The prodrug DHED selectively delivers 17β-estradiol to the brain for treating estrogen-responsive disorders.

Autor: Prokai, Laszlo, Vien Nguyen, Szarka, Szabolcs, Garg, Puja, Sabnis, Gauri, Bimonte-Nelson, Heather A., McLaughlin, Katie J., Talboom, Joshua S., Conrad, Cheryl D., Shughrue, Paul J., Gould, Todd D., Brodie, Angela, Merchenthaler, Istvan, Koulen, Peter, Prokai-Tatrai, Katalin
Předmět:
Zdroj: Science Translational Medicine; 7/22/2015, Vol. 7 Issue 297, p1-10, 10p, 1 Chart, 6 Graphs
Abstrakt: The article focuses on a study concerning the efficacy of a small-molecule bioprecursor prodrug, 10b,17b-dihydroxyestra-1,4-dien-3-one (DHED) in the treatment of estrogen-responsive disorders such as neurological and psychiatric maladies. Topics discussed include conversion of DHED to 17b-estradiol in the brain after systemic administration; formation of estrogen from the prodrug; and changes in gene expression and neuronal morphology.
Databáze: Complementary Index