Hofmann B, Ostermann G, Hoffmann A, Klöcking H P, Kertscher H P
Institut für Pathologische Biochemie, Medizinische Akademie, Erfurt, GDR.
Biomed Biochim Acta. 1988;47(10-11):S157-60.
We investigated the inhibitory effects of two synthetic phospholipids KO-286,001 and KO-286,006 on the platelet-activating factor (PAF) induced release of plasminogen activator (PA) in the isolated pig ear preparation as well as aggregation of pig platelets. The action was compared with that of the natural PAF antagonist BN 52021. The activator release induced by 5 x 10(-9) mol/l PAF was inhibited by 10(-6) mol/l KO-286,006, whereas BN 52021 and KO-286,001 had no effect. All three PAF antagonists tested inhibited the aggregation in a dose-dependent manner. Comparison of the IC50 values confirmed the considerably lower inhibitory action of BN 52021 and KO-286,001. Our results suggested that similar receptor sites are involved in both PAF activities tested and furthermore, that are species differences in the inhibition of PAF effects.
我们研究了两种合成磷脂KO - 286,001和KO - 286,006对血小板活化因子(PAF)诱导的离体猪耳标本中纤溶酶原激活物(PA)释放以及猪血小板聚集的抑制作用。将该作用与天然PAF拮抗剂BN 52021的作用进行了比较。10(-6)mol/l的KO - 286,006可抑制5×10(-9)mol/l PAF诱导的激活物释放,而BN 52021和KO - 286,001则无此作用。所测试的所有三种PAF拮抗剂均以剂量依赖方式抑制聚集。IC50值的比较证实了BN 52021和KO - 286,001的抑制作用明显较低。我们的结果表明,所测试的两种PAF活性涉及相似的受体位点,此外,在PAF效应的抑制方面存在种属差异。