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Nicainoprol

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Chemical Structure| 76252-06-7 同义名 : RU-42924
CAS号 : 76252-06-7
货号 : A385536
分子式 : C21H27N3O3
纯度 : 99%+
分子量 : 369.457
MDL号 : MFCD00865522
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(81.2 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Genetic defects in sodium channel-related genes can cause a loss- or gain-of-function of sodium channel current (INa) leading to the manifestation of various disease phenotypes, including Brugada syndrome, long QT syndrome, progressive cardiac conduction disease, sick sinus syndrome, multifocal ectopic Purkinje-related premature contractions, and atrial fibrillation [3]. Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent. In isolated working rat hearts, nicainoprol (1 μM, 5 μM and 10 μM) induced concentration-related protection against reperfusion arrhythmia without changing the cardiodynamics. Given to anesthetized rats, nicainoprol (5 and 10 mg/kg i.v.) reduced 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. 5 or 10 mg/kg nicainoprol induced a decrease in heart rate, blood pressure and myocardial oxygen consumption. The ratio of infarct mass to ventricular mass was significantly reduced by 20% at a dose of 5 mg/kg and by 28% at the dose of 10 mg/kg. Thus, nicainoprol could be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction[4]. The intranodal conduction time (p ≤ 0.01) and the infranodal conduction time (p ≤ 0.001) increased, and the QRS duration (p ≤ 0.05) lengthened significantly even during 1 mg/kg/h intravenous administration of nicainoprol[5]. 1.5-2 mg/kg nicainoprol successfully terminated the tachycardia in 17 patients due to block in the retrograde tachycardia limb in 15 and the antegrade limb in 2 patients. Prolongation of the cycle length preceded the termination in each case[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Linz W, Scholkens BA, 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]Yang S, Xiao Y, et al. Discovery of a selective NaV1.7 inhibitor from centipede venom with analgesic efficacy exceeding morphine in rodent pain models. Proc Natl Acad Sci U S A. 2013 Oct 22;110(43):17534-9.

[3]Savio-Galimberti E, Argenziano M, Antzelevitch C. Cardiac Arrhythmias Related to Sodium Channel Dysfunction. Handb Exp Pharmacol. 2018;246:331-354.

[4]Martorana PA, Linz W, Göbel H, Petry P, Schölkens BA. 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;143(3):391-401.

[5]Sen S, Rettig G, Ozbek C, Fröhlig G, Schieffer H, Bette L. Electrophysiological effects of a new antiarrhythmic agent, nicainoprol, in humans. J Cardiovasc Pharmacol. 1986;8(1):144-150.

[6]Sen S, Rettig G, Heisel A, Ozbek C, Schieffer H. Electrophysiological effects of nicainoprol in patients with paroxysmal supraventricular tachycardias. Int J Cardiol. 1990;29(2):221-227.