Hoffmann A, Markwardt F
Haemostasis. 1984;14(2):164-9. doi: 10.1159/000215052.
The influence of hirudin on the thrombin-platelet reaction was studied by determination of thrombin-induced serotonin release from blood platelets. The dissociation constant for the thrombin-hirudin complex calculated from data obtained by measuring the platelet reaction (Ki 50 pmol/1) was in accordance with the value obtained by determination of fibrinogen clotting. Prevention of the effect of thrombin on platelets required the addition of hirudin in at least 10-fold molar excess. The release of serotonin could be immediately stopped by hirudin at any time when the special conditions for the reaction of thrombin with the tight-binding inhibitor and the receptors on the platelet surface were taken into account.
通过测定凝血酶诱导的血小板5-羟色胺释放,研究了水蛭素对凝血酶-血小板反应的影响。根据测量血小板反应所得数据计算出的凝血酶-水蛭素复合物的解离常数(Ki为50 pmol/1)与通过测定纤维蛋白原凝血所得到的值一致。要防止凝血酶对血小板的作用,所需添加的水蛭素摩尔量至少要超过10倍。当考虑到凝血酶与紧密结合抑制剂及血小板表面受体反应的特殊条件时,水蛭素可在任何时候立即阻止5-羟色胺的释放。