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DPI 201-106的抗心律失常作用。

Antiarrhythmic effects of DPI 201-106.

作者信息

Scholtysik G, Williams F M

出版信息

Br J Pharmacol. 1986 Oct;89(2):287-92. doi: 10.1111/j.1476-5381.1986.tb10258.x.

DOI:10.1111/j.1476-5381.1986.tb10258.x
PMID:3779211
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1917020/
Abstract

The cardiotonic agent DPI 201-106 (4-[3-(4-diphenylmethyl-1-piperazinyl-2- hydroxypropyl]-1H-indole-2-carbonitrile) which modifies the sarcolemmal Na+ channel gating system and has electrophysiological properties of class III antiarrhythmics was investigated for local anaesthetic and antiarrhythmic activity. The compound action potential amplitude of cat cervical vagus nerves in vitro was decreased by DPI 201-106 in a concentration-dependent manner, the IC50 being 1.82 X 10(-5) M. This was paralleled by a slowing in conduction velocity and demonstrates local anaesthetic effects. Ventricular fibrillation which occurs in response to coronary artery reperfusion in rats was prevented by intravenous infusions of 0.3 mg kg-1 min-1 of DPI 201-106. The arrhythmogenic intravenous doses of aconitine in rats were increased following pretreatment with DPI 201-106 in a dose-dependent manner. DPI 201-106 did not protect against ouabain-induced arrhythmias in guinea-pigs. The results demonstrate that DPI 201-106 has local anaesthetic effects and is a potential antiarrhythmic.

摘要

强心剂DPI 201-106（4-[3-(4-二苯甲基-1-哌嗪基)-2-羟丙基]-1H-吲哚-2-腈）可改变肌膜钠通道门控系统，具有Ⅲ类抗心律失常药的电生理特性，对其局部麻醉和抗心律失常活性进行了研究。体外实验中，DPI 201-106可使猫颈迷走神经的复合动作电位幅度呈浓度依赖性降低，IC50为1.82×10(-5)M。这伴随着传导速度减慢，表明其具有局部麻醉作用。静脉输注0.3mg kg-1 min-1的DPI 201-106可预防大鼠冠状动脉再灌注时发生的心室颤动。用DPI 201-106预处理大鼠后，乌头碱致心律失常的静脉给药剂量呈剂量依赖性增加。DPI 201-106对豚鼠哇巴因诱导的心律失常无保护作用。结果表明，DPI 201-106具有局部麻醉作用，是一种潜在的抗心律失常药。

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