从广义来说抗雌激素药为一组具有对抗雌激素活力的物质,其中有些物质并不直接对抗,而是改变雌激素的作用,例如雄激素和孕激素。有些物质则对靶细胞浆的雌激素受体有亲和力,因而对雌激素起竞争抑制作用,例如氯菧酚,Nafoxidin,Cyclofenil,Tamoxifen等。雌三醇和雌激素受体也有亲和力,对雌二醇也起竞争抑制作用。但雌三醇本身为一弱雌激素,具有雌激素的功能,故不列入抗雌激素类。本文仅对Tamoxifen临床应用的进展作些介绍。 Tamoxifen的药理 Tamoxifen为双苯乙烯(diphenylethylene)衍生物,和氯菧酚的化学结构类似(见图)。但Tamoxifen的逆式异构体 Anti-estrogen drugs in a broad sense are a group of substances that have antiestrogen activity, some of which do not directly antagonize but alter the effects of estrogens such as androgens and progestins. Some substances have an affinity for the estrogen receptor of the target cytoplasm, and thus play a competitive inhibitory effect on estrogen such as chlorophenol, Nafoxidin, Cyclofenil, Tamoxifen and the like. Estriol and estrogen receptors also have affinity for estradiol also play a competitive inhibitory effect. However, estriol itself is a weak estrogen, with estrogen function, it is not included in anti-estrogens. This article only describes the progress of Tamoxifen clinical application. Tamoxifen’s pharmacology Tamoxifen is a diphenylethylene derivative, similar in chemical structure to chlorophenol (see photo). But Tamoxifen’s trans isomer