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

[Effects of 6-(alpha alpha-diphenylacetylpiperazinyl) phenyl-5-methyl-4,5-dihydro-3 (2H)-pyridazinone on rabbit platelet aggregation and TXB2, cAMP production].

作者信息

Zeng G Q, Wang X S, Sun D X, Lin A Y, Ji Y, Chu J X, Rui Y C

机构信息

Department of Pharmacology, College of Pharmacy, Second Military Medical University, Shanghai.

出版信息

Yao Xue Xue Bao. 1993;28(4):256-9.

PMID:8213167
Abstract

6-(alpha alpha-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 platelet aggregation, and its IC50s were found to be 1.12 +/- 0.1, 4.19 +/- 0.5 and 2.97 +/- 0.1 mumol/L, respectively. At the concentration range of 1-500 mumol/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 platelets.

摘要

6-(αα-二苯基乙酰哌嗪基)苯基-5-甲基-4,5-二氢-3(2H)-哒嗪酮(DMDP)是一种新型合成哒嗪酮衍生物。该化合物被证明可抑制花生四烯酸(AA)、二磷酸腺苷(ADP)和血小板活化因子(PAF)诱导的兔血小板聚集,其半数抑制浓度(IC50)分别为1.12±0.1、4.19±0.5和2.97±0.1μmol/L。在1-500μmol/L的浓度范围内,发现该化合物能以剂量依赖性方式降低洗涤过的兔血小板中血栓素B2(TXB2)的含量并提高环磷酸腺苷(cAMP)水平。这些可能是该化合物抑制兔血小板的作用机制。

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