Janssens J P, Billiet G, Bonte J, De Loecker W
Anticancer Res. 1984 May-Jun;4(3):157-62.
The effects of daily Tamoxifen treatment on adult rat uterus weight depend on the degree of estrogenic impregnation of the animal. In intact animals, Tamoxifen caused a decrease of the uterine weight. A weight increase was observed, after castration, which was dose-dependent without reaching saturation even with 500 micrograms of Tamoxifen per day. This uterine weight increase, reaching its peak during the first 24 h after the initial Tamoxifen application, is attributable to water retention. The uterine progesterone receptor (PgR) concentrations are stimulated by daily antiestrogen treatment of intact and castrated animals. This increase in the PgR levels is initially dose-dependent up to 10 micrograms of Tamoxifen per day reaching maximal levels after 4 days of treatment. The results indicate that growth and PgR induction in adult rat uterus are essentially controlled by independent mechanisms, constituting the biological basis of the synergistic effects of anti-estrogens and progestagens.
每日给予他莫昔芬对成年大鼠子宫重量的影响取决于动物的雌激素浸润程度。在未阉割的动物中,他莫昔芬导致子宫重量减轻。阉割后观察到子宫重量增加,且呈剂量依赖性,即使每天给予500微克他莫昔芬也未达到饱和。这种子宫重量增加在首次给予他莫昔芬后的最初24小时内达到峰值,是由于水分潴留所致。未阉割和阉割动物每日接受抗雌激素治疗均可刺激子宫孕酮受体(PgR)浓度升高。PgR水平的这种升高最初呈剂量依赖性,每天给予他莫昔芬达10微克时,在治疗4天后达到最高水平。结果表明,成年大鼠子宫的生长和PgR诱导基本上由独立机制控制,这构成了抗雌激素和孕激素协同作用的生物学基础。