用兔血小板膜受体筛选血小板激活因子（TAF）拮抗剂  

Screening of platelet activating factor antagonist with rabbit’s platelet membrane receptor

作　　者：姚远[1] 刘景玉[1] 许津[1] 

机构地区：[1]中国医学科学院医药生物技术研究所

出　　处：《中国抗生素杂志》1995年第5期321-324,共4页Chinese Journal of Antibiotics

摘　　要：在兔血小板膜中，血小板激活因子（ＰＡＦ）结合部位显示高度亲合性（Ｋｄ＝０．１±０．００７ｎｍｏｌ／Ｌ）、饱和性、显著的药理学特异性，其最大结合容量为２．８９±０．３２ｐｍｏｌ／ｍｇ蛋白。３Ｈ－ＰＡＦ饱和结合浓度为０．２ｎｍｏｌ／Ｌ。等温线表明为单一结合位点。红曲霉（Ｍｏｎａｓｃｕｓｓｐ．Ｆ４００）代谢产物中的小成份Ｄ（２Ａ）和Ｃ（４Ａ）与ＰＡＦ竞争受体结合部位，它们是ＰＡＦ的拮抗剂。Ｄ２Ａ的ＩＣ５０为３．１６×１０－５ｍｏｌ／Ｌ，Ｃ４Ａ的ＩＣ５０为３．０３×１０－５ｍｏｌ／Ｌ。In rabbit platelet membrane 3H-PAF binding sites exhibited high affinity(Kd=0.1±0. 007nmol/L),saturability and marked pharmacological specificity, Themaximal binding capacity was 2.89±0.32pmol/mg protein.aturation of3H-PAF bindingwas obtained with 0. 2nmol/L ligand and its isotherm wf1s compatible with a single class ofbinding site. Two minor components (D2A and C4A)of the metabolites from Monascus sp.F400 inhibited the binding of PAF with the receptor.IC50 of D42A and C4A,were 3.16×10-5and 3.03×10-5mol/L respectively.

关 键 词：血小板激活因子 拮抗剂 解离常数 红曲霉 

分 类 号：R973.2[医药卫生—药品]