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Sprague-Dawley去卵巢雌性大鼠,经雌激素刺激6天后,取垂体制成胞液。以3~H-R5020为配基,用羟基磷灰石吸附已结合配基的受体分子来测定垂体胞液中孕激素受体的结合活性;由测得的饱和曲线Scatchard作图法计算孕激素受体和配基结合的平衡解离常数(Kd)等于1.8nM,最大结合位点为138fmoles/mg蛋白。RU486可抑制3~H-R5020与垂体胞液孕激素受体的结合,抑制是竞争性的。非标记的RU486、R5020或孕酮都可竞争3~H-R5020与孕激素受体的结合,三者的竞争能力无明显差异。本实验表明在离体情况下RU486可与垂体胞液孕激素受体相结合,其亲和力与R5020或天然配基孕酮相类似。
Sprague-Dawley ovariectomized female rats, stimulated by estrogen after 6 days, the pituitary made of cytosol. Using 3 ~ H-R5020 as ligand, the binding activity of progesterone receptor in pituitary cytosol was determined by hydroxyapatite adsorption of the bound ligand receptor molecule. The saturation curve Scatchard plot was used to calculate the pregnancy The equilibrium dissociation constant (Kd) of hormone receptor and ligand binding is equal to 1.8 nM and the maximum binding site is 138 fmoles / mg protein. RU486 inhibits the binding of 3-H-R5020 to pituitary progesterone receptors, and inhibition is competitive. Unlabeled RU486, R5020 or progesterone could compete for the binding of 3-H-R5020 to progesterone receptors, with no significant difference in their ability to compete. This experiment shows that in vitro RU486 and pituitary cytokine progesterone receptor binding, its affinity and R5020 or natural ligand progesterone similar.