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Nα-乙酰 -精氨酰 -甘氨酰 -天冬氨酰 -对甲氧基苯乙胺 (W2 0 0 2 )是精 -甘 -天冬氨酸 (Arg- Gly- Asp)肽类血小板聚集抑制剂 .为探讨其抗血小板聚集的活性 ,分别用比浊法和血小板计数的方法测定二磷酸腺苷 (ADP)及高剪切速率诱导的血小板聚集 ,并用放射性配体分析法测定血小板表面结合 [12 5I]纤维蛋白原 (FGN)的含量 ,以了解 W2 0 0 2竞争性抑制 [12 5I]FGN与血小板糖蛋白 (GP) b/ a结合的生物活性 .结果显示 :W2 0 0 2有明显的抑制 ADP诱导血小板聚集的活性 ,除最低终浓度(9 μmol· L-1)外 ,其余各浓度点 (2 70 ,1 35,45μmol· L-1)与生理盐水对照组比较差异均非常显著 ;其对抗高剪切速率诱导的血小板聚集也有明确的量 -效关系 ;抑制 [12 5I]FGN与血小板结合的 IC50值为 (41 .5± 2 .9)μmol· L-1,在老年人和青年人群中比较无明显差异 .研究提示 W2 0 0 2通过抑制FGN与血小板 GP b/ a的结合而发挥作用 .
Nα-Acetyl-Arginyl-Glycyl-Aspartyl-p-Methoxyphenethylamine (W2 0 0 2) is a platelet aggregation of peptides of the Arg-Gly-Asp Peptide Inhibitor.In order to investigate its anti-platelet aggregation activity, platelet aggregation induced by adenosine diphosphate (ADP) and high shear rate was determined by turbidimetric method and platelet count respectively, and platelet surface binding was determined by radioligand analysis [12 5I] fibrinogen (FGN) levels in order to understand the biological activity of W2 0 0 2 competitively inhibiting the binding of [125 I] FGN to platelet glycoprotein (GP) b / a The results showed that Significant inhibition of ADP-induced platelet aggregation activity, except the lowest concentration (9 μmol · L-1), the other concentration points (2 70,1 35,45 μmol · L-1) compared with the saline control group were significantly different The platelet aggregation induced by high shear rate also had a clear dose-effect relationship. The IC50 value of inhibition of [125I] FGN and platelet aggregation was (41.5 ± 2.9) μmol · L-1, There was no significant difference between people and young people.The research suggests that W2 0 0 2 can inhibit the combination of FGN and platelet GP b / a Effect.