盐酸贝凡洛尔

盐酸贝凡洛尔用途

Bevantolol hydrochloride 是一种选择性的 β1/α1-肾上腺素受体 (β1/α1-adrenergic receptor) 拮抗剂,在大鼠大脑皮层中的 pKi 值分别为 7.83、6.9。Bevantolol hydrochloride 是有效的 Ca2+ 拮抗剂。

盐酸贝凡洛尔名称

[ CAS 号 ]:
42864-78-8

[ 中文名 ]:
盐酸贝凡洛尔

[ 英文名 ]:
Bevantolol hydrochloride

[中文别名 ]:

[英文别名 ]:

UNII:4VB9HU07BC
Bevantolol Hydrochloride

盐酸贝凡洛尔生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 代谢疾病

研究领域 >> 神经疾病

[ 靶点 ]

pKi: 7.83 (β1-adrenergic receptor), 6.9 (α1-adrenergic receptor), 6.23 (β2-adrenergic receptor) and Ca2+[1][2]

[体外研究]

盐酸贝伐洛尔对β2肾上腺素能受体的pKi为6.23[1]。

[体内研究]

盐酸贝万托洛尔(200mg/kg；口服,6周)可显著降低β1肾上腺素受体mRNA的表达水平[2]。动物模型：雄性Wistar大鼠体重250-300g[2]剂量：200mg/kg给药：PO,给药6周,结果：β1肾上腺素能受体mRNA表达水平显著降低。

[参考文献]

[1]. M Takita, et al. Selectivity of Bevantolol Hydrochloride Towards Alpha- And Beta-Adrenoceptor Subtypes in Rat Cerebral Cortex. Jpn J Pharmacol. 1992 Feb;58(2):193-6.

[2]. Takahiro Horinouchi, et al. Different Changes of Plasma Membrane Beta-Adrenoceptors in Rat Heart After Chronic Administration of Propranolol, Atenolol and Bevantolol. Life Sci. 2007 Jul 12;81(5):399-404.

盐酸贝凡洛尔物理化学性质

[ 沸点 ]:
518.3°C

[ 分子式 ]:
C₂₀H₂₈ClNO₄

[ 分子量 ]:
381.894

[ 精确质量 ]:
381.170685

[ PSA ]:
59.95000

[ LogP ]:
3.77710

[ 储存条件 ]:
室温，干燥

盐酸贝凡洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UB2709000

CHEMICAL NAME :: 2-Propanol, 1-((3,4-dimethoxyphenethyl)amino)-3-(m-tolyloxy)-, monohydrochloride

CAS REGISTRY NUMBER :: 42864-78-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C20-H27-N-O4.Cl-H

MOLECULAR WEIGHT :: 381.94

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 :: 460 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: 26,364,1995

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 130 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: 26,364,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 25100 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: 26,364,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 419 mg/kg

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

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 3,85,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 16200 mg/kg/52W-C

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - hypermotility, diarrhea

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: 25,3937,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2730 mg/kg/13W-C

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Kidney, Ureter, Bladder - hematuria Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

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: 25,3905,1991

盐酸贝凡洛尔安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2922299090

盐酸贝凡洛尔合成路线

详细合成路线

盐酸贝凡洛尔上下游产品

盐酸贝凡洛尔上游产品

盐酸贝凡洛尔下游产品

盐酸贝凡洛尔海关

[ 海关编码 ]: 2922299090

[ 中文概述 ]:
2922299090. 其他氨基(萘酚、酚)及醚、酯〔包括它们的盐, 但含有一种以上含氧基的除外〕. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ Summary ]:
2922299090. other amino-naphthols and other amino-phenols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%