尼卡普醇 T4539

Product Introduction
Bioactivity


英文名: Nicainoprol

描述: Nicainoprol (RU-42924) 是一种快速钠通道阻断剂，是有效的抗心律失常剂。

体外活性: The antiarrhythmic agent Nicainoprol is a fast-sodium-channel blocking drug that also protects isolated rat hearts against reperfusion arrhythmias. However, it is without beneficial effects on cardiac hemodynamics and biochemical parameters, in contrast to the ACE inhibitor[1].

体内活性: 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. Nicainoprol (10 μM, 5 μM and 100 μM) in isolated working rat hearts induces concentration-related protection against reperfusion arrhythmia without changing the cardiodynamics while 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (148.87 mM)


关键字: Na+ channels | inhibit | Sodium Channel | Inhibitor | Na channels | Nicainoprol | RU 42924 | RU42924

相关产品: Orphenadrine hydrochloride | DS-1971a | Vernakalant Hydrochloride | BmK-M1 | Permethrin | Dibucaine | Propafenone hydrochloride | Sodium Channel inhibitor 2 | A-803467 | Solpecainol

相关库: Ion Channel Inhibitor Library | ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Sodium Channel Blocker Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途