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很多年以来人们关注雌激素受体及作用于这些受体的化合物,并简单得把这些化合物划分雌激素受体激动剂和雌激素受体拮抗剂。然而近年来的报道以及临床资料显示了这类化合物在不同组织会显示出不同的作用,因此把此类化合物称为选择性雌激素受体调节剂(SERMs)应该更准确。对SERMs的这种认识使我们希望找到一种化合物能在骨、心脏和中枢系统保持雌激素样作用,同时对那些雌激素可能致瘤的器官如子宫内膜、乳腺产生雌激素拮抗作用。这种化合物至今还没有发现。目前SERMs主要是三苯乙烯(triphemylethylene)家族,代表物为他莫昔芬;苯并噻吩(benzothiophenes)家族,代表物为拉乐西芬,以及一些新合成的化合物。作为传统的SERMs类化合物他莫昔芬对子宫内膜的作用一直是一个有争议的问题。大量数据都表明它对子宫内膜具有活性作用。有限的关于拉乐西芬的资料表明它对子宫内膜的作用是中性的。这里我们把SERMs主要两个家族的代表物他莫昔芬和拉乐西芬对子宫内膜的影响综述如下。
For many years, people have been concerned with estrogen receptors and compounds that act on these receptors, and it is easy to classify these compounds as estrogen receptor agonists and estrogen receptor antagonists. However, recent reports and clinical data show that these compounds show different effects in different tissues, so it should be more accurate to call these compounds as selective estrogen receptor modulators (SERMs). This understanding of SERMs has led us to hopefully find a compound that will maintain estrogen-like effects in the bone, heart and central nervous system while producing estrogen antagonism in those organs where estrogen may become tumorigenic, such as endometrium and breast. This compound has not been found so far. Currently SERMs is mainly a family of triphemylethylene, represented by tamoxifen; the benzothiophenes family, represented by laurexifene, as well as some newly synthesized compounds. The role of tamoxifen as a traditional SERMs-like compound on the endometrium has been a controversial issue. A large number of data indicate that it has an active role in the endometrium. Limited information on laurexifene indicates that its effect on the endometrium is neutral. Here we summarize the effects of tamoxifen and lazepam on the endometrium, which are the representatives of two major SERMs families, as follows.