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CAS No.: 76252-06-7

Nicainoprol/尼卡普醇 Catalog No. CSN17076

Synonyms: RU-42924;CAS-924;尼卡普醇

Nicainoprol is a sodium channels blocker which is used as an antiarrhythmic agent.

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描述Genetic defects in sodium channel-related genes can cause a loss- or gain-of-function of sodium channel current (I_Na) 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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7067 mL
- 13.5334 mL
- 27.0667 mL
- 5 mM
- 0.5413 mL
- 2.7067 mL
- 5.4133 mL
- 10 mM
- 0.2707 mL
- 1.3533 mL
- 2.7067 mL

技术信息

CAS号

76252-06-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H27N3O3

运输

蓝冰

分子量

369.46

别名

RU-42924;CAS-924;尼卡普醇

溶解度

DMSO	115.0 mg/mL (311.3 mM)
Water	17.0 mg/mL (46.0 mM) warming

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