| 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 |
| DOI：10.11656/j.issn.1672-1519.2017.04.19 |
| 分类号: |
| 基金项目:国家自然科学基金项目（81202798）；国家自然基金项目（81473381）. |
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| Research progress of platelet ADP receptor and its antagonist |
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ZHAI Ting1,2, HUA Sheng-yu1
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1.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;2.Research and Development Center of Traditional Chinese Medicine, Tianjin International Joint Academy of Biotechnology and Medicine, Tianjin 300457, China
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| 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. |
| Key words: platelet P2Y1 receptor P2Y12 receptor P2X1 receptors antagonists |
