Description
Tiboloneisasyntheticsteroidhormoneselectiveestrogenreceptormodulator(SERM)thatactsasanagoNISTorantagonistdependingonthetissuelocation.Tiboloneexhibitsanti-osteoporotic,vasodilatory,andanti-metastaticactivities.Tibolonehasestrogenicandandrogenicactivityandisusedforhormonereplacementtherapy,preventingbonelossinpostmenopausalwomen;itactsasanagonistatprogesteroneandandrogenreceptors.Tiboloneanditsvariousmetabolitesactonmanyenzymes;theyinhibitSTS,17β-HSD1,andaromatase,andactivatesteroidsulfotransferaseand17β-HSD2.Tiboloneproducesvascularrelaxationincoronaryarteriesaswell.Additionally,thiscompoundinhibitsmammarycarcinomacellinvasion,likelybydecreasingactivityofMMP9.Tiboloneisanantagonistatmineralocorticoidandglucocorticoidreceptors.
References
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