Thieulant M L, Sampérez S, Jouan P
C R Acad Hebd Seances Acad Sci D. 1977 May 2;284(17):1725-7.
The presence of a specific receptor for 5alpha-androstan-3beta, 17beta-diol (3beta-diol) in the pituitary cytosol from prepubertal male rats was demonstrated. Its characteristics were: Ka = 5.2.10(7) M-1 KD = 1.9 X 10(-8) M, number of specific binding = 8.7 10(-14) moles per mg of proteins. Its sedimentation constant was 3 S. Competition assays showed that only 3beta-diol itself and estrogens were able to compete for the binding sites for 3beta-diol. Androgens, including 3alpha-diol, were inefficient. This receptor was found only in pituitary cytosol, it was missing from hypothalamic or cortical cytosols. This special localization seemed to foreshadow a specific role for 3beta-diol in the anterior hypophysis.
已证实在青春期前雄性大鼠的垂体胞质溶胶中存在5α-雄甾烷-3β,17β-二醇(3β-二醇)的特异性受体。其特征为:Ka = 5.2×10⁷ M⁻¹,KD = 1.9×10⁻⁸ M,特异性结合数 = 8.7×10⁻¹⁴摩尔/毫克蛋白质。其沉降常数为3 S。竞争分析表明,只有3β-二醇本身和雌激素能够竞争3β-二醇的结合位点。包括3α-二醇在内的雄激素则无效。该受体仅在垂体胞质溶胶中发现,下丘脑或皮质胞质溶胶中不存在。这种特殊定位似乎预示着3β-二醇在前叶垂体中具有特定作用。