A selective estrogen receptor modulator for the treatment of hot flushes |
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| Authors: | Wallace Owen B Lauwers Kenneth S Dodge Jeffrey A May Scott A Calvin Joel R Hinklin Ronald Bryant Henry U Shetler Pamela K Adrian Mary D Geiser Andrew G Sato Masahiko Burris Thomas P |
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| Affiliation: | Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. owen.wallace@lilly.com |
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| Abstract: | ![]()
A selective estrogen receptor modulator (SERM) for the potential treatment of hot flushes is described. (R)-(+)-7,9-difluoro-5-[4-(2-piperidin-1-ylethoxy)phenyl]-5H-6-oxachrysen-2-ol, LSN2120310, potently binds ERalpha and ERbeta and is an antagonist in MCF-7 breast adenocarcinoma and Ishikawa uterine cancer cell lines. The compound is a potent estrogen antagonist in the rat uterus. In ovariectomized rats, the compound lowers cholesterol, maintains bone mineral density, and is efficacious in a morphine dependent rat model of hot flush efficacy. |
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