米非司酮和利洛司酮对大白鼠肝胞浆糖皮质激素受体亲和力的影响  

Analysis of Rat Liver Cytosol Glucocorticoid Receptor Binding Affinities of Mifepristone and Lilopristone

作　　者：刘永强[1] 吴熙瑞[2] 

机构地区：[1]同济医科大学生殖医学中心 [2]同济医科大学计划生育研究所

出　　处：《同济医科大学学报》1989年第6期376-379,共4页Acta Universitatis Medicinae Tongji

基　　金："七五"期间国家重点科技攻关项目

摘　　要：本文以放射配体结合实验测定了国产米非司酮、进口米非司酮和利洛司酮在大白鼠肝胞浆糖皮质激素受体水平的竞争抑制特性。[~3H]地塞米松与其受体结合之kd为0.57±0.06nmol/L,3种化合物Ki分别为0.55+0.09nmol/L、0.55±0.14nmol/L和1.02±0.07nmol/L,地塞米松、米非司酮和利洛司酮的相对结合亲和力LRBA)比值约为1:4:2。国产米非司酮和进口米非司酮的各项受体药理特性指标差异无显著性意义。In this experiment, the radioligand binding assay has been used to measure the receptor binding characteristics of three compounds to the rat liver cytosol glucocorticoid receptor, Mifepristone (our product and Roussel-Uclaf product) and Lilopristone. kd of [3H] Dexamethasone to glucocorticoid receptor is 0.57 ± 0.06 nmol/ L. Ki of these 3 compounds are 0.55 ± 0.09 nmol/L, 0.55 ±0.14 nmol/L and 1.02 ± 0.07 nmol/L respectively. The relative binding affinity (RBA) of Mifepristone is about 4 times higher than that of dexamethasone, but the RBA of Lilopristone only 2 times. No statistically significant difference is found between our product and Roussel-Uclaf product of Mifepristone in parameters. The results indicate that Lilopristone has lower affinity to glucocorticoid receptor than Mifepristone. Consequently, Lilopristone might be more suitable for termination of early pregnancy because of its weaker anti-glucocorticoid actvity.

关 键 词：米非司酮 糖皮质激素 药理学 受体 

分 类 号：R979.21[医药卫生—药品]