Estrogen receptor 3 selective agonist

A selective estrogen receptor-p agonist causes lesion regression in an experimentally induced model of endometriosis. Human Reproduction, 20, 936-941. 

Selective estrogen receptor modulators (SERMs) are synthetic compounds with partially agonistic and partially antagonistic estrogenic properties. In bone, SERMs inhibit bone resorption via the mechanisms known for estrogens. Major SERMs are tamoxifen, a triphenylethylene compound, and raloxifene. In postmenopausal women, the latter has been shown to prevent bone loss and to reduce fracture risk by 40%. 

Lonard DM, Smith CL (2002) Molecular perspectives on selective estrogen receptor modulators (SERMs) progress in understanding their tissue-specific agonist and antagonist actions. Steroids 67 15-24... 

Wijayaratne AL, McDonnell DP (2001) The human estrogen receptor-alpha is a ubiq-uitinated protein whose stability is affected differentially by agonists, antagonists, and selective estrogen receptor modulators. J Biol Chem 276 35684-35692... 

This is a third-generation SERM. It binds with high affinity to human estrogen receptors and acts as a tissue-selective estrogen antagonist or agonist. 

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