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拉贝洛尔

拉贝洛尔用途

拉贝洛尔(AH5158)是一种口服活性选择性α1-和非选择性β-肾上腺素能受体竞争性拮抗剂。拉贝洛尔是一种抗高血压药物,可用于心血管疾病的研究,如妊娠高血压[1][2][3]。

拉贝洛尔名称

[ CAS 号 ]:
36894-69-6

[ 中文名 ]:
拉贝洛尔

[ 英文名 ]:
Labetalol

[中文别名 ]:

拉本他乐

[英文别名 ]:

Amipress
MFCD00242941
Labetalol hydrochloride
Labetalol
Pressalolo
Trandate
Labrocol
rac Labetalol
labetolol
Ipolab

拉贝洛尔生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

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 >> 炎症/免疫

[ 靶点 ]

α1-adrenergic receptor

β-adrenoceptor

[体外研究]

拉贝洛尔对豚鼠心脏和肺膜上的β-肾上腺素能位点表现出更大的亲和力(IC50分别为0.8和4.0μM)[2]。拉贝洛尔对兔子宫膜上的α-肾上腺素能结合位点(IC50=15μm)有亲和力。Labctalol对心脏膜β结合位点的结合亲和力是子宫膜α结合位点的19倍[2]。

[体内研究]

拉贝洛尔(10 mg/kg；i.h.)通过血脑屏障,在注射后90分钟,在10天大鼠幼鼠大脑中达到2.1 ug/g组织水平[4]。拉贝洛尔(5.0 mg/kg；i.p.)可减弱尾波休克应激大鼠的循环IL-1β和IL-6[5]。

[参考文献]

[1]. Brogden RN, et al. Labetalol: a review of its pharmacology and therapeutic use in hypertension. Drugs. 1978;15(4):251-270.

[2]. Greenslade FC, et al. Labetalol binding to specific alpha- and beta-adrenergic sites in vitro and its antagonism of adrenergic responses in vivo. J Mol Cell Cardiol. 1979 Aug;11(8):803-11.

[3]. Easterling T, et al. Oral antihypertensive regimens (nifedipine retard, labetalol, and methyldopa) for management of severe hypertension in pregnancy: an open-label, randomised controlled trial. Lancet. 2019 Sep 21;394(10203):1011-1021.

[4]. Erdtsieck-Ernste EB, et al. Changes in adrenoceptors and monoamine metabolism in neonatal and adult rat brain after postnatal exposure to the antihypertensive labetalol. Br J Pharmacol. 1992 Jan;105(1):37-44.

[5]. Johnson JD, et al. Catecholamines mediate stress-induced increases in peripheral and central inflammatory cytokines. Neuroscience. 2005;135(4):1295-307.

拉贝洛尔物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
552.7±50.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₂₄N₂O₃

[ 分子量 ]:
328.405

[ 闪点 ]:
288.1±30.1 °C

[ 精确质量 ]:
328.178680

[ PSA ]:
95.58000

[ LogP ]:
2.31

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.609

[ 储存条件 ]:
2-8°C

拉贝洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV5375500

CHEMICAL NAME :: Benzamide, 2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)am ino)ethyl)-

CAS REGISTRY NUMBER :: 36894-69-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C19-H24-N2-O3

MOLECULAR WEIGHT :: 328.45

WISWESSER LINE NOTATION :: ZVR BQ EYQ1MY1&2R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 8571 mg/kg/D

TOXIC EFFECTS :: Behavioral - changes in psychophysiological tests

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 282,1824,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 240 mg/kg/14D

TOXIC EFFECTS :: Peripheral Nerve and Sensation - paresthesis

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,580,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2 mg/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, allergic (after systemic exposure)

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 104,729,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,229,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >50 mg/kg

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

REFERENCE :: PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,229,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 660 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #5326774

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 97500 ug/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #5326774

拉贝洛尔安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2924299090

拉贝洛尔上下游产品

拉贝洛尔上游产品

拉贝洛尔下游产品

拉贝洛尔海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%