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在体外培养的脑微血管内皮细胞及大脑前动脉平滑肌细胞上研究了血小板激活因子(PAF)对~(14)C-花生四烯酸(~(14)C-AA)释放的作用,并观察了新合成药物SZ-1的作用。结果表明~(14)C-AA在此两种细胞上参入很快,4h可达平衡,PAF 0.1～20μmol/L能显著刺激AA释放。SZ-1 0.2～20μmol/L能剂量依赖性地抑制PAF诱导的AA释放,且可剂量依赖性地抑制PAF诱导的兔洗涤血小板的聚集,但对由AA,ADP诱导的PRP的聚集无抑制作用,亦不能抑制脑微血管内皮细胞产生PAF,结果提示,SZ-1具有特异性的PAF受体拮抗作用。
The effect of platelet activating factor (PAF) on the release of ~ (14) C-arachidonic acid (~ (14) C-AA) was studied in cultured brain microvascular endothelial cells and anterior cerebral artery smooth muscle cells. The role of the new synthetic drug SZ-1. The results showed that ~ (14) C-AA could quickly enter into these two kinds of cells and reached equilibrium in 4h. PAF 0.1 ~ 20μmol / L could significantly stimulate the release of AA. SZ-1 0.2 ~ 20μmol / L dose-dependently inhibited PAF-induced AA release and inhibited PAF-induced aggregation of washed platelets in rabbits in a dose-dependent manner, but did not inhibit the aggregation of PRP induced by AA and ADP , Also can not inhibit the PAF of brain microvascular endothelial cells, the results suggest that, SZ-1 has a specific PAF receptor antagonism.