Chackalamannil Samuel
Chemical Research, Schering-Plough Research Institute, Galloping Hill Road, Kenilworth, NJ 07033, USA.
Curr Top Med Chem. 2003;3(10):1115-23. doi: 10.2174/1568026033452122.
Inhibition of thrombin receptor (PAR-1) is a promising therapeutic approach for the treatment of various cardiovascular disorders such as unstable angina, acute myocardial infarction, stroke, and restenosis. Since a PAR-1 antagonist is specific for the cellulalr actions of thrombin, and does not interfere with fibrin generation, it is expected to have less bleeding liability than the currently available treatments. Several peptide and non-peptide PAR-1 antagonists with potent inhibition of platelet aggregation have been reported. Antithrombotic effect of a PAR-1 antibody has been demonstrated in a baboon thrombosis model and the antirestenosis property of a PAR-1 antagonist has been demonstrated in a rat model.
抑制凝血酶受体（PAR-1）是治疗各种心血管疾病（如不稳定型心绞痛、急性心肌梗死、中风和再狭窄）的一种有前景的治疗方法。由于PAR-1拮抗剂对凝血酶的细胞作用具有特异性，且不干扰纤维蛋白生成，因此预计其出血风险低于目前可用的治疗方法。已经报道了几种对血小板聚集有强力抑制作用的肽类和非肽类PAR-1拮抗剂。在狒狒血栓形成模型中已证明PAR-1抗体的抗血栓作用，在大鼠模型中已证明PAR-1拮抗剂的抗再狭窄特性。
