Doughty C, Booth J E, McDonald P G, Parrott R F
J Endocrinol. 1975 Dec;67(3):419-24. doi: 10.1677/joe.0.0670419.
Groups of neonatal female rats were treated for the first 5 days of life with oestradiol-17beta, oestradiol benzoate or a synthetic oestrogen, 11beta-methoxy-17-ethynyl-1,3,5(10)-oestratriene-3,17beta-diol (RU 2858), in daily doses ranging from 0-5 to 1000 ng. Oestradiol-17beta had no effect on adult ovarian cyclicity or sexual receptivity after ovariectomy and oestrogen+ progesterone treatment. Ovarian cyclicity was prevented by 100 ng or more oestradiol benzoate/day, and by all doses of RU 2858. Only rats receiving 50 ng oestradiol benzoate/day or 0-5 ng RU 2858/day showed normal receptivity. The defeminizing action of RU 2858 was at least 100 times greater than that of oestradiol benzoate; it is suggested that this greater potency is due to the low affinity of RU 2858 for the oestradiol-binding protein in the plasma of neonatal rats. These results indicate that defeminization of the neonatal rat brain can be induced by physiological amounts of oestrogen, and are discussed with reference to the action of testosterone.
在新生雌性大鼠出生后的头5天,用17β - 雌二醇、苯甲酸雌二醇或一种合成雌激素11β - 甲氧基 - 17 - 乙炔基 - 1,3,5(10) - 雌三烯 - 3,17β - 二醇(RU 2858)进行处理,日剂量范围为0.5至1000纳克。切除卵巢并给予雌激素加孕酮处理后,17β - 雌二醇对成年大鼠的卵巢周期性或性接受能力没有影响。每天100纳克或更多的苯甲酸雌二醇以及所有剂量的RU 2858均可阻止卵巢周期性。只有每天接受50纳克苯甲酸雌二醇或0.5纳克RU 2858的大鼠表现出正常的接受能力。RU 2858的去雌性化作用至少比苯甲酸雌二醇强100倍;有人认为这种更强的效力是由于RU 2858与新生大鼠血浆中雌二醇结合蛋白的亲和力较低。这些结果表明,生理剂量的雌激素可诱导新生大鼠脑的去雌性化,并结合睾酮的作用进行了讨论。