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新型钙通道阻滞剂FRC 8653与硝苯地平对麻醉犬的全身血流动力学及心肌耗氧量的比较研究。

Comparative studies of the systemic hemodynamics and myocardial oxygen consumption of FRC 8653, a new Ca++ channel blocker, and nifedipine in anesthetized dogs.

作者信息

Chibana T, Noguchi K, Ojiri Y, Sakanashi M

机构信息

Department of Pharmacology, School of Medicine, University of the Ryukyus, Okinawa, Japan.

出版信息

Jpn Heart J. 1992 Mar;33(2):239-52. doi: 10.1536/ihj.33.239.

DOI:10.1536/ihj.33.239
PMID:1593752
Abstract

Effects of FRC 8653, a new dihydropyridine derivative, on regional blood flow, cardiac function and myocardial oxygen consumption were examined and compared with those of nifedipine in anesthetized open-chest dogs. Intravenous administration of FRC 8653 at doses of 1, 3 and 10 micrograms/kg dose-dependently decreased aortic pressure and increased aortic, vertebral and coronary blood flow similar to nifedipine. No significant change was observed in left ventricular end-diastolic pressure, left ventricular positive dP/dt and heart rate following i.v. administration of FRC 8653. Myocardial oxygen consumption was dose-dependently decreased by FRC 8653. When changes in mean aortic pressure and aortic and coronary blood flow were compared at the same dose of 10 micrograms/kg i.v., both FRC 8653 and nifedipine showed almost the same degree of reduction of mean aortic pressure, but the time from drug administration to peak responses and the duration for which half the maximal effects were maintained, were significantly longer with FRC 8653 than nifedipine. Results suggest that FRC 8653 may be useful for the treatment of patients with hypertension and ischaemic heart disease.

摘要

在麻醉开胸犬中,研究了新型二氢吡啶衍生物FRC 8653对局部血流、心脏功能和心肌耗氧量的影响,并与硝苯地平进行了比较。静脉注射剂量为1、3和10微克/千克的FRC 8653,与硝苯地平相似,剂量依赖性地降低主动脉压,并增加主动脉、椎动脉和冠状动脉血流量。静脉注射FRC 8653后,左心室舒张末期压力、左心室dp/dt正值和心率未观察到明显变化。FRC 8653使心肌耗氧量呈剂量依赖性降低。当静脉注射相同剂量10微克/千克时,比较平均主动脉压以及主动脉和冠状动脉血流量的变化,FRC 8653和硝苯地平降低平均主动脉压的程度几乎相同,但FRC 8653从给药到达到峰值反应的时间以及维持最大效应一半的持续时间明显长于硝苯地平。结果表明,FRC 8653可能对高血压和缺血性心脏病患者的治疗有用。

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