S81437 |
Ipratropium bromide |
源叶(MedMol) | 98% |
- 产品描述: Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma
- 靶点: 2.9 nM (mAChR M1), 2 nM (mAChR M2), and 1.7 nM (mAChR M3);AChR
- 体外研究:
Ipratropium bromide (1 nM, 10 nM, 100 nM; 15 min) exerts its toxic effects via disruption of mitochondrial membrane potential. Ipratropium bromide (1 nM-1 μM; 4 h) increases infarct size in isolated perfused heart ischaemia/reperfusion experiments with a dose-responsive manner (EC50=22.7 nM). Ipratropium bromide (0.001 nM-0.1 mM; 2 h) inhibits adult rat cardiac myocyte growth after 4 h hypoxia treatment. Cell Viability Assay Cell Line: Adult Rat Cardiac Myocyte Concentration: 0.001 nM-0.1 mM Incubation Time: 2 h in dark; prior to 4 h hypoxia Result: Resulted cell viability in a dose-dependent manner, with the inhibition rate of 52.7% at 0.1 mM dose.
- 体内研究:
Ipratropium bromide (1.0 μg/kg; i.v.; single dose) enhances vagal nerve stimulation induing bronchoconstriction. Ipratropium bromide (0.04 mg/20 mL and 0.20 mg/20 mL; 30 min, rate=30 mL/30 min) can protect the lungs against the cadmium-induced acute neutrophilic inflammation by reducing the parenchyma inflammatory infiltration of neutrophils. Animal Model: Guinea-pigs of the Dunkin Hartley strain. Dosage: 0.1-1 μg/kg Administration: Intravenous injection; single dose Result: Resulted little blocking effect on post-junctional muscarinic receptors at 0.3 μg/kg, and inhibited ACh-induced bronchoconstriction at 0.5 μg/kg. Animal Model: Male Sprague-Dawley rats (300-350 g) Dosage: 0.04 mg/20 mL and 0.20 mg/20 mL Administration: Inhalation; atomization rate of 30 mL/30 min; 30 min Result: Had no significant effects on any parameters recorded in healthy rats but exerted a protective effect against the inflammatory reaction elicited by cadmium.
- 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.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.425 ml 12.125 ml 24.25 ml 5 mM 0.485 ml 2.425 ml 4.85 ml 10 mM 0.243 ml 1.213 ml 2.425 ml 50 mM 0.049 ml 0.243 ml 0.485 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)