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Biol Pharm Bull ; 44(1): 63-68, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33390551

RESUMEN

BACKGROUND/AIM: Hormone replacement therapy during menopause increases the risk of thromboembolic diseases and cancer, so safety alternative therapeutic strategies are needed. 17ß-Aminoestrogens are a synthetic estrogens group that possess mild anticoagulant activity that contrasts with the pro-coagulant effects showed by estradiol's (E2) in rodents. Being considered an alternative to conventional hormone replacement therapy during menopause without thrombogenic risks producing. The present study aimed to determine the estrogenic profile and anxiolytic activity of 17ß-[hydroxy-ethylimine]-1,3,5(10)-estratrien-3-ol (IE2), a related compound unknown until now. METHODS: IE2 was assessed in immature rats by uterotrophic assay administering IE2, E2, or vehicle. In ovariectomized adult Wistar rats (Ovx) to facilitating the lordotic behavior compared with E2, estradiol benzoate, or vehicle. The effect of IE2 on anxiety was estimated in Ovx animals treated with IE2, E2, or vehicle group and evaluated in the elevated plus-maze model. RESULTS AND CONCLUSION: IE2 produced an uterotrophic effect, lordotic behavior, and anxiolytic effect in a dose-dependent manner, similar to E2. IE2 depicted estrogenicity, indicating potential clinical use as hormone replacement therapy during menopause.


Asunto(s)
Estradiol/análogos & derivados , Estradiol/farmacología , Estrógenos/análogos & derivados , Estrógenos/farmacología , Menopausia/efectos de los fármacos , Animales , Ansiolíticos/química , Ansiolíticos/farmacología , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Menopausia/metabolismo , Ratas , Ratas Wistar , Útero/efectos de los fármacos , Útero/metabolismo
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