Sugidachi A, Asai F, Koike H
Biological Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Thromb Res. 1993 Jan 1;69(1):71-80. doi: 10.1016/0049-3848(93)90004-8.
The in vivo effects of a new synthetic inhibitor of blood coagulation, aprosulate sodium, were investigated. Intravenous bolus injection of aprosulate or standard heparin in rats produced an immediate prolongation of the APTT which were characterized by a moderate dose-dependency and long-lasting duration when compared with those of standard heparin. Standard heparin inhibited plasma factor Xa activity, but aprosulate did not even at the highest dose used. Both agents inhibited thrombus formation in a dose-dependent manner in an arterio-venous shunt model. At antithrombotic doses, standard heparin prolonged the bleeding time measured by the tail transection method, but aprosulate did not. The present results suggest that aprosulate has promising in vivo profile as an anticoagulant and antithrombotic agent.
研究了一种新型合成凝血抑制剂阿普罗磺酸钠的体内效应。在大鼠中静脉推注阿普罗磺酸钠或标准肝素后，活化部分凝血活酶时间（APTT）立即延长，与标准肝素相比，其具有适度的剂量依赖性和持久的作用时间。标准肝素可抑制血浆因子Xa活性，但即使使用最高剂量的阿普罗磺酸钠也未产生此作用。在动静脉分流模型中，两种药物均以剂量依赖的方式抑制血栓形成。在抗血栓剂量下，标准肝素可延长通过尾切断法测得的出血时间，但阿普罗磺酸钠不会。目前的结果表明，阿普罗磺酸钠作为一种抗凝和抗血栓药物具有良好的体内特性。
