Thrower S, Lim L
Biochem J. 1980 Jan 15;186(1):295-300. doi: 10.1042/bj1860295.
The progestin-high-affinity-binding components in rat target tissues have been assayed by a simple and precise procedure by using spheroidal hydroxylapatite. The progestin 'receptors' in the uterus and hypothalamus of female rats are highly specific for progestins, which they bind with high affinity (Kd for [3H]progesterone in hypothalamus is 1.9 nM and in uterus is 3.7 nM). The dissociation of [3H]progesterone from receptor in vitro is rapid: t1/2 6 degrees C = 45 min in uterine cytosol; t1/2 6 degrees C = 160 min in hypothalamic cytosol. The binding is destroyed by proteinase. In the cytosol of hypothalamus and cortex of developing rats, progestin 'receptors' were present in both male and female rats by 2-3 days after birth; subsequent changes in concentration of these 'receptors' appeared to be independent of sex. Concentrations of progestin 'receptor' were close to adult values by 8-9 days, and thereafter changed relatively little.
利用球状羟基磷灰石，通过一种简单而精确的方法对大鼠靶组织中的孕激素高亲和力结合成分进行了测定。雌性大鼠子宫和下丘脑的孕激素“受体”对孕激素具有高度特异性，它们以高亲和力与之结合（下丘脑[3H]孕酮的解离常数Kd为1.9 nM，子宫为3.7 nM）。[3H]孕酮在体外与受体的解离很快：在子宫胞液中，6℃时的半衰期为45分钟；在下丘脑胞液中，6℃时的半衰期为160分钟。这种结合会被蛋白酶破坏。在新生大鼠出生后2 - 3天，雄性和雌性大鼠发育中的下丘脑和皮质胞液中均存在孕激素“受体”；这些“受体”浓度随后的变化似乎与性别无关。到8 - 9天时，孕激素“受体”浓度接近成年值，此后变化相对较小。
