Estrogenic effects of 17β-aminoestrogens assessed in uteri of rats and mice

• Published in: European journal of pharmacology Vol. 510; no. 3; pp. 235 - 239
• Main Authors: Lemini, Cristina, Franco, Yanira, Avila, Ma. Estela, Jaimez, Ruth
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 14.03.2005; Elsevier
• Subjects: 17β-aminoestrogen; Amino Alcohols - administration & dosage; Amino Alcohols - pharmacology; Animals; Biological and medical sciences; Dose-Response Relationship, Drug; Estradiol; Estradiol - administration & dosage; Estradiol - pharmacology; Estradiol Congeners - administration & dosage; Estradiol Congeners - pharmacology; Estrenes - administration & dosage; Estrenes - pharmacology; Estrogenic effect; Female; Medical sciences; Mice; Organ Size - drug effects; Pharmacology. Drug treatments; Rats; Rats, Wistar; Uterotrophic effect; Uterus - anatomy & histology; Uterus - drug effects; Uterotrophic effect; 17β-aminoestrogen; Estradiol; Estrogenic effect; Rat; Rodentia; Estrogen; 17β-Estradiol; Ovarian hormone; Vertebrata; Mammalia; Mouse; Animal; 17β-am#noestrogen; Sex steroid hormone
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/j.ejphar.2005.01.028

Administration of exogenous estrogens has been associated with an increase of thromboembolic events. The 17β-aminoestrogens produce anticoagulant effects contrasting with the procoagulant effects of the natural occurring estradiol in rodents. This work compares the estrogenic effects induced by 17β-aminoestrogens prolame, butolame, pentolame, and estradiol in vivo models. Dose–response curves were performed using immature CD1 mice and Wistar rats. The animals were injected with estradiol or 17β-aminoestrogens (0.01 to 1000 μg/kg), or vehicle. The uterine wet and dry weights were determined. The 17β-aminoestrogens increased uterine weight in a dose-dependent manner. The uterotrophic effect produced by estradiol induced lower ED 50 (6.5 and 4 μg/kg) and higher E max values (+523–350%) in mice as compared with those from the rat, indicating more susceptibility of the mice model. The 17β-aminoestrogens are partial estrogenic agonists with a relative uterotrophic effect of estradiol (100%) from 9–86%. Only the ED 50 values of 17β-aminoestrogens in CD1 mice showed a direct correlation to the length of the amine group substitution in C-17 since their efficacy and potency were in the order: prolame>butolame>pentolame.