Gross G J, Warltier D C, Hardman H F
Gen Pharmacol. 1983;14(6):677-80. doi: 10.1016/0306-3623(83)90167-2.
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.
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。