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波吲洛尔

波吲洛尔用途

波平多洛是一种具有部分激动剂活性的口服β-肾上腺素能受体(ARs)拮抗剂。波平多洛对β1-和β2-ARs无选择性,对β3-AR亚型亲和力低。波平多洛是平多洛的前药,可用于原发性高血压和肾血管性高血压研究[1][2]。

波吲洛尔名称

[ CAS 号 ]:
62658-63-3

[ 中文名 ]:
波吲洛尔

[ 英文名 ]:
Bopindolol

[中文别名 ]:

吲苯脂心安

[英文别名 ]:

波吲洛尔生物活性

[ 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

[ 靶点 ]

β2 adrenoceptor

Beta-1 adrenergic receptor

Beta-3 adrenergic receptor

[体内研究]

波平多洛(静脉注射；l8、16和32μg/kg)对异丙肾上腺素诱发的心动过速具有剂量依赖性抑制作用,在麻醉狗中,该药物的效力是普萘洛尔的4倍[1]。波平多洛(腹腔注射；3.0 mg/kg)可降低去髓大鼠的舒张压(DBP)。而平多洛(1.0 mg/kg)在DBP中也产生了类似的降低,约为8 mmHg。它还会导致心率的剂量依赖性下降[2]。

[参考文献]

[1]. D W Harron, et al. Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy. Drugs

[2]. H Tanaka, et al. Hypotensive effect of bopindolol in pithed rats. Gen Pharmacol. 1993 Mar;24(2):373-5.

[3]. Y Hosohata, et al. Bopindolol is a slowly dissociating beta 1-adrenoceptor antagonist when compared to other beta-blockers. Biol Pharm Bull. 1995 Aug;18(8):1066-71.

波吲洛尔物理化学性质

[ 密度 ]:
1.143 g/cm3

[ 沸点 ]:
557ºC at 760 mmHg

[ 分子式 ]:
C₂₃H₂₈N₂O₃

[ 分子量 ]:
380.48000

[ 闪点 ]:
290.7ºC

[ 精确质量 ]:
380.21000

[ PSA ]:
63.35000

[ LogP ]:
4.85970

[ 折射率 ]:
1.592

波吲洛尔毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UB3773750

CHEMICAL NAME :: 2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((2-methyl-1H-indol-4- yl)oxy)-, benzoate (ester), (+-)-

CAS REGISTRY NUMBER :: 62658-63-3

LAST UPDATED :: 199701

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C23-H28-N2-O3

MOLECULAR WEIGHT :: 380.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 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: #2635209 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - other effects to embryo

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: 26,115,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1188 mg/kg

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

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

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: 23,4373,1989

波吲洛尔安全信息

[ 海关编码 ]:
2933990090

波吲洛尔制备

3.5g1-(叔丁氨基)-3-[(2-甲基-4-吲哚基)氧]-2-丙醇(Ⅰ)、26g苯甲酸和50ml六甲基磷酰胺，在室温下反应20h，得波吲洛尔。化合物(Ⅰ)也可先和苯甲酸在六甲基磷酰胺中成盐，再加入苯甲酸酐，在室温下反应20h，得波吲洛尔。

波吲洛尔海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%