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通过使用血液灌注的犬乳头肌同时评估冠状动脉扩张剂对冠状动脉血流量和心肌收缩力的影响。

Simultaneous assessment of effects of coronary vasodilators on the coronary blood flow and the myocardial contractility by using the blood-perfused canine papillary muscle.

作者信息

Himori N, Ono H, Taira N

出版信息

Jpn J Pharmacol. 1976 Aug;26(4):427-35. doi: 10.1254/jjp.26.427.

Abstract

Effects of 6 coronary vasodilators on the coronary blood flow and the contractile force of the ventricular muscle were examined simultaneously by injecting these drugs to the arterially blood-perfused canine papillary muscle preparation. All compounds produced a dose-dependent increase in blood flow rate, and relative potencies determined on the basis of doses producing a 100% increase in blood flow rate, ED100, were in the descending order : nifedipine greater than verapamil greater than diltiazem greater than dilazep greater than dipyridamole greater than carbochromen, and approximately 1 : 1/12 : 1/26 : 1/100 : 1/300 : 1/500. All drugs except for dipyridamole caused a dose-dependent decrease in the developed tension of the papillary muscle, although nifedipine and diltiazem in low doses produced a slight increase. Relative potencies determined on the basis of doses producing a 50% decrease in developed tension, ID50, were as follows: nifedipine (1), verapamil (1/13), diltiazem (1/40), dilazep (1/100), and carbochromen (1/270). Ratios of the ID50 to ED100 were as follows: diltiazem (5.2), nifedipine (3.5), verapamil (3.5), dilazep (2.5), and carbochromen (1.8). The higher the value the more predominant on the coronary vascular bed or the less depressant on the myocardial contractility were their actions.

摘要

通过向动脉血灌注的犬乳头肌标本中注射6种冠状动脉血管扩张剂,同时检测它们对冠状动脉血流量和心室肌收缩力的影响。所有化合物均使血流速率呈剂量依赖性增加,根据使血流速率增加100%的剂量(ED100)确定的相对效价顺序为:硝苯地平>维拉帕米>地尔硫卓>地拉齐普>双嘧达莫>卡波孟,约为1:1/12:1/26:1/100:1/300:1/500。除双嘧达莫外,所有药物均使乳头肌的张力呈剂量依赖性降低,尽管低剂量的硝苯地平和地尔硫卓会使其略有增加。根据使张力降低50%的剂量(ID50)确定的相对效价如下:硝苯地平(1)、维拉帕米(1/13)、地尔硫卓(1/40)、地拉齐普(1/100)和卡波孟(1/270)。ID50与ED100的比值如下:地尔硫卓(5.2)、硝苯地平(3.5)、维拉帕米(3.5)、地拉齐普(2.5)和卡波孟(1.8)。该值越高,其作用在冠状动脉血管床的主导性越强,对心肌收缩力的抑制作用越小。

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