Hauptmann J, Kaiser B, Nowak G, Stürzebecher J, Markwardt F
Institute of Pharmacology and Toxicology, Medical Academy Erfurt, GDR.
Thromb Haemost. 1990 Apr 12;63(2):220-3.
The anticoagulant effect of selected synthetic inhibitors of thrombin and factor Xa was studied in vitro in commonly used clotting assays. The concentrations of the compounds doubling the clotting time in the various assays were mainly dependent on their thrombin inhibitory activity. Factor Xa inhibitors were somewhat more effective in prolonging the prothrombin time compared to the activated partial thromboplastin time, whereas the opposite was true of thrombin inhibitors. In vivo, in a venous stasis thrombosis model and a thrombo-plastin-induced microthrombosis model in rats the thrombin inhibitors were effective antithrombotically whereas factor Xa inhibitors of numerically similar Ki value for the respective enzyme were not effective at equimolar dosage. The results are discussed in the light of the different prerequisites and conditions for inhibition of thrombin and factor Xa in the course of blood clotting.
在常用的凝血试验中，对选定的凝血酶和Xa因子合成抑制剂的抗凝作用进行了体外研究。在各种试验中使凝血时间加倍的化合物浓度主要取决于它们的凝血酶抑制活性。与活化部分凝血活酶时间相比，Xa因子抑制剂在延长凝血酶原时间方面更有效，而凝血酶抑制剂则相反。在体内，在大鼠的静脉淤滞血栓形成模型和凝血酶原诱导的微血栓形成模型中，凝血酶抑制剂具有有效的抗血栓形成作用，而在等摩尔剂量下，对相应酶的Ki值在数值上相似的Xa因子抑制剂则无效。根据凝血过程中抑制凝血酶和Xa因子的不同前提条件和情况对结果进行了讨论。
