米非司酮与利洛司酮对兔子宫胞浆孕激素受体结合力的比较

Comparison of Rabbit Uterus Cytosol Progesterone Receptor Binding Affinities of Mifepristone and Lilopristone

本文以放射配体结合实验,分析了国产米非司酮、进口米非司酮和利洛司酮在兔子宫胞浆孕激素受体水平的竞争抑制特性。结果表明,[~3H]R5020与兔子宫胞浆孕激素受体结合之kd为0.19±0.02nmol/L,竞争抑制实验结果显示3种化合物与孕激素受体结合力皆强,其ki值分别为1.34±0.37nmol/L、1.18±0.21nmol/L和1.11±0.28nmol/L。对孕激素受体的相对结合亲和力(RBA)皆为孕酮的3倍左右。3种化合物之间各项受体药理指标均无显著性差异。

Mifepristone and Lilopristone are recently synthesized antiprogesterone compounds. In this experiment, using radioligand binding assay the receptor binding affinities of Mifepristone and Lilopristone to the rabbit uterus cytosol progesterone receptor were measured.[3H] R5020 can bind specifically to the receptor, kd=0.19± 0.02 nmol/L. Ki of Mifepristone (both our product and Roussel-Uclaf product) and Ki of Lilopristone are 1.34 ±0.37nmol/L, 1.18 ±0.2lnmol/L and 1.11 ± 0.28nmol/L respectively. Relative binding affinity (RBA)of the three compounds is about 3 times higher than that of progesterone. The results indicate that both Mifepristone and Lilopristone have high affinity to uterus progesterone receptor.