Fiedler V B, Seuter F, Perzborn E
Department of Pharmacology, Bayer AG, Wuppertal, FRG.
Stroke. 1990 Dec;21(12 Suppl):IV149-51.
Bay U 3405 is a novel thromboxane receptor blocker. The present investigations describe its effects on experimental canine and porcine cardiac damage. In anesthetized dogs, a coronary artery was occluded for 6 hours and reperfused for 30 minutes. Bay U 3405 was administered intravenously 15 minutes after occlusion (1 mg/kg) followed by infusion of 10 mg/kg/hr from 30 minutes after ligature. In a second study, the effects of Bay U 3405 on endoperoxide analogue U-46619-induced coronary constriction were studied in anesthetized, open-chest pigs. Bay U 3405 reduced myocardial infarct expansion by 65% (p less than 0.01) assessed with biochemical staining. Hemodynamics and collateral blood flow were unaffected. However, reperfusion arrhythmias were suppressed. In porcine experiments, 1 mg/kg Bay U 3405, given intravenously or intraduodenally, antagonized U-46619-induced coronary vasoconstriction over 5 hours. The studies demonstrate anti-ischemic and antivasoconstrictor properties of Bay U 3405 probably due to binding to platelet and smooth muscle thromboxane receptors. This may have clinical relevance in angina pectoris and myocardial infarction.
Bay U 3405是一种新型血栓素受体阻滞剂。本研究描述了其对实验性犬和猪心脏损伤的影响。在麻醉的犬中，冠状动脉闭塞6小时后再灌注30分钟。在闭塞后15分钟静脉注射Bay U 3405（1毫克/千克），然后从结扎后30分钟开始以10毫克/千克/小时的速度输注。在第二项研究中，在麻醉的开胸猪中研究了Bay U 3405对内过氧化物类似物U - 46619诱导的冠状动脉收缩的影响。通过生化染色评估，Bay U 3405使心肌梗死扩展减少了65%（p小于0.01）。血流动力学和侧支血流未受影响。然而，再灌注心律失常受到抑制。在猪实验中，静脉注射或十二指肠内给予1毫克/千克的Bay U 3405，在5小时内拮抗了U - 46619诱导的冠状动脉血管收缩。这些研究表明Bay U 3405具有抗缺血和抗血管收缩特性，可能是由于其与血小板和平滑肌血栓素受体结合。这可能在心绞痛和心肌梗死中具有临床意义。
