米非司酮与孕激素受体及糖皮质激素受体结合力的研究

Binding affinity of mifepriston to progesterone and glucocorticoid receptors

目的探讨米非司酮的抗孕激素及抗糖皮质激素作用。方法用放射配体结合实验测定米非司酮与猕猴子宫胞浆孕激素受体及大鼠肝胞浆糖皮质激素受体的结合力(BA)。结果米非司酮和孕酮与孕激素受体的BA分别为175.58%±19.20%、100%,50%抑制浓度(IC50)分别为(17.20±1.20)nm o l/L、(30.20±2.31)nm o l/L,两者相比,P均<0.01;米非司酮和地塞米松与糖皮质激素受体的BA分别为344.41%±57.41%、100%,IC50分别为(4.21±1.02)nm o l/L、(14.50±1.89)nm o l/L,两者相比,P均<0.01。结论米非司酮具有强的抗孕激素作用和一定的抗糖皮质激素作用。

Objective ：To study the binding affinity （BA） to progesterone receptors and glucocorticoid receptors of the mifepristone. Method ：With radioligand binding assay,the BA of mifepristone to the monkey uterus cytosol progesterone receptor and the rat liver glucocorticoid receptor was measured. Results： The BA of mifepristone and progesterone to progesterone receptor were 175.58 ± 19.20 % and 100 %,the 50 % inhibitory concentration （IC50） were（17.20± 1.20）nmol/L and （30.20± 2.31）nmol/L, P 〈0.01. The BA of mifepristone and dexamethasone to glucocorticoid receptor were 344. 41± 57.41% and 100%,the IC50 were （4. 21± 1.02）nmol/L and （14.50 ± 1.89） nmol/L, P 〈 0.01. Conclusion ： Mifepristone, as a strong agent of antiprogestin, can block progesterone and glucocorticoid activities.