α-DHED is a bioprecursor prodrug of 17α-estradiol ((Alfatradiol)) that results in 17α-estradiol being produced selectively in the brain with little production in the periphery. α-DHED has no estrogenic activity itself with little affinity for either ERα and ERβ estrogen receptors. 17α-estradiol (αE2) has been proposed to have potential roles in various neurodegenerative disorders including neuroprotection of the brain and the prevention/treatment of Alzheimer′s disease, but peripheral side-effects on estrogen-sensitive organs have been problematic. α-DHED, a prodrug without estrogenic activity, could help alleviate those concerns.
Bioprecursor prodrug of 17α-estradiol that results in 17α-estradiol being produced selectively in the brain
ACS chemical neuroscience, 9(11), 2528-2533 (2018-05-31)
Uterotrophic effect of 17α-estradiol, the C17 epimer of the main human estrogen 17β-estradiol, was shown to manifest in animal models at doses lower than those necessary for central outcome raising concerns about its potential to treat maladies of the central
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