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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 paper, radioligand binding assay was used to determine the competitive inhibition of domestic mifepristone, imported mifepristone and lilopristone on the level of glucocorticoid receptor in the liver of rats. The kd of [~ 3H] dexamethasone and its receptor was 0.57 ± 0.06 nmol / L, and the three compounds Ki were 0.55 ± 0.09 nmol / L, 0.55 ± 0.14 nmol / L and 1.02 ± 0.07 nmol / L, The relative binding affinity (LRBA) ratio of mitoxantrone, mifepristone and lilopristone is about 1: 4: 2. Domestic mifepristone and imported mifepristone receptor pharmacological characteristics of the difference was not statistically significant.