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  • Title: A selective estrogen receptor modulator for the treatment of hot flushes.
    Author: Wallace OB, Lauwers KS, Dodge JA, May SA, Calvin JR, Hinklin R, Bryant HU, Shetler PK, Adrian MD, Geiser AG, Sato M, Burris TP.
    Journal: J Med Chem; 2006 Feb 09; 49(3):843-6. PubMed ID: 16451049.
    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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