Heinroth-Hoffmann I, Hauser A, Mest H J
Martin Luther University Halle-Wittenberg, School of Medicine, Department of Pharmacology and Toxicology, GDR.
Prostaglandins Leukot Essent Fatty Acids. 1990 Nov;41(3):181-2. doi: 10.1016/0952-3278(90)90087-2.
The effects of the PAF receptor antagonists WEB 2086, WEB 2170, BN 50739 and BN 52021 on AA-induced platelet aggregation (PA) and TXA2 formation were investigated in comparison with the TXA2 synthetase inhibitor HOE 944 and the TXA2 receptor antagonist BM 13.177. All PAF antagonists tested were weak inhibitors of AA-induced PA and TXA2 formation (IC50 values between 80 and 2,737 mumol/l). HOE 944 was effective in concentrations 2-3 orders of magnitude lower than PAF antagonists in inhibiting TXA2 generation. These results imply that the inhibition of TXA2 formation is of minor relevance for the actions of the investigated PAF antagonists in AA-induced PA.
将血小板活化因子（PAF）受体拮抗剂WEB 2086、WEB 2170、BN 50739和BN 52021与血栓素A2（TXA2）合成酶抑制剂HOE 944以及TXA2受体拮抗剂BM 13.177进行比较，研究了它们对花生四烯酸（AA）诱导的血小板聚集（PA）和TXA2形成的影响。所有测试的PAF拮抗剂都是AA诱导的PA和TXA2形成的弱抑制剂（IC50值在80至2737μmol/L之间）。在抑制TXA2生成方面，HOE 944的有效浓度比PAF拮抗剂低2至3个数量级。这些结果表明，在所研究的PAF拮抗剂对AA诱导的PA的作用中，抑制TXA2形成的相关性较小。
