血小板ADP受体及其拮抗剂的研究进展

Advances in Research of ADP Receptors and Antagonists of Platelets

ADP是人们发现最早也是体内最重要的诱导血小板聚集的物质,其在止血块和病理性动脉血栓形成中起到关键的作用。ADP对血小板的作用主要是通过与血小板膜ADP受体结合后导致血小板形态变化或使cAMP水平降低而聚集,但与凝血酶或胶原相比,其本身是一种弱的血小板激活剂,另因为ADP可以增强或放大其他激活剂的作用,而被认为是血小板激活必需的共同因子。ADP受体拮抗剂可以抑制ADP受体的表达、结合及其活性,从而有效地抑制了血小板的聚集,对血栓性疾病的治疗具有重要的作用。目前,ADP受体拮抗剂类药物因为具有较好的抗栓活性和较高的安全性,已经被较广泛的应用于临床。本文对血小板ADP受体的类型及重要的受体拮抗剂进行了综述,对该类药物的研究开发具有一定的参考价值。

ADP is found to be the potent substance inducing the platelet aggregation in the early time in vivo and it plays a key role in the formation of coagulation clot and pathological arterial thrombus. The platelet aggregation induced by ADP starts by the changing of platelet morphology or the decrease of cAMP level after ADP combines with the ADP receptor. However compared with thrombin and collagen, ADP is a weak platelet agonist alone. In addition, ADP is considered as co-factor of the platelet activation for if can enhance or magnify the effects of other agonists. ADP receptor antagonists inhibit the expression, combination and the activity of the ADP receptor and thus repress the aggregation of the platelet, which is very important to the treatment of the thrombosis. Now, because of their valid antithrombotic activity and safety, the ADP receptor antagonists are widely used as clinical drugs. In this article we summarize the types of the platelet ADP receptor and several crucial receptor antagonists and provide valuable references to the research and development of these drugs.