摘要
Y-909是已知磷酸二酯酶抑制剂CI-930的类似物。本实验发现Y-909(1O^(-)～10^(-5)M)明显抑制凝血酶诱导的血小板聚集。IC_(50)为1.1×10^(-7)M.用钙的荧光指示剂quin-z标记血小板测胞浆游离钙水平,发现该药(10^(-7)～10^(-4))也抑制凝血酶诱导的胞浆游离钙水平的增加。IC50为1.2×10^(-6)M。抑制钙释放以及钙内流的IG_(50)分别为1.1×10^(-7)和1.4×10^(-6)M。本实验提示Y-909是一种新的血小板功能抑制剂,其抑制血小板聚集的机理与降低血小板胞浆游离钙水平有关。
Y-909is an analogue of phosphodiesteraSe inhibitor CI-930.The experiment has found that Y-909 ( 10-9-10-5M ) inhibited thrombin-induced platelet aggregation. IC50 Was 1.1 × 10-7M. Measuring the platelet cytopl-asmic free calcium by fluorescent calcium indicator quin-2 has found that Y-909 ( 10-7-10-4M ) inhibited thrombin- induce elevation of cy toplasmic free calcium level.IC50 was 1, 2×10-6M. calcium re lease from intracellul-ar pools and calcium influx stimulated by thrombin Were both antagonized by Y-909.IC50 were 1.1×10-7 M and 1.4×10-6M respectively. It suggests that Y-909 may be a nove antiplatelet drug. The mechanism of inhibition of platelet function by Y-909 is closely related to inhibition of calcium release and influx.
