Morio H, Hirai A, Terano T, Tamura Y, Yoshida S
Second Department of Internal Medicine, Chiba University Medical School, Japan.
Thromb Haemost. 1993 Mar 1;69(3):276-81.
The influence of OKY-046, a selective thromboxane synthase inhibitor, on prostanoid formation in healthy human subjects was studied. Vehicle (5% glucose solution) or OKY-046 in 5% glucose solution at 15 micrograms kg-1 min-1 was intravenously administered to five male healthy volunteers for 6 h. Platelet aggregation and thromboxane B2 (TXB2) formation induced by collagen and arachidonic acid were suppressed by the infusion of OKY-046, while both were not affected by the infusion of vehicle. Urinary excretion of 11-dehydro-thromboxane B2, one of major urinary metabolites of thromboxane A2 (TXA2) was decreased by the infusion of OKY-046, while that of 2,3-dinor-6-keto-prostaglandin F1 alpha, one of major urinary metabolites of prostacyclin (PGI2) was increased. The present study demonstrated that the infusion of OKY-046 improved the balance of TXA2/PGI2 into antithrombotic state in healthy subjects. It was also suggested that endogenously produced (probably platelet-derived) endoperoxides could be redirected into prostacyclin in vivo.
研究了选择性血栓素合酶抑制剂OKY - 046对健康人体前列腺素生成的影响。将溶媒（5%葡萄糖溶液）或5%葡萄糖溶液中浓度为15微克/千克·分钟的OKY - 046静脉注射给5名健康男性志愿者，持续6小时。输注OKY - 046可抑制胶原和花生四烯酸诱导的血小板聚集和血栓素B2（TXB2）生成，而输注溶媒对两者均无影响。输注OKY - 046可使血栓素A2（TXA2）的主要尿代谢产物之一11 - 脱氢 - 血栓素B2的尿排泄量降低，而前列环素（PGI2）的主要尿代谢产物之一2,3 - 二去甲 - 6 - 酮 - 前列腺素F1α的尿排泄量增加。本研究表明，输注OKY - 046可使健康受试者体内TXA2/PGI2的平衡向抗血栓状态改善。还提示内源性产生的（可能源自血小板的）内过氧化物在体内可被重定向生成前列环素。
