新型吡考他胺类似物抗血栓及舒张血管研究

Research of New Picotamide Analogues Antithrombotic and Vasodilating

研究了新型吡考他胺类似物4-甲氧基-N1,N3-双(3,5,6-三甲基吡嗪-2-基)甲基间苯二甲酰胺(PKL1)对血栓形成的影响和血管的舒张作用研究。利用大鼠动静脉旁路模型观察PKL1的抑制血栓生成作用,大鼠胸主动脉血管环离体检测PKL1对NE和KCl预收缩的拮抗作用。结果表明:PKL1 50、100 mg/kg可显著抑制血栓形成,且PKL1对NE和KCl引起的大鼠胸主动脉血管环收缩有显著抑制效果。结论:PKL1具有一定的舒张血管和抑制体内血栓生成作用。

The effect of PKL1 on thrombosis formation and vasodilatation was observed.The model of vivo artery -vein bypass thrombosis in rat were established to observe the effect of PKL 1 on thrombosis formation , the model of isolated thoracic aorta rings were established to observe the vasodilatation effects of accumulated PKL 1 on isotonic tension of thoracic aortic rings pre -contracted by NE or KCl.PKL1 50 mg/kg and 100 mg/kg can significantly reduced the thrombus weight in the bypass thrombosis test.PKL1 also relaxed isolated thoracic aorta rings pre -contracted by NE and KCl.PKL1 possessed certain vasodilatation effect and exerted better effect on anti -thrombosis formation in vivo.