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P6A及其类似物的抗血栓效应

王银叶, 赵明, 彭师奇*, 李长龄, 周琴璐, 李强   

  1. 1. 北京医科大学药学院, 北京 100083
    2. 北京市体育科学研究所, 北京 100050
  • 收稿日期:1996-03-12 修回日期:1996-09-03 出版日期:1996-12-15 发布日期:1996-12-15
  • 通讯作者: 彭师奇*

The Antithrombotic Effects of P6A and its Derivatives

Yin-Ye Wang, Ming Zhao, Shi-Qi Peng*, Chang-Ling Li, Qin-Lu Zhou, Qiang Li   

  1. 1.School of Pharmaceutical Sciences; Beijing Medical University; Beijing 100083
    2.Beijing Research Institute of Sports Sciences; Beijing 100050
  • Received:1996-03-12 Revised:1996-09-03 Online:1996-12-15 Published:1996-12-15
  • Contact: Shi-Qi Peng*

摘要: 在狗的冠脉血栓模型上, P6A可以增加冠脉血流量, 并改善血流动力学。纤维蛋白与GP IIb/IIIa受体结合时, RGD是关键序列。本文测了P6A, QP6ARGDS, RGDV, RGDF生成的偶联化合物的效应。研究了这些偶联化合物的抗动脉血栓作用。在5 μmol/kg剂量下, RGDSRGDV不显示抗血栓活性, 而在2.5 μmol/kg剂量下, RGDF却能够明显减小血栓干重。此外, P6A(5 μmol/kg)QP6A (2.5 μmol/kg) 显示明显的抗血栓活性。除P6A-RGDFQP6A-RGDF以外, 所有的偶联化合物都有强抗血栓作用。

关键词: P6A, RGD序列, 抗血栓

Abstract: P6A was able to increase coronary blood flow and improve hemodynamics in the coronary thrombosis model of dogs In the binding of fibrinogen to GP IIb/IIIa, RGD is the key sequence In the present paper the effects of the coupling compounds of P6A and its derivatives, QP6A with RGDS, RGDV and RGDF were tested The effects of the coupling compounds so obtained on carotid thrombosis in rats were investigated At the dose of 5 μmol/kg, RGDS and RGDV exhibited no antithrombotic effects, whereas at 2.5 μmol/kg RGDF decreased the dry-weight ofthrombus significantly On the other hand, P6A(5 μmol/kg)and QP6A(2.5 μmol/kg)showed significant antithrombosis activities.All of the coupling compounds, except P6A-RGDF and QP6A-RGDF, had potent antithrombosis effects.

Key words: P6A, RGD sequence, Anti-thrombosis

Supporting: This project was supported by National Natural Science Foundation.