Degtiar V G
Endocrinol Exp. 1983 Jun;17(2):145-53.
In cytosol fraction obtained from the pituitaries of adolescent female rats a protein was found which showed a specific binding of [3H]5 alpha-androstan-3 beta, 17 beta-diol [( 3H]3 beta-diol). With the aid of Scatchard plot two binding sites were detected showing K'D = 0.21 +/- 0.02 mmol 1(-1) and K"D = 17 +/- 2 nmol 1(-1) with a number of binding sites N' = 3.5 +/- 1 and N" = 28 +/- 4 fmol per mg of total protein, respectively. The data are presented showing the effects of various natural or synthetic estrogens and androgens on such a binding of [3H]3 beta-diol. With the aid of linear sucrose gradient a specific binding of [3H]3 beta-diol was found at 4.0-4.5 S and an unspecific binding at 8.0-8.5 S. Similarly, two fractions were detected with the aid of Sephadex G-200 gel filtration: 1. specific binding fraction approximately in a zone of bovine serum albumin; 2. unspecific binding in a zone of high molecular weight fraction. Specific binding of 3[H]3 beta-diol was decreased to about a half at 3 h after the administration of unlabelled 3 beta-diol in a dose of 100 micrograms kg-1; while it was increased after a daily administration of such a dose for 3 days. However, a dose of 1000 micrograms kg-1 suppressed the specific binding either after a single administration or after daily injections for 3 days.
在青春期雌性大鼠垂体的胞质溶胶组分中发现了一种蛋白质，它显示出对[3H]5α-雄甾烷-3β,17β-二醇[（3H]3β-二醇）的特异性结合。借助Scatchard图检测到两个结合位点，其解离常数K'D = 0.21±0.02 mmol/L和K"D = 17±2 nmol/L，结合位点数N' = 3.5±1和N" = 28±4 fmol/mg总蛋白。给出的数据显示了各种天然或合成雌激素和雄激素对[3H]3β-二醇这种结合的影响。借助线性蔗糖梯度，在4.0 - 4.5 S处发现了[3H]3β-二醇的特异性结合，在8.0 - 8.5 S处发现了非特异性结合。同样，借助Sephadex G - 200凝胶过滤检测到两个组分：1. 特异性结合组分大致在牛血清白蛋白区域；2. 非特异性结合在高分子量组分区域。在以100μg/kg的剂量给予未标记的3β-二醇后3小时，3[H]3β-二醇的特异性结合降低至约一半；而在每天给予该剂量3天后则增加。然而，1000μg/kg的剂量在单次给药后或每日注射3天后均抑制了特异性结合。
