Biochem/physiol Actions

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.