P2Y1受体拮抗剂作为新型抗血栓药物。
P2Y1 receptor antagonists as novel antithrombotic agents.
作者信息
Pfefferkorn Jeffrey A, Choi Chulho, Winters Thomas, Kennedy Robert, Chi Liguo, Perrin Lisa A, Lu Gina, Ping Yun-Wen, McClanahan Tom, Schroeder Richard, Leininger Michael T, Geyer Andrew, Schefzick Sabine, Atherton James
机构信息
Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, 28/2099E, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3338-43. doi: 10.1016/j.bmcl.2008.04.028. Epub 2008 Apr 15.
The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable.
P2Y(1)和P2Y(12)嘌呤能受体负责介导二磷酸腺苷（ADP）依赖性血小板聚集。来自P2Y(1)基因敲除研究以及基于核苷酸的小分子P2Y(1)拮抗剂的证据表明，该受体的拮抗作用可能为血栓性疾病的治疗提供一种新颖且有效的方法。在此，我们报告了一系列强效且口服生物可利用的非核苷酸P2Y(1)拮抗剂的鉴定和优化。
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