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Nicainoprol(RU-42924)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nicainoprol(RU-42924)图片
CAS NO:76252-06-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议

产品介绍
Nicainoprol (RU-42924) 是一种快速钠通道阻断药,是一种有效的抗心律失常药物。
Cas No.76252-06-7
别名尼卡普醇,RU-42924
Canonical SMILESO=C(N1CCCC2=C1C(OCC(O)CNC(C)C)=CC=C2)C3=CC=CN=C3
分子式C21H27N3O3
分子量369.46
溶解度DMSO : ≥ 29 mg/mL (78.49 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

The antiarrhythmic agent Nicainoprol, a fast-sodium-channel blocking drug, also protected isolated rat hearts against reperfusion arrhythmias, but is without beneficial effects on cardiac hemodynamics and biochemical parameters, in contrast to the ACE inhibitor[1].

The effect of the novel antiarrhythmic agent Nicainoprol on coronary occlusion and reperfusion arrhythmia is investigated in isolated working rat hearts and in anesthetized rats. In isolated working rat hearts Nicainoprol (10 μM, 5 μM and 100 μM) induces concentration-related protection against reperfusion arrhythmia without changing 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 cardiac tissue 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 post occlusion (0-30 min) period, the percentage of animals with premature ventricular complexes (PVCs) and ventricular tachycardia while completely preventing the occurrence of ventricular fibrillation. In the reperfusion period no animal treated with 5 mg/kg and 12% of the rats treated with 10 mg/kg showed PVCs (the only form of arrhythmia observed in this period) versus 60% of the control rats. Both doses of Nicainoprol induces a decrease in heart rate, blood pressure and myocardial oxygen consumption. The ratio of infarct mass to ventricular 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 treatment of arrhythmias associated with acute myocardial infarction[2].

[1]. Linz W, et al. Cardiac arrhythmias are ameliorated by local inhibition of angiotensin formation and bradykinin degradation with the converting-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 reperfusion arrhythmia and myocardial infarct size in the anesthetized rat. Eur J Pharmacol. 1987 Nov 17;143(3):391-401.