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(±)-Pronethalo hydrochloride

(±)-Pronethalo hydrochloride用途

Pronethalol ((±)-Pronethalo) 是一种非选择性的 β-肾上腺素 (β-adrenergic) 拮抗剂。 Pronethalol 是有效的 Sox2 表达抑制剂。Pronethalol 可预防和逆转洋地黄引起的室性心律失常,也可以限制脑动静脉畸形 (AVMs)。

(±)-Pronethalo hydrochloride名称

[ CAS 号 ]:
51-02-5

[ 中文名 ]:
盐酸丙萘洛尔

[ 英文名 ]:
Pronethalol hydrochloride

[中文别名 ]:

[英文别名 ]:

(±)-Pronethalo hydrochloride生物活性

[ 描述 ]:

Pronethalol ((±)-Pronethalo) 是一种非选择性的 β-肾上腺素 (β-adrenergic) 拮抗剂。 Pronethalol 是有效的 Sox2 表达抑制剂。Pronethalol 可预防和逆转洋地黄引起的室性心律失常,也可以限制脑动静脉畸形 (AVMs)。

[ 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 >> 神经疾病

[体外研究]

普罗沙洛尔(2,10,20μM)以剂量和时间依赖的方式抑制ReNcell-VM细胞中EGFP的表达。普诺沙洛尔(10μM；2天)在治疗2天后将Sox2表达降低到10%以下[2]。

[体内研究]

普诺沙洛尔(0.15 mg/g；每日；持续14天)可稳定Mgp-/–小鼠的内皮分化、管腔形成和改善脑动静脉畸形(AVMs)[2]。

[参考文献]

[1]. Aroesty JM, et al. The effects of a beta-adrenergic blocking agent, pronethalol, on digitalis-induced ventricular arrhythmias. Am Heart J. 1966 Apr;71(4):503-508.

[2]. Jiayi Yao, et al. Elevated endothelial Sox2 causes lumen disruption and cerebral arteriovenous malformations. J Clin Invest. 2019 Jun 24;129(8):3121-3133.

(±)-Pronethalo hydrochloride物理化学性质

[ 密度 ]:
1.074g/cm3

[ 沸点 ]:
322.4ºC at 760mmHg

[ 分子式 ]:
C15H20ClNO

[ 分子量 ]:
265.77800

[ 闪点 ]:
84.3ºC

[ 精确质量 ]:
265.12300

[ PSA ]:
32.26000

[ LogP ]:
4.06410

[ 折射率 ]:
1.596

[ 储存条件 ]:
2-8°C，密封，干燥

(±)-Pronethalo hydrochloride毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QJ9275000
CHEMICAL NAME :
Naphthalenemethanol, alpha-((isopropylamino)methyl)-, hydrochloride
CAS REGISTRY NUMBER :
51-02-5
LAST UPDATED :
199512
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C15-H19-N-O.Cl-H
MOLECULAR WEIGHT :
265.81
WISWESSER LINE NOTATION :
L66J CYQ1MY1&1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
425 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 18,48,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
102 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IJPPAZ Indian Journal of Physiology and Pharmacology. (All India Institute of Medical Sciences, Dept. of Physiology, Ansari Nagar, New Delhi 110 029, India) V.1- 1957- Volume(issue)/page/year: 17,235,1973
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
35 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 18,48,1968 ** TUMORIGENIC DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
10 gm/kg/25W-C
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - tumors
REFERENCE :
NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 207,594,1965 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,227,1977 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,227,1977 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987

(±)-Pronethalo hydrochloride安全信息

[ 海关编码 ]:
2922199090

(±)-Pronethalo hydrochloride海关

[ 海关编码 ]: 2922199090

[ 中文概述 ]:
2922199090. 其他氨基醇及其醚，酯和它们的盐（但含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 ]:
2922199090. other amino-alcohols, 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%

推荐生产厂家/供应商：

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥1789.0/10mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：李先生

产品详情：Pronethalol hydrochloride

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥1764.0/10mg

联系人：夏言

产品详情：Pronethalol hydrochloride

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相关化合物

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