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A selective estrogen receptor modulator for the treatment of hot flushes

Academic Article
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Overview

authors

  • Wallace, O. B.
  • Lauwers, K. S.
  • Dodge, J. A.
  • May, S. A.
  • Calvin, J. R.
  • Hinklin, R.
  • Bryant, H. U.
  • Shetler, P. K.
  • Adrian, M. D.
  • Geiser, A. G.
  • Sato, M.
  • Burris, Thomas

publication date

  • February 2006

journal

  • Journal of Medicinal Chemistry  Journal

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.

subject areas

  • Adenocarcinoma
  • Animals
  • Anticholesteremic Agents
  • Benzopyrans
  • Bone Density
  • Breast Neoplasms
  • Cell Line, Tumor
  • Cell Proliferation
  • Cholesterol
  • Estrogen Antagonists
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Female
  • Hot Flashes
  • Humans
  • Morphine
  • Naphthalenes
  • Ovariectomy
  • Rats
  • Rats, Sprague-Dawley
  • Selective Estrogen Receptor Modulators
  • Stereoisomerism
  • Uterine Neoplasms
  • Uterus
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm0509795

PubMed ID

  • 16451049
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Additional Document Info

start page

  • 843

end page

  • 846

volume

  • 49

issue

  • 3

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