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通过使用犬离体血液灌注心脏标本揭示的苄普地尔的冠状血管扩张和心脏作用概况。

Profile of coronary vasodilator and cardiac actions of bepridil revealed by use of isolated, blood-perfused heart preparations of the dog.

作者信息

Kawada M, Satoh K, Taira N

出版信息

J Cardiovasc Pharmacol. 1983 Jul-Aug;5(4):604-12. doi: 10.1097/00005344-198307000-00015.

Abstract

We investigated the coronary vasodilator and cardiac actions of bepridil in various isolated, blood-perfused dog heart preparations. Intra-arterial bepridil increased blood flow in all preparations. In sinoatrial (SA) node preparations bepridil decreased sinus rate and produced atrial standstill in large doses. In paced atrioventricular (AV) node preparations, bepridil injected into the posterior septal artery (which supplies the AV node) increased AV conduction time (i.e., AV nodal conduction time) and in large doses produced second- or third-degree AV block. In the same preparations, bepridil in large doses injected into the anterior septal artery (which supplies the His-Purkinje ventricular system) prolonged AV conduction time (i.e., intraventricular conduction time). In paced papillary muscle preparations, bepridil reduced force of contraction only in large doses. In spontaneously beating papillary muscle preparations, bepridil decreased the rate of automaticity and the force of contraction as well. The order of effectiveness of bepridil on the above cardiovascular variables is as follows: coronary blood flow greater than AV nodal conduction greater than SA nodal automaticity much greater than ventricular automaticity ventricular muscle contraction much greater than intraventricular conduction. The results indicate bepridil to have a pharmacological profile different from that of verapamil, diltiazem, nifedipine, nicardipine, or KB-944.

摘要

我们在各种离体、血液灌注的犬心脏标本中研究了苄普地尔的冠状血管舒张作用和心脏效应。动脉内注射苄普地尔可使所有标本中的血流量增加。在窦房(SA)结标本中,苄普地尔可降低窦性心率,大剂量时可导致心房停搏。在起搏的房室(AV)结标本中,注入供应房室结的后间隔动脉中的苄普地尔可增加房室传导时间(即房室结传导时间),大剂量时可产生二度或三度房室传导阻滞。在相同标本中,注入供应希氏-浦肯野心室系统的前间隔动脉中的大剂量苄普地尔可延长房室传导时间(即室内传导时间)。在起搏的乳头肌标本中,苄普地尔仅在大剂量时才降低收缩力。在自发搏动的乳头肌标本中,苄普地尔也降低自律性频率和收缩力。苄普地尔对上述心血管变量的作用效果顺序如下:冠状血流量>房室结传导>窦房结自律性>心室自律性>心室肌收缩>室内传导。结果表明,苄普地尔具有与维拉帕米、地尔硫䓬、硝苯地平、尼卡地平或KB-944不同的药理学特征。

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