Nicainoprol-RU-42924-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENicainoprolCat. No.: HY-100572CAS No.: 76252-06-7Synonyms: RU-42924分式: CHNO分量: 369.46作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO :

2、29 mg/mL (78.49 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7067 mL 13.5333 mL 27.0665 mL5 mM 0.5413 mL 2.7067 mL 5.4133 mL10 mM 0.2707 mL 1.3533 mL 2.7067 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Nicainoprol种快速钠通道 (sodi

3、um-channel) 阻断剂， 种有效的抗律失常剂。IC50 & Target Sodium Channel 1体外研究The antiarrhythmic agent Nicainoprol, a fast-sodium-channel blocking drug, also protected isolated rat hearts1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEagainst reperfusion arrhythmias, but is without beneficial effects on cardiac hem

4、odynamics and biochemicalparameters, in contrast to the ACE inhibitor 1.体内研究 The effect of the novel antiarrhythmic agent Nicainoprol on coronary occlusion and reperfusion arrhythmia isinvestigated in isolated working rat hearts and in anesthetized rats. In isolated working rat hearts Nicainoprol(10

5、 M, 5 M and 100 M) induces concentration-related protection against reperfusion arrhythmia withoutchanging the cardiodynamics, with the exception of a decrease in heart rate at the highest concentration.Enzyme levels (lactate dehydrogenase and creatine kinase) in the coronary venous effluent, and ca

6、rdiactissue concentrations of glycogen, lactate, ATP and creatine phosphate are not affected by Nicainoprol.Given to anesthetized rats, Nicainoprol (5 and 10 mg/kg i.v.) reduces dose dependently in the early postocclusion (0-30 min) period, the percentage of animals with premature ventricular comple

7、xes (PVCs) andventricular tachycardia while completely preventing the occurrence of ventricular fibrillation. In the reperfusionperiod no animal treated with 5 mg/kg and 12% of the rats treated with 10 mg/kg showed PVCs (the onlyform of arrhythmia observed in this period) versus 60% of the control r

8、ats. Both doses of Nicainoprol inducesa decrease in heart rate, blood pressure and myocardial oxygen consumption. The ratio of infarct mass toventricular mass is significantly reduced by 20% at a dose of 5 mg/kg and by 28% at the dose of 10 mg/kg.Nicainoprol could be useful in the prevention and tre

9、atment of arrhythmias associated with acute myocardialinfarction 2.REFERENCES1. Linz W, et al. Cardiac arrhythmias are ameliorated by local inhibition of angiotensin formation and bradykinin degradation with theconverting-enzyme inhibitor ramipril. Cardiovasc Drugs Ther. 1989 Dec;3(6):873-82.2. Martorana PA, et al. Effects of nicainoprol on reperfusion arrhythmia in the isolated working rat heart and on ischemia and reperfusionarrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401.McePdfHeightCaution: Product has not been fully validat