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喜巴辛衍生物SCH-530348是蛋白酶激活受体1(PAR-1)的抑制剂,PAR-1是人血小板凝血酶最主要的一种受体。SCH-530348是第一种能抑制凝血酶诱导的血小板聚集而不影响凝血酶对胶原酶原活化能力的化合物。文中综述了SCH-530348的临床前和Ⅰ～Ⅲ期临床试验结果。这些研究表明SCH-530348具有降低缺血性事件发生风险的几率,同时不会明显增加机体出血的风险,临床上可应用于急性冠脉综合征的治疗和缺血性心血管事件的预防。
Hibasin derivative SCH-530348 is an inhibitor of protease-activated receptor 1 (PAR-1), the most important receptor for human platelet thrombin. SCH-530348 is the first compound that inhibits thrombin-induced platelet aggregation without affecting the ability of thrombin to activate collagenase. The results of preclinical and stage Ⅰ ~ Ⅲ clinical trials of SCH-530348 were reviewed. These studies show that SCH-530348 has a reduced risk of ischemic events without significantly increasing the risk of bleeding in the body and is clinically applicable to the treatment of acute coronary syndromes and the prevention of ischemic cardiovascular events.