Pharmacology of tamoxifen in laboratory animals

摘要: This paper reviews the recent laboratory findings about nonsteroidal antiestrogen, tamoxifen, and its more potent major metabolite, monohydroxytamoxifen. Both compounds stimulate progesterone receptor synthesis in rat uterus, there is an inhibition of cell division uterine luminal epithelial cells. The effects tamoxifen vivo may be a result net parent compound In rats with dimethylbenzanthracene (DMBA)-induced mammary carcinomata, young tumors that are estrogen receptor- receptor-rich respond favorably to do older receptor-poor tumors. However, antitumor effect DMBA-induced carcinoma model probably blockade tumor receptors, reduction circulating gonadotropins, lower levels, prolactin levels. 30-days treatment 30 days after DMBA resulted dose-related decrease appearance numbers tumors; however, only continuous therapy maintained animals tumor-free state. Monohydroxytamoxifen was less-potent agent, because it cleared from rapidly than tamoxifen. present support clinical use as endometrial resultant metastases adjuvant surgery for breast cancer.