蛋白酶激活受體-4（PAR-4）是一個(gè)由300個(gè)氨基酸經(jīng)過7次跨膜形成的G蛋白偶聯(lián)受體，它可通過與凝血酶的結(jié)合誘導(dǎo)血小板聚集，參與凝血過程。因此，PAR-4受體可以作為抗血小板藥物的新靶點(diǎn)。近年來研究者發(fā)現(xiàn)了3種不同結(jié)構(gòu)類型的小分子PAR-4受體拮抗劑，分別含有吲唑、吲哚和咪唑并噻二唑結(jié)構(gòu)。對這幾種拮抗劑的結(jié)構(gòu)、藥理活性等方面的研究進(jìn)展進(jìn)行綜述。

Protease-activated receptor-4 (PAR-4) is a G protein-coupled receptor formed by 300 amino acids through 7 transmembrane. It can induce platelet aggregation by binding to the thrombin, and participate in the process of blood coagulation. As a result, PAR-4 can be considered as a very valuable potential treatment of antiplatelet target. In recent years, three type of small molecules PAR-4 inhibitors, including indazoles, indoles, and imidazothiadiazoles have been developed. Research progress on the structure and pharmacological activities of PAR-4 inhibitors are reviewed in this paper.