摘要
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。
Adult female SD rats were ovariectomized and primed by estradiol benzoate. Pituitarycytosol progesterone receptor concentration was determined by hydroxylapatite adsorption ofthe radioactive steroid-receptor complex. Scatchard analysis of ~3H-R 5020 binding showed that the dissociation equilibriumconstant (Kd) was 1.8nM and the maximum binding sites was 138fmoles/mg protein. RU 486 inhibited the binding of ~3H-R 5020. Competition binding studies indicated thatunlabelled RU 486 as well as R 5020 or progesterone was an effective alternative for ~3H-R 5020 binding to rat pituitary progesterone receptor.
出处
《生殖与避孕》
CAS
CSCD
北大核心
1990年第1期8-12,共5页
Reproduction and Contraception
关键词
RU486
垂体胞液
孕激素受体
RU 486
Pituitary cytosol progesterone receptor
Binding activity
Competition
Affinity
