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10β,17β-Dihydroxyestra-1,4-dien-3-one

From Encyclopedia & World Directory

10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED), also known as estradiol paraquinol, is an orally active, centrally selective estrogen and a biosynthetic prodrug of estradiol. Upon systemic administration, regardless of route of administration, DHED has been found to rapidly and selectively convert into estradiol in the brain, whereas no such conversion occurs in the rest of the body. Moreover, DHED itself possesses no estrogenic activity, requiring transformation into estradiol for its estrogenicity. As such, the drug shows selective estrogenic effects in the brain (e.g., alleviation of hot flashes, neuroprotection) that are said to be identical to those of estradiol, whereas estrogenic effects elsewhere in the body are not observed.

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