Abstract
A novel SERM (selective estrogen receptor modulators), 1-(R), a chromene-derived bisbenzopyran, was discovered to alleviate hot flushes and effectively increase vaginal fluidity in rats. Moreover, 1-(R) was found to have beneficial effects on plasma cholesterol and bone metabolism while maintaining antiestrogenic activity in the uterus. The biological profile of its enantiomer 1-(S) was also evaluated.
MeSH terms
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Animals
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Benzopyrans / chemical synthesis*
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Benzopyrans / chemistry
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Benzopyrans / pharmacology
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Body Fluids / drug effects*
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Bone Density / drug effects
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Cell Line
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Cholesterol / blood
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Female
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Hot Flashes / drug therapy*
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Humans
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Organ Size / drug effects
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Ovariectomy
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Rats
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Selective Estrogen Receptor Modulators / chemical synthesis*
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Selective Estrogen Receptor Modulators / chemistry
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Selective Estrogen Receptor Modulators / pharmacology
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Stereoisomerism
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Uterus / drug effects
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Vagina / drug effects*
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Vagina / metabolism
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Vaginal Diseases / drug therapy*
Substances
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Benzopyrans
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Selective Estrogen Receptor Modulators
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Cholesterol