哒嗪类药物Y－909对凝血酶诱导的人血小板聚集和胞浆游离钙水平的影响

Effect of pyridazine agent Y-909 on human platelet aggregation and the change og free concentratin activated by thrombin

哒嗪类药物Ｙ－９０９对凝血酶诱导的人血小板聚集和胞浆游离钙水平的影响汪钟，于润，张宏，白建平（中国医学科学院基础医学研究所，北京１００００５）６－［对－（４－（４－甲氧基苯基）哌嗪基）－乙酰胺基苯基］－５－甲基－４，５－二氢－３（２氢）哒嗪酮｛６－［...

p-(4-(4-methoxyphenyl)pyrazinyl)-acetamidophenyl]-5-methyl-4,5-dihydro-3(2H)pyridazlnone(Y-909)0.01～10 μmol·L-1 significantly in-hibited thrombin-indueed platelet aggregation. IC50 was 0.11 μmol·L-1 .The platelet cytosolic free calcium meas-ured with fluorescent calcium indieator Quin-2/AM indi- cated that Y-909 (0.1-100 μmol ·L-1)inhibited thrombin -induced elevation of cytosolic free calcium level. IC50 was 1.2 μmol·L-1.Calcium release trom intracellular pools and caicium iuflux stimulated by thrombin were both antagonized by Y-909. IC50 were 0.11 and 1.4 μmol·L-1 respotively.It suggests that Y-909 may be a novelantiplatelet drug. The mechanism of iuhibition of platelet function by Y-909 is closely related to inhibition of calciumrelease and influx.