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血小板ADP受体及其拮抗剂的研究进展
引用本文:翟婷,华声瑜. 血小板ADP受体及其拮抗剂的研究进展[J]. 天津中医药, 2017, 34(4): 280-284
作者姓名:翟婷  华声瑜
作者单位:天津市现代中药重点实验室-省部共建国家重点实验室培育基地, 天津中医药大学, 天津 300193;中药新药研发中心, 天津国际生物医药联合研究院, 天津 300457,天津市现代中药重点实验室-省部共建国家重点实验室培育基地, 天津中医药大学, 天津 300193
基金项目:国家自然科学基金项目(81202798);国家自然基金项目(81473381).
摘    要:
二磷酸腺苷(ADP)是第1个已知的低分子血小板弱聚集诱导剂,ADP以较高的浓度储存在血小板致密颗粒中,当血小板受到刺激活化后,ADP从致密颗粒中释放出来,作为二次激动剂,通过作用于多种受体,可增强自身及其他诱导剂对血小板的诱导作用并有助于血栓的稳定化。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,对治疗血栓性疾病具有重要的作用。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,已经被广泛的应用于临床。通过对血小板ADP受体的类型及重要的受体拮抗剂进行了综述,对该类药物的开发具有一定的参考价值。

关 键 词:血小板  P2Y1 受体  P2Y12 受体  P2X1 受体  拮抗剂
收稿时间:2016-12-31

Research progress of platelet ADP receptor and its antagonist
ZHAI Ting and HUA Sheng-yu. Research progress of platelet ADP receptor and its antagonist[J]. Tianjin Journal of Traditional Chin Medicine, 2017, 34(4): 280-284
Authors:ZHAI Ting and HUA Sheng-yu
Affiliation:Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;Research and Development Center of Traditional Chinese Medicine, Tianjin International Joint Academy of Biotechnology and Medicine, Tianjin 300457, China and Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Abstract:
Adenosine diphosphate (ADP) is the first known low molecular weak platelet aggregation inducer. It is stored in platelet dense granules with high concentration. When the platelets were stimulated, ADP was released from the dense particles . As a secondary agonist, it can strengthen induction on itself and other revulsants. ADP contributes to stabilize thrombus by acting on a variety of receptors. Antagonists of ADP receptor can inhibit the expression and activation of ADP receptor, and can also inhibit platelet aggregation effectively. The antagonist plays an important role in treating thrombotic diseases. Currently, as ADP receptor antagonists have good antithrombotic activity and higher safety, it has been widely used in clinic. The data of different types of ADP receptor and some important receptor antagonists were reviewed in this study. We intent to provide a certain guide in the development of ADP receptor antagonists.
Keywords:platelet  P2Y1 receptor  P2Y12 receptor  P2X1 receptors  antagonists
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