CAS: 549-02-0

Applications 10,17β-Dihydroxy-estra-1,4-dien-3-one is a prodrug that can be converted to the main human estrogen, 17β-estradiol, in the brain and not elsewhere in the body due to an enzyme expressed only in the brain. It provides positive estrogenic effects on the brain and relieve symptoms in patients with a broad range of central nervous system diseases without side effects in other tissues. References Prokai, L., et al.: Sci. Transl. Med., 7, 297 (2015)

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) has neuroprotective effects, can improve cognitive dysfunction, and can be used to study brain injury.

DHED is a neuroactive steroid precursor, specifically a bioprecursor prodrug of estradiol, which is derived from chemical synthesis pathways. It is unique in its targeted mode of action, as it selectively converts to the active hormone estradiol within the brain via enzymatic processes that occur in situ. This specificity is facilitated by 17β-hydroxysteroid dehydrogenase type 1, which catalyzes the conversion of DHED to estradiol exclusively in the brain, minimizing peripheral estrogenic effects. The principal applications of DHED are centered on addressing neurological and psychological disorders that are associated with reduced estrogen levels in the brain, including neurodegenerative diseases like Alzheimer's, depression, and cognitive decline in post-menopausal conditions. The ability of DHED to act centrally without influencing systemic estrogen levels bears potential for therapeutic strategies aimed at enhancing brain function while circumventing systemic side effects traditionally linked with estrogen therapy. This targeted delivery approach paves the way for advancements in treating neurologically relevant conditions with greater precision and reduced risk of peripheral side effects.