异丙托溴铵

异丙托溴铵用途

水合异丙托溴铵(Sch 1000)是毒蕈碱受体拮抗剂,M1、M2和M3受体的IC50分别为2.9 nM、2 nM和1.7 nM。水合异丙托溴铵可松弛平滑肌,可用于COPD(慢性阻塞性肺疾病)和哮喘的研究[1][2][3][4][5]。

异丙托溴铵名称

[ 英文名 ]:
3-(3-Hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-(1-methylethyl)-8-azoniabicyclo(3.2.1)octane bromide monohydrate

[中文别名 ]:

[英文别名 ]:

Ipratropium Bromide Monohydrate

异丙托溴铵生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[ 靶点 ]

muscarinic M1 receptor:2.9 nM (IC50)

muscarinic M2 receptor:2 nM (IC50)

muscarinic M3 receptor:1.7 nM (IC50)

[体外研究]

水合异丙托溴铵(1 nM,10 nM,100 nM；15分钟)通过破坏线粒体膜电位发挥毒性作用[1]。水合异丙托溴铵(1 nM-1μM；4 h)以剂量反应方式(EC50=22.7 nM)增加离体灌注心脏缺血/再灌注实验中的梗死面积[1]。水合异丙托溴铵(0.001 nM-0.1 mM；2 h)在缺氧处理4 h后抑制成年大鼠心肌细胞生长[1]。细胞活力测定[1]细胞系：成年大鼠心肌细胞浓度：0.001 nM-0.1 mM孵育时间：黑暗中2小时；结果：缺氧4h前,细胞存活率呈剂量依赖性,0.1mM剂量时抑制率为52.7%。

[体内研究]

水合异丙托溴铵(1.0μg/kg；静脉注射；单剂量)增强迷走神经刺激,包括支气管收缩[2]。水合异丙托溴铵(0.04 mg/20 mL和0.20 mg/20 mL；吸入30分钟,速率=30 mL/30分钟)可以通过减少中性粒细胞的实质炎症浸润来保护肺部免受镉诱导的急性中性粒细胞炎症[4]。动物模型：Dunkin Hartley株豚鼠[2]剂量：0.1-1μg/kg给药：静脉注射；单剂量结果：0.3μg/kg对连接后毒蕈碱受体几乎没有阻断作用,0.5μg/kg抑制ACh诱导的支气管收缩。动物模型：雄性Sprague-Dawley大鼠(300-350 g)[4]剂量：0.04 mg/20 mL和0.20 mg/20 mL给药：吸入；雾化速度为30mL/30min；30min结果：对健康大鼠记录的任何参数均无明显影响,但对镉引起的炎症反应有保护作用。

[参考文献]

[1]. Fryer AD, et al. Maclagan, Ipratropium bromide potentiates bronchoconstriction induced by vagal nerve stimulation in the guinea-pig. Eur J Pharmacol, 1987. 139(2): p. 187-91.

[2]. Harvey, et al. Maddock, Ipratropium Bromide-Mediated Myocardial Injury in In Vitro Models of Myocardial Ischaemia/Reperfusion. Toxicol Sci, 2014.

[3]. Maria Prat, et al. Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1736-1741.

[4]. Wenhui Zhang, et al. Anti-inflammatory effects of formoterol and ipratropium bromide against acute cadmium-induced pulmonary inflammation in rats. Eur J Pharmacol. 2010 Feb 25;628(1-3):171-8.

[5]. Venkatasamy R, et al. Novel relaxant effects of RPL554 on guinea pig tracheal smooth muscle contractility. Br J Pharmacol. 2016 Aug;173(15):2335-51.

异丙托溴铵物理化学性质

[ 分子式 ]:
C₂₀H₃₂BrNO₃

[ 分子量 ]:
414.377

[ 精确质量 ]:
413.156555

[ PSA ]:
46.53000

[ LogP ]:
0.02610

[ 外观性状 ]:
white

[ 储存条件 ]:
室温，干燥

[ 水溶解性 ]:
H2O: soluble10mg/mL

异丙托溴铵MSDS

详细MSDS(安全技术说明书)

异丙托溴铵安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H332-H319

[ 警示性声明 ]:
P261-P301 + P312 + P330-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20/22-36

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
YM3700000

[ 海关编码 ]:
2933990090

异丙托溴铵海关

[ 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%

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