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新型慢通道钙阻滞剂FR 34235与硝苯地平对麻醉犬血流动力学和心肌耗氧量的比较效应

Comparative effects of FR 34235, a new slow channel calcium blocker, and nifedipine on hemodynamics and myocardial oxygen consumption in the anesthetized dog.

作者信息

Gross G J, Warltier D C, Hardman H F

出版信息

Gen Pharmacol. 1983;14(6):677-80. doi: 10.1016/0306-3623(83)90167-2.

DOI:10.1016/0306-3623(83)90167-2
PMID:6662348
Abstract

Five doses of two dihydropyridine calcium antagonists, FR 34235 and nifedipine, were given intravenously to anesthetized dogs to determine effects on hemodynamics and myocardial oxygen balance. Both agents produced dose-related decreases in mean arterial blood pressure and tension time index with little effect on heart rate, dP/dt or myocardial contractile force except at high doses where small decreases were observed. Coronary blood flow increased markedly in the presence of both agents with a maximum increase observed at doses of 10 and 30 micrograms/kg for FR 34235 and nifedipine, respectively. Both compounds decreased myocardial oxygen extraction at all doses and reduced myocardial oxygen consumption at higher doses. These results indicate that FR 34235, a new slow channel calcium blocker, is a potent coronary vasodilator. In addition, this compound possesses oxygen-sparing activity at higher doses.

摘要

将两种二氢吡啶类钙拮抗剂FR 34235和硝苯地平的五剂分别静脉注射给麻醉犬,以确定其对血流动力学和心肌氧平衡的影响。两种药物均使平均动脉血压和张力时间指数呈剂量依赖性下降,对心率、dp/dt或心肌收缩力影响较小,高剂量时除外,此时观察到有小幅下降。两种药物均使冠状动脉血流量显著增加,FR 34235和硝苯地平分别在10和30微克/千克剂量时观察到最大增加。两种化合物在所有剂量下均降低心肌氧摄取,在较高剂量时降低心肌氧消耗。这些结果表明,新型慢通道钙阻滞剂FR 34235是一种强效冠状动脉血管扩张剂。此外,该化合物在较高剂量时具有氧节省活性。

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