Godfraind T, Eglème C, Finet M, Jaumin P
Laboratory of General Pharmacodynamics and Pharmacology, Catholic University of Louvain, Bruxelles, Belgium.
Pharmacol Toxicol. 1987 Aug;61(2):79-84. doi: 10.1111/j.1600-0773.1987.tb01779.x.
We have studied the action of nifedipine and nisoldipine on the contractile activity of human isolated coronary arteries and human isolated auricular and ventricular muscles. Nisoldipine depressed dose dependently the spontaneous rhythmic contractions displayed by the coronary artery preparations and at 1 nM abolished these contractions. Nisoldipine was twenty times more potent than nifedipine as an inhibitor of increase in tone induced by depolarization (100 mM K+). The rhythmic activity induced by serotonin (10 microM) was about five times more sensitive to nisoldipine than to nifedipine. In both auricular and ventricular preparations, isoprenaline evoked an increase in the rate of force development and in the rate of relaxation. Nifedipine was five times (ventricular muscles) and ten times (auricular muscles) more potent than nisoldipine as a negative inotropic agent. The present observations in human isolated preparations indicate that nisoldipine shows a higher vascular selectivity than nifedipine.
我们研究了硝苯地平和尼索地平对人离体冠状动脉以及人离体心房和心室肌收缩活性的作用。尼索地平剂量依赖性地抑制冠状动脉制剂所显示的自发性节律性收缩,在1纳摩尔时可消除这些收缩。作为去极化(100毫摩尔钾离子)诱导的张力增加的抑制剂,尼索地平的效力比硝苯地平强20倍。血清素(10微摩尔)诱导的节律性活动对尼索地平的敏感性比对硝苯地平高约5倍。在心房和心室制剂中,异丙肾上腺素均可引起力量发展速率和舒张速率增加。作为负性肌力药,硝苯地平的效力比尼索地平高5倍(心室肌)和10倍(心房肌)。在人离体制剂中的当前观察结果表明,尼索地平比硝苯地平具有更高的血管选择性。