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Prodrug
10β,17β-Dihydroxyestra-1,4-dien-3-one
Другие языки:

    10β,17β-Dihydroxyestra-1,4-dien-3-one

    Подписчиков: 0, рейтинг: 0
    10β,17β-Dihydroxyestra-1,4-dien-3-one
    (17β)-10,17-Dihydroxyestra-1,4-dien-3-one.svg
    Clinical data
    Other names DHED; Estradiol paraquinol; Estra-1,4-diene-10β,17β-diol-3-one
    Routes of
    administration    		 By mouth
    Drug class Estrogen
    Identifiers
    • (8S,9S,10S,13S,14S,17S)-10,17-dihydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-one
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    Chemical and physical data
    Formula C18H24O3
    Molar mass 288.387 g·mol−1
    3D model (JSmol)
    • C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=O)C=C[C@]34O
    • InChI=1S/C18H24O3/c1-17-8-7-15-13(14(17)4-5-16(17)20)3-2-11-10-12(19)6-9-18(11,15)21/h6,9-10,13-16,20-21H,2-5,7-8H2,1H3/t13-,14-,15-,16-,17-,18+/m0/s1
    • Key:UIKDFTLKOKNUJP-UGDFAFBOSA-N

    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.

    DHED has been proposed as a possible novel estrogenic treatment for neurological and psychiatric conditions associated with hypoestrogenism (e.g., menopausal hot flashes, depression, cognitive decline, Alzheimer's disease, and stroke) that uniquely lacks potentially detrimental estrogenic side effects in the periphery.



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