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 |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |