Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
Article Details
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Jain N, Kanojia RM, Xu J, Jian-Zhong G, Pacia E, Lai MT, Du F, Musto A, Allan G, Hahn D, Lundeen S, Sui Z
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
J Med Chem. 2006 Jun 1;49(11):3056-9.
- PubMed ID
- 16722623 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Ethinylestradiol Estrogen receptor alpha IC 50 (nM) 2 N/A N/A Details Raloxifene Estrogen receptor alpha IC 50 (nM) 1.8 N/A N/A Details Raloxifene Estrogen receptor beta IC 50 (nM) 8.2 N/A N/A Details