Moguilewsky M, Raynaud J P
Steroids. 1977 Jul;30(1):99-109. doi: 10.1016/0039-128x(77)90140-4.
Specific, estrogen-inducible, nuclear radioactivity uptake has been demonstrated in the uterus, pituitary and hypothalamus of immature female rats after injection of a highly potent labelled progestin, R 5020 (17, 21-dimethyl-19-nor-pregna-4, 9-diene-3, 20-dione). A cytoplasmic progestin "receptor" has been characterized in these target tissues by an in vitro Dextran-coated charcoal adsorption method. R 5020 binds with the same intrinsic dissociation constant to the receptor present in these tissues; it dissociates at the same rate from the uterine and pituitary receptor (k-1 = 1 multiplied by 10(-2) min (-1), but about 6 times slower than progesterone. This evidence, together with the similar hormone specificity in the uterus and pituitary, suggests that the progestin "receptor" is a similar entity in central and peripheral target tissues.
在未成熟雌性大鼠注射高效标记孕激素R 5020（17, 21 - 二甲基 - 19 - 去甲孕甾 - 4, 9 - 二烯 - 3, 20 - 二酮）后，已证实在其子宫、垂体和下丘脑中存在特异性的、雌激素诱导的核放射性摄取。通过体外葡聚糖包被活性炭吸附法，已在这些靶组织中对一种细胞质孕激素“受体”进行了表征。R 5020以相同的固有解离常数与这些组织中存在的受体结合；它从子宫和垂体受体上以相同速率解离（k - 1 = 1×10⁻² min⁻¹），但比孕酮慢约6倍。这一证据，连同子宫和垂体中相似的激素特异性，表明孕激素“受体”在中枢和外周靶组织中是相似的实体。
