Jordan V C, Collins M M, Rowsby L, Prestwich G
J Endocrinol. 1977 Nov;75(2):305-16. doi: 10.1677/joe.0.0750305.
The oestrogenic and antioestrogenic properties of tamoxifen and its monohydroxylated (monohydroxytamoxifen) and dihydroxylated (dihydroxytamoxifen) metabolites have been investigated in the immature rat. Whether administered orally or subcutaneously, monohydroxytamoxifen was more active than tamoxifen as an antioestrogen. Dihydroxytamoxifen was less active than tamoxifen as an antioestrogen, but this derivative alone was unable to induce a uterotrophic response. Both metabolites of tamoxifen were potent inhibitors of the binding of [3H]oestradiol to oestrogen receptors in vitro. It is possible that the metabolites play a supportive role in the antioestrogenic activity of tamoxifen. The potent activity of monohydroxytamoxifen in vivo and in vitro suggests that this compound could be an important new tool for the subcellular investigation of oestrogenic and antioestrogenic events.
已在未成熟大鼠中研究了他莫昔芬及其单羟基化（单羟基他莫昔芬）和二羟基化（二羟基他莫昔芬）代谢产物的雌激素和抗雌激素特性。无论口服还是皮下给药，单羟基他莫昔芬作为抗雌激素的活性均高于他莫昔芬。二羟基他莫昔芬作为抗雌激素的活性低于他莫昔芬，但仅该衍生物无法诱导子宫增重反应。他莫昔芬的两种代谢产物在体外均是[3H]雌二醇与雌激素受体结合的有效抑制剂。这些代谢产物可能在他莫昔芬的抗雌激素活性中起辅助作用。单羟基他莫昔芬在体内和体外的强效活性表明，该化合物可能是用于雌激素和抗雌激素事件亚细胞研究的重要新工具。
