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消炎痛(0.003-1.0μmol/L)抑制由花生四烯酸(AA,3μmol/L)诱导的家兔洗脱血小板细胞内游离钙浓度增加及血小板聚集反应,呈剂量依赖性。血栓烷A2拮抗剂ONO-3708(0.3.0μmol/L)使AA的上述两个反应的量效曲线平行右移。另一种血栓烷A2拮抗剂S145也非竞争性的抑制AA的上述反应。延长S-145的温培时间可增加S-145的抑制作用,另外S-145的抑制作用不能被冲洗掉,而ONO-3708冲洗后其抑制作用消失。平行线测定的结果表明,以S-145处理后的洗脱血小板其AA量效曲线的斜率与S-145加ONO-3708处理组的量效曲线并不平行,这一结果提示至少S-145和ONO-3708很可能与同一受体的不同位点相结合,但分别与S-145和ONO-3708结合的两种不同TXA2/PGH2受体存在的可能性依然存在。
Indomethacin (0.003-1.0 μmol / L) inhibited the increase of intracellular free calcium concentration and platelet aggregation induced by arachidonic acid (AA, 3 μmol / L) in a dose-dependent manner. The thromboxane A2 antagonist ONO-3708 (0.3.0 μmol / L) shifted the dose-response curves of the above two reactions of AA parallel to the right. Another thromboxane A2 antagonist, S145, also non-competitively inhibited the above reaction of AA. Prolonged S-145 incubation time increased the inhibitory effect of S-145. In addition, the inhibitory effect of S-145 could not be washed away, while the inhibitory effect disappeared after ONO-3708 washing. The results of parallel lines showed that the slope of AA dose-response curve of S-145-treated elution platelets was not parallel with the dose-response curve of S-145 plus ONO-3708 treatment group. This result suggests that at least S-145 And ONO-3708 are likely to bind to different sites on the same receptor, but the possibility of two different TXA2 / PGH2 receptors bound to S-145 and ONO-3708, respectively, still exists.