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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
引用本文:曾国钱,王雪松,孙笃新,林爱友,嵇杨,褚建雄,芮耀诚.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[J].药学学报,1993,28(4):256-259.
作者姓名:曾国钱  王雪松  孙笃新  林爱友  嵇杨  褚建雄  芮耀诚
作者单位:第二军医大学药学院药理教研室,上海200433
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。

关 键 词:6-(αα-二苯基乙酰哌嗪基苯基)-4  5-二氢-5-甲基-3(2H)-哒嗪酮  血栓素B2  环腺苷酸  血小板聚集
收稿时间:1992-08-11

EFFECTS OF 6-(αα-DIPHENYLACETYLPIPERAZINYL) PHENYL-5-METHYL-4, 5-DIHYDRO- 3 (2H) -PYRIDAZINONE ON RABBIT PLATELET AGGREGATION AND TXB2, cAMP PRODUCTION
GQ Zeng,XS Wang,DX Sun,AY Lin,Y Ji,JX Chu and YC Rui.EFFECTS OF 6-(αα-DIPHENYLACETYLPIPERAZINYL) PHENYL-5-METHYL-4, 5-DIHYDRO- 3 (2H) -PYRIDAZINONE ON RABBIT PLATELET AGGREGATION AND TXB2, cAMP PRODUCTION[J].Acta Pharmaceutica Sinica,1993,28(4):256-259.
Authors:GQ Zeng  XS Wang  DX Sun  AY Lin  Y Ji  JX Chu and YC Rui
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 IC50s 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.
Keywords:Thromboxane B2 (TXB2)  cAMP  Platelet aggregation  6-(αα-diphenylacetylpiperazinyl) phenyl- 5- methyl- 4  5- dihydro- 3 (2H)-pyridazinone
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