Barley J, Ginsburg M, Greenstein B D, MacLusky N J, Thomas P J
Brain Res. 1975 Dec 19;100(2):383-93. doi: 10.1016/0006-8993(75)90490-4.
Dihydrotestosterone (DHT) binding was measured in cytosols from brain regions and pituitary of adult female rats and, with the addition of ventral prostate, in adult male rats. Two types of binding were distinguished: one, saturable at concentration of DHT greater than or equal to 5 X 10(-9) M and an unsaturable component. In intact males saturable (limited capacity) binding was detected only in ventral prostate cytosol; 3 days after orchidectomy the saturable binding sites increase 3-fold in prostate and in pituitary, hypothalamus, amygdala and cortex to detectable levels in approximately the same abundance as in females. There were significant differences in the affinities of the limited capacity binding reactions in cytosols of different tissues though all were in the order of magnitude, 10(-9) M DHT. The affinity in pituitary cytosol was lower than in brain regions with the single exception of female amygdala in which the affinity was significantly lower than in cytosol of the same region from 3-day castrate males. The specificity of the limited capacity binding was investigated by competition between [3h]DHT and unlabelled steroids; the most effective competitors were potent androgen agonists and antagonists.
在成年雌性大鼠的脑区和垂体以及成年雄性大鼠(添加腹侧前列腺)的细胞溶胶中测量了二氢睾酮(DHT)结合情况。区分出两种结合类型:一种在DHT浓度大于或等于5×10⁻⁹ M时可饱和,另一种是不饱和成分。在完整雄性大鼠中,仅在腹侧前列腺细胞溶胶中检测到可饱和(有限容量)结合;去势后3天,前列腺以及垂体、下丘脑、杏仁核和皮质中的可饱和结合位点增加3倍,达到与雌性大致相同丰度的可检测水平。不同组织细胞溶胶中有限容量结合反应的亲和力存在显著差异,尽管所有亲和力都在10⁻⁹ M DHT的数量级。垂体细胞溶胶中的亲和力低于脑区,唯一的例外是雌性杏仁核,其亲和力显著低于去势3天雄性大鼠同一区域的细胞溶胶。通过[³H]DHT与未标记类固醇之间的竞争研究了有限容量结合的特异性;最有效的竞争者是强效雄激素激动剂和拮抗剂。