| 名称 | Nicainoprol |
| 描述 | Nicainoprol (RU-42924) is a fast-sodium-channel blocking drug. Nicainoprol is a potent antiarrhythmic agent. |
| 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 | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (148.87 mM)
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| 关键字 | Na+ channels | inhibit | Sodium Channel | Inhibitor | Na channels | Nicainoprol | RU 42924 | RU42924 |
| 相关产品 | Lidocaine hydrochloride | Benzocaine | Valproic Acid | Lidocaine | Mebeverine hydrochloride | Safinamide | Procaine | Amitriptyline hydrochloride | L-Aspartic aicd sodium | Lidocaine Hydrochloride hydrate | Riluzole | Phenytoin sodium |
| 相关库 | 神经保护化合物库 | 抑制剂库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | NO PAINS 化合物库 | 离子通道库 | 膜蛋白靶向化合物库 | 疼痛相关化合物库 | 表型筛选靶点鉴定库 |
