拉贝洛尔

• 常用名: 拉贝洛尔
• 英文名: Labetalol
• CAS号: 36894-69-6
• 分子量: 328.405
• 密度: 1.2±0.1 g/cm3
• 沸点: 552.7±50.0 °C at 760 mmHg
• 分子式: C₁₉H₂₄N₂O₃
• 熔点: N/A
• 闪点: 288.1±30.1 °C

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

• 中文名: 拉贝洛尔
• 英文名: labetalol
• 中文别名: 2-羟基-5-{1-羟基-2-[(1-甲基-3-苯基丙基)氨基]乙基}苯甲酰胺 | 拉本他乐

拉贝洛尔生物活性

• 描述: 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]。
• 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

拉贝洛尔安全信息

• 危害码 (欧洲): Xi
• 海关编码: 2924299090

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%

拉贝洛尔英文别名

• 2-Hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide
• 2-Hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide hydrochloride (1:1)
• Amipress
• MFCD00242941
• Labetalol hydrochloride
• benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-, monohydrochloride
• Labetalol
• Benzamide, 2-hydroxy-5-(1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)ethyl)-
• Pressalolo
• Trandate
• 2-Hydroxy-5-{1-hydroxy-2-[(4-phenyl-2-butanyl)amino]ethyl}benzamide
• Salicylamide, 5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-, hydrochloride
• Benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-, hydrochloride (1:1)
• Benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-
• Labrocol
• 2-hydroxy-5-{1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl}benzamide hydrochloride
• 2-Hydroxy-5-{1-hydroxy-2-[(4-phenyl-2-butanyl)amino]ethyl}benzamide hydrochloride (1:1)
• 2-Hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]benzamide hydrochloride
• 2-Hydroxy-5-(1-hydroxy-2-((4-phenylbutan-2-yl)amino)ethyl)benzamide hydrochloride
• 2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide,hydrochloride
• 5-[1-Hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]salicylamide hydrochloride
• 2-hydroxy-5-{1-hydroxy-2-[(1-méthyl-3-phénylpropyl)amino]éthyl}benzamide chlorhydrate
• rac Labetalol
• labetolol
• Ipolab
• UNII:R5H8897N95
• 2-Hydroxy-5-{1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl}benzolcarboxamidhydrochlorid
• LABETALOL HCL
• EINECS 253-258-3