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Vasodilation Effects of RGD Containing Peptides and De rivatives

Vasodilation Effects of RGD Containing Peptides and De rivatives *
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摘要 The binding of Fgn to GPIIb / IIIa has confirmed that there are two distinct amino acid sequences within the Fgn molecule that are responsible for mediating its attachment to GP IIb / IIIa receptor. In addition to monoclonal antibodies, the binding function of GP IIb / IIIa can be blocked by synthetic small peptides containing the RGD and APLRV sequence. In our preliminary study it was found that besides inhibition of platelet aggregation and thrombus formation RGDS showed vasodilation effects as well. In an attempt to confirm the vasodilation effect of RGDS related peptides, RGDF, APLRV, APLRVRGDS and APLRVRGDF were investigated. The effects of these synthetic peptides on rat aortic strips pretreated with NE in vitro were observed. The relaxing extents of contracted strips for the peptides at three doses (10 5 mol / L, 10 6 mol / L and 10 7 mol / L) were recorded. 已经证实纤维蛋白分子内两个区域内的氨基酸序列可以介导纤维蛋白与GPIb/I┐Ia受体的结合。除单克隆抗体外,用合成的含RGD和APLRV的小分子多肽可以封闭GPIb/I┐Ia的这种结合功能,我们的初步研究发现,RGDS除具有抑制血小板聚集和抗血栓形成的作用外,还显示舒血管作用。为了证实RGDS相关多肽的舒血管作用,研究了RGDF,APLRV,APLRVRGDS,APLRVRGDF,在体外用NE预处理大鼠的动脉肌条后观察了上述合成多肽的舒血管作用,检测了三种剂量(10┐5mol/L,10┐6mol/L,10┐7mol/L)下收缩的肌条舒张的程度。
出处 《Journal of Chinese Pharmaceutical Sciences》 CAS 1997年第1期44-47,共4页 中国药学(英文版)
关键词 RGD Sequeence APLRV VASODILATION RGD序列 APLRV 舒血管作用
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