title: Non-Feminizing Estrogens Do Not Exhibit Antidepressant-like Activity.
abstract: In this exploratory study, we performed an evaluation of non-feminizing estrogens as lead compounds for the safe treatment of menopausal symptoms. Despite confirming an enhancement of antioxidant potency as a consequence of increased lipophilicity of the prototype structures, our analyses have revealed serious shortcomings regarding pharmaceutically important properties and drug-likeness. In addition, our assessment in an animal model of estrogen deprivation has confirmed that genomic mechanisms are required for the alleviation of menopause-associated depression. Therefore, non-feminizing estrogens are not suitable to fulfill their implicated premise to address unmet needs to treat neurological and psychiatric conditions associated with estrogen deprivation of the brain.
authors.affiliation: Center for Neuroscience Discovery, Institute for Healthy Aging, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107, USA.
authors.forename: Katalin
authors.initials: K
authors.lastname: Prokai-Tatrai
authors.affiliation: Center for Neuroscience Discovery, Institute for Healthy Aging, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107, USA.
authors.forename: Vien
authors.initials: V
authors.lastname: Nguyen
authors.affiliation: Center for Neuroscience Discovery, Institute for Healthy Aging, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107, USA.
authors.forename: Laszlo
authors.initials: L
authors.lastname: Prokai
keywords: Antidepressant; Drug-likeness; Estrogens; Non-feminizing; Porsolt swim test