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新型二氢吡啶衍生物依福地平对犬冠状动脉结扎所致心肌代谢变化的影响:与硝苯地平的比较。

Effect of efonidipine, a novel dihydropyridine derivative, on myocardial metabolic changes induced by coronary artery ligation in dogs: comparison with nifedipine.

作者信息

Yokoyama T, Ichihara K, Abiko Y

机构信息

Department of Pharmacology, Asahikawa Medical College, Japan.

出版信息

Fundam Clin Pharmacol. 1997;11(3):245-51. doi: 10.1111/j.1472-8206.1997.tb00192.x.

Abstract

Efonidipine is a dihydropyridine derivative having a vasodilating action, which is slower in onset and longer in duration than that of nifedipine. In the present study, we compared the effects of efonidipine with those of nifedipine on the ischemic myocardial metabolism in anesthetized dogs. The heart was made ischemic by ligating the left anterior descending coronary artery (LAD) completely for 3 or 30 min. Efonidipine or nifedipine was injected intravenously, 10 or 3 min, respectively, before the start of LAD occlusion. Efonidipine (0.01 or 0.03 mg/kg) decreased both blood pressure and heart rate, whereas nifedipine (0.003 mg/kg) decreased blood pressure and increased heart rate. The magnitude of decrease in mean blood pressure induced by 0.03 mg/kg efonidipine was similar to that induced by 0.003 mg/kg nifedipine. Although efonidipine did not modify the changes in myocardial carbohydrate metabolism induced by ischemia, it attenuated the ischemia-induced decrease in the myocardial level of adenosine triphosphate and energy charge potential. Nifedipine, however, did not modify the changes in both myocardial energy and carbohydrate metabolism induced by ischemia. The results suggest that efonidipine has a cardioprotective effect in the dog, probably because of its negative chronotropic effect.

摘要

依福地平是一种具有血管舒张作用的二氢吡啶衍生物,其起效比硝苯地平慢,作用持续时间比硝苯地平长。在本研究中,我们比较了依福地平和硝苯地平对麻醉犬缺血心肌代谢的影响。通过完全结扎左冠状动脉前降支(LAD)3分钟或30分钟使心脏缺血。在LAD闭塞开始前10分钟或3分钟分别静脉注射依福地平或硝苯地平。依福地平(0.01或0.03mg/kg)可降低血压和心率,而硝苯地平(0.003mg/kg)可降低血压并增加心率。0.03mg/kg依福地平引起的平均血压下降幅度与0.003mg/kg硝苯地平引起的相似。虽然依福地平没有改变缺血引起的心肌碳水化合物代谢变化,但它减轻了缺血引起的心肌三磷酸腺苷水平和能量电荷电位的下降。然而,硝苯地平没有改变缺血引起的心肌能量和碳水化合物代谢变化。结果表明,依福地平对犬具有心脏保护作用,可能是由于其负性变时作用。

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