Nicoletti F, Speciale C, Sortino M A, Panetta M S, Di Giorgio R M, Canonico P L
Eur J Pharmacol. 1985 Sep 24;115(2-3):297-300. doi: 10.1016/0014-2999(85)90703-4.
Repeated but not single injections of estradiol benzoate significantly reduced nigral glutamic acid decarboxylase (GAD, EC 4.1.1.15). A single injection of the catecholestrogen 2-hydroxyestradiol produced similar results. Tolerance developed to the latter effect, as reflected by the lack of nigral GAD activity changes in rats repeatedly injected with 2-hydroxyestradiol. Repeated injection of the antiestrogen tamoxifen not only failed to antagonize the action of estradiol benzoate but itself reduced nigral GAD activity. Hypophysectomy, which itself decreased nigral GAD activity prevented the lowering effects of either repeated estradiol benzoate administration or single 2-hydroxyestradiol injection on the enzymatic activity.
多次注射苯甲酸雌二醇而非单次注射,可显著降低黑质谷氨酸脱羧酶(GAD,EC 4.1.1.15)的活性。单次注射儿茶酚雌激素2-羟基雌二醇也产生了类似的结果。反复注射2-羟基雌二醇的大鼠黑质GAD活性未发生变化,这表明对后一种效应产生了耐受性。反复注射抗雌激素他莫昔芬不仅未能拮抗苯甲酸雌二醇的作用,反而自身降低了黑质GAD的活性。垂体切除术本身会降低黑质GAD的活性,它可防止多次给予苯甲酸雌二醇或单次注射2-羟基雌二醇对酶活性产生的降低作用。