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本文用放射配基受体结合实验方法研究了兔血小板膜上血小板活化因子(PAF)受体的性质。[~3H]-PAF 与膜的特异结合率达70～80%,在25℃测得 PAF 与膜结合的平衡解离常数(Kd)为40.8nmol/L,最大结合位点为5.4pmol/mg 蛋白。特异的 PAF 受体拮抗剂海风藤酮对结合有较强的抑制作用,IC_(50)为30.0μmol/L。(-)-denudatin B,樟叶素(polysyphorin)和南藤素(wallichinine)是从中草药中分离的化合物,均能抑制这一结合,其IC_(50)分别为0.6 μmol/L、10 μmol/L和2.5μmol/L。
Radioligand receptor binding assay was used to study the properties of platelet activating factor (PAF) receptors on rabbit platelet membranes. The specific binding rate of [~ 3H] -PAF to the membrane was 70-80%. The equilibrium dissociation constant (Kd) of PAF bound to the membrane was 40.8 nmol / L and the maximum binding site was 5.4 pmol / mg protein. The specific PAF receptor antagonist kurdalone has a strong inhibitory effect on the binding, IC50 (50) was 30.0 micromol / L. (-) - denudatin B, polysyphorin and wallichinine are all compounds isolated from Chinese herbal medicine, and their IC 50 values are 0.6 μmol / L and 10 μmol / L and 2.5 μmol / L.