6-(αα-二苯基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮对兔血小板聚集及TXB<sub>2</sub>,cAMP的影响

6-(αα-二苯基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮对兔血小板聚集及TXB₂,cAMP的影响

摘要: 6-(αα-二苯基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮(简称DMDP)是我院新合成的哒嗪酮的衍生物。DMDP可以显著抑制由花生四烯酸(AA(?),ADP和血小板活化因子(PAF)诱导的免血小板聚集,其IC₅₀分别为1.12±0.1.4.19±0.5和2.97±0.1μmol/L。实验还表明DMDP在1～500 μmol/L浓度范围内呈剂量依赖性地抑制兔血小板内血栓素B₂含量,但升高兔血小板内环腺苷酸水平,这可能是其抑制血小板聚集的作用机理之一。

Abstract: 6-(αα-diphenylacetylpiperazinyl) phenyl- 5-methyl- 4,5-dihydro- 3 (2H)-pyridazinone (DMDP) is a new synthetic pyridazinone derivative. This compound was shown to inhibit AA, ADP and PAF-induced rabbit platclet aggregation, and its IC_50s were found to be 1.12±0. 1, 4. 19±0. 5 and 2. 97±0. 1 μmol/L, respectively. At the concentration range of 1～500 μmol/L, the compound was found to depress TXB₂ content and to increase cAMP levels in washed rabbit platelets in a dose--dependent manner. These might be the mechanisms of the compound on the inhibition of rabbit olatelets.