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2-萘-3-(3,4-二甲氧基)苯丙烯酸抗血小板聚集作用及其机理

Effect of 2-naphthyl-3-(3,4-dimethoxyl)phenylpropenoic acid on platelet aggregation and its mechanism

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【作者】 孙晓明徐黻本

【Author】 SUN Xiao-ming, XU Fu-ben Dept of Pharmacology, China Pharmaceutical University, Nanjing, 210009

【机构】 中国药科大学药理教研室中国药科大学药理教研室 南京 210009南京 210009

【摘要】 研究发现,NMPA在体外可抑制花生四烯酸、胶原及凝血酶诱导的家兔血小板聚集,IC50分别为189±9,105±11.0,49.8±16.6μM。小鼠ig NMPA(25mg/kg)后,以ADP诱导的血小板聚集明显受到抑制。大鼠ig NMPA后(52mg/kg一次或10mg/(kg·d)连续7d,出血时间延长、胶原诱导的血小板聚集率下降、丙二醛生成减少、但对动脉壁PGI2样物质影响较小。说明MNPA的作用机理可能在于改变体内TXA2/PGI2比值,而达到抑制血小板聚集的效应。

【Abstract】 Previous study showed that phenylpropenoic acid derivatives may inhibit platelet function. In this paper, the inhibitory effect of 2-naphthyl-3-(3,4) dimethoxyl)-phenylpropenoic acid (NMPA) on rabbit platelet aggregation has been revealed. The NMPA concentration of fifty percent inhibition (IC50) of platelet aggregation induced by arachidonic acid (AA), collagen or thrombin were 189 ?SD 9, 105 ?11 and .50?7 μM respectively. NMPA (25 mg/kg, ig) decreased the percentage of platelet aggregation induced by adenosine di phosphate (ADP)in mice.NMPA 25 mg/kgin a single dose or 10 mg/(kg·d) for 7 d, ig, prolonged the bleeding time, decreased the percentage of platelet aggregation induced by collQgen,and decreased the MDA forma tion, triggered by thrombin in rats. But the effect of NMPA on the formation of PGI2 like substance in rat artery, determined by bioactivity, was lesser than that of acetyl salicylic acid at same dosage.

  • 【文献出处】 中国药理学与毒理学杂志 ,Chinese Journal of Pharmacology and Toxicology , 编辑部邮箱 ,1988年03期
  • 【下载频次】22
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