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伊拉地平:一种对血小板功能和血管前列环素生成具有有益作用的强效钙阻滞剂。

Isradipine: a potent calcium blocker with beneficial effects on platelet function and vascular prostacyclin production.

作者信息

Weiss K, Fitscha P, O'Grady J, Sinzinger H

机构信息

Atherosclerosis Research Group (ASF), Vienna, Austria.

出版信息

Thromb Res. 1989 May 15;54(4):311-7. doi: 10.1016/0049-3848(89)90089-3.

Abstract

Calcium blockers inhibit platelet aggregation induced in vitro by various stimuli, such as ADP and collagen. In this study the in vitro effects of isradipine, a new dihydropyridine-derivative, and of nifedipine on platelet aggregation and malondialdehyde-production were tested. The lowest concentrations affecting ADP-induced platelet aggregation were 1.0 micrograms/ml isradipine and 12.5 micrograms/ml nifedipine. Both drugs exhibited an inhibitory action on malondialdehyde-production in concentrations 2 to 3 times lower than those affecting platelet aggregation. In vitro, PGI2-formation by rat aortic rings incubated with calcium blockers was increased in a dose-dependent manner. The lowest concentration of isradipine which increased PGI2-generation amounted 0.5 micrograms/ml. The corresponding value for nifedipine was 10 micrograms/ml. The findings demonstrate isradipine to be more potent than nifedipine in affecting in vitro platelet aggregation and enhancing PGI2-formation.

摘要

钙阻滞剂可抑制多种刺激物(如ADP和胶原)在体外诱导的血小板聚集。在本研究中,测试了新型二氢吡啶衍生物伊拉地平以及硝苯地平对血小板聚集和丙二醛生成的体外作用。影响ADP诱导的血小板聚集的最低浓度分别为伊拉地平1.0微克/毫升和硝苯地平12.5微克/毫升。两种药物对丙二醛生成的抑制作用浓度比影响血小板聚集的浓度低2至3倍。在体外,与钙阻滞剂一起孵育的大鼠主动脉环生成前列环素(PGI2)的量呈剂量依赖性增加。增加PGI2生成的伊拉地平最低浓度为0.5微克/毫升。硝苯地平的相应值为10微克/毫升。研究结果表明,在影响体外血小板聚集和增强PGI2生成方面,伊拉地平比硝苯地平更有效。

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