Dillingham E O, Lasslo A, Gollamudi R, Bond S E, Carter-Burks G
Department of Medicinal Chemistry, University of Tennessee, Memphis 38163.
Res Commun Chem Pathol Pharmacol. 1990 Feb;67(2):179-99.
There is a striking congruence between the inhibitory effects of three synthetic entities on ADP-induced (i) human blood platelet aggregation and (ii) platelet factor 3 availability as evidenced by prolonged 'Stypven time'. The pronounced parallel between each compound's potency in inhibiting aggregation (e.g. IA 48.9 +/- 1.3, S.E., %; n = 16) and in impeding platelet factor 3 availability (e.g. IPF-3av 42.3 +/- 2.5, S.E., %; n = 12), determined concurrently in platelet-rich plasma of four different donors, further substantiates that the antiplatelet activity of our carbamoylpiperidine and nipecotoylpiperazine congeners is exerted through their interaction with anionic phospholipids.
三种合成物质对(i)ADP诱导的人血小板聚集以及(ii)血小板因子3活性(通过延长的“蛇毒时间”证明)的抑制作用之间存在显著的一致性。在来自四个不同供体的富血小板血浆中同时测定的每种化合物抑制聚集的效力(例如IA 48.9±1.3,标准误,%;n = 16)和阻碍血小板因子3活性的效力(例如IPF-3av 42.3±2.5,标准误,%;n = 12)之间的明显平行关系,进一步证实了我们的氨基甲酰哌啶和哌嗪同系物的抗血小板活性是通过它们与阴离子磷脂的相互作用发挥的。