Mentz P, Pawelski K E, Giessler C
Biomed Biochim Acta. 1984;43(8-9):S163-6.
U 46619 (11,9-epoxymethano-PGH2) appears to be a selective and stable thromboxane-like agonist. In isolated preparations the substance (3.10(-9) - 3.10(-6) mol/l) induced an increase of cardiac performance of auricles and a decrease of contraction force and coronary flow of perfused hearts of guinea pigs. Intravenous infusion of U 46619 (10 micrograms/kg/min) to rabbits caused a marked reduction of heart contractility and blood pressure and the death of the animals within 10 minutes. Antianginal drugs, especially dipyridamole, propranolol, trapidil and verapamil, significantly reduced the TXA2 agonistic effects in auricles and anesthetized rabbits. The results indicate that some antianginal drugs inhibit TXA2 effects in the cardiocirculatory system. This may be regarded as an important factor for the therapeutic use of these substances.
U 46619（11,9-环氧甲撑-PGH2）似乎是一种选择性且稳定的类血栓素激动剂。在离体标本中，该物质（3.10（-9）-3.10（-6）摩尔/升）可使豚鼠心房的心脏功能增强，并使豚鼠灌流心脏的收缩力和冠状动脉血流量降低。给兔子静脉输注U 46619（10微克/千克/分钟）会导致心脏收缩力和血压显著降低，并在10分钟内导致动物死亡。抗心绞痛药物，尤其是双嘧达莫、普萘洛尔、曲匹地尔和维拉帕米，可显著降低U 46619对心房和麻醉兔子的血栓素A2激动作用。结果表明，一些抗心绞痛药物可抑制血栓素A2在心脏循环系统中的作用。这可能被视为这些物质治疗用途的一个重要因素。
