs[5]。

[体内研究]

单次给药后盐酸贝普利地尔的半衰期平均为33±15小时[6]。

[参考文献]

[1]. A Gill, et al. Pharmacology of Bepridil. Am J Cardiol. 1992 Apr 9;69(11):11D-16D.

[2]. D R Harder, et al. Bepridil Blockade of Ca2+-dependent Action Potentials in Vascular Smooth Muscle of Dog Coronary Artery. J Cardiovasc Pharmacol. Jul-Aug 1981;3(4):906-14.

[3]. Yasuhide Watanabe. Cardiac Na +/Ca 2+ Exchange Stimulators Among Cardioprotective Drugs. J Physiol Sci. 2019 Nov;69(6):837-849.

[4]. A Yatani, et al. Bepridil Block of Cardiac Calcium and Sodium Channels. J Pharmacol Exp Ther. 1986 Apr;237(1):9-17.

[5]. J C Wang, et al. Bepridil Differentially Inhibits Two Delayed Rectifier K(+) Currents, I(Kr) and I(Ks), in Guinea-Pig Ventricular Myocytes. Br J Pharmacol. 1999 Dec;128(8):1733-8.

[6]. L Z Benet, et al. Pharmacokinetics and Metabolism of Bepridil. Am J Cardiol. 1985 Mar 15;55(7):8C-13C.

盐酸苄普地尔物理化学性质

[ 熔点 ]:
91 ±2°

[ 分子式 ]:
C₂₄H₃₇ClN₂O₂

[ 分子量 ]:
421.01600

[ 精确质量 ]:
420.25400

[ PSA ]:
24.94000

[ LogP ]:
5.50580

[ 外观性状 ]:
powder | white

[ 储存条件 ]:
Desiccate at RT

盐酸苄普地尔MSDS

详细MSDS(安全技术说明书)

盐酸苄普地尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY1162000

CHEMICAL NAME :: 1-Pyrrolidineethanamine, beta-((2-methylpropoxy)methyl)-N-phenyl-N-(phenylmeth yl)-, monohydrochloride, monohydrate

CAS REGISTRY NUMBER :: 74764-40-2

LAST UPDATED :: 199506

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C24-H34-N2-O.Cl-H.H2-O

MOLECULAR WEIGHT :: 421.08

WISWESSER LINE NOTATION :: T5NTJ AY1O1Y1&1&1NR&1R &GH &QH

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 :: 6850 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >21300 ug/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1955 mg/kg

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

REFERENCE :: GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2802864

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 23,682,1992

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23500 ug/kg

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

REFERENCE :: GWXXBX German Offenlegungsschrift Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2802864

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盐酸苄普地尔安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

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

[ WGK德国 ]:
2

[ RTECS号 ]:
UY1162000

盐酸苄普地尔文献

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