Estrogenic effects of 17ß-aminoestrogens assessed in uteri of rats and mice
Por:
Lemini C., Franco Y., Avila Ma.E., Jaimez R.
Publicada:
1 ene 2005
Resumen:
Administration of exogenous estrogens has been associated with an increase of thromboembolic events. The 17?-aminoestrogens produce anticoagulant effects contrasting with the procoagulant effects of the natural occurring estradiol in rodents. This work compares the estrogenic effects induced by 17?-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 17?-aminoestrogens (0.01 to 1000 ?g/kg), or vehicle. The uterine wet and dry weights were determined. The 17?-aminoestrogens increased uterine weight in a dose-dependent manner. The uterotrophic effect produced by estradiol induced lower ED50 (6.5 and 4 ?g/kg) and higher Emax values (+523-350%) in mice as compared with those from the rat, indicating more susceptibility of the mice model. The 17?-aminoestrogens are partial estrogenic agonists with a relative uterotrophic effect of estradiol (100%) from 9-86%. Only the ED 50 values of 17?-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. © 2005 Elsevier B.V. All rights reserved.
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