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1-异丁氧基-2-吡咯烷基-3-(N-苄基苯胺基)丙烷盐酸盐

用途

Bepridil hydrochloride (CERM 1978) 是一种钙离子通道 (calcium channel) 抑制剂,具有抗心绞痛的作用。

名称

[ CAS 号 ]:
68099-86-5

[ 中文名 ]:
1-异丁氧基-2-吡咯烷基-3-(N-苄基苯胺基)丙烷盐酸盐

[ 英文名 ]:
Bepridil hydrochloride

[英文别名 ]:

Bepricor
BEPRIDIL HYDROCHLORIDE
Einecs 268-472-2
1978cerm
cordium

生物活性

[ 描述 ]:

Bepridil hydrochloride (CERM 1978) 是一种钙离子通道 (calcium channel) 抑制剂,具有抗心绞痛的作用。

[ 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 ]

Calcium channel[1]

[体外研究]

盐酸Bepridil是一种钙通道阻滞剂,具有抗心绞痛作用[1]。

[体内研究]

盐酸Bepridil(21 mg/kg)可降低心率和平均动脉压,降低平均冠状动脉血管阻力并增加大鼠的每搏输出量[1]。

[参考文献]

[1]. Flaim SF, et al. Effects of bepridil hydrochloride on cardiocirculatory dynamics, coronary vascular resistance, and cardiac output distribution in normal, conscious rats. J Cardiovasc Pharmacol. 1988 Mar;11(3):363-72.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.054g/cm3

[ 沸点 ]:
492.3ºC at 760 mmHg

[ 分子式 ]:
C₂₄H₃₅ClN₂O

[ 分子量 ]:
403.00100

[ 闪点 ]:
133.2ºC

[ 精确质量 ]:
402.24400

[ PSA ]:
15.71000

[ LogP ]:
5.57010

[ 储存条件 ]:
2-8℃

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY1161000

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

CAS REGISTRY NUMBER :: 68099-86-5

LAST UPDATED :: 199806

DATA ITEMS CITED :: 6

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

MOLECULAR WEIGHT :: 403.06

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 :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1256,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2069 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1256,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 50600 ug/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 225,133,1977 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7800 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3155,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7800 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - physical

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3155,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3300 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,3130,1991