[Comparative study of the estrogenic activity of modified estrogens based on data of competitive binding analysis and biological assay].
A series of bromo- and silyl-derivatives was studied in experiments on immature female rats in vivo and in vitro. All the estrogens studied were conventionally divided into 4 groups according to their ability for concurrent binding with the rat uterus cytosol receptors and their specific bioeffect: equally concurrent and bioeffective compounds (estrone, ethynyl estradiol); slightly concurrent substances with a pronounced uterotropic action (4-silyl estrogens, mestranol); little effective compounds with 4 to 8% of estradiol concurrent activity (2- and 4-bromo-and silyl estradiols, estriol); compounds, not having concurrent and biological effects (2-silyl estrones, 4-bromoestradiol diacetate).
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001681:Biological Assay; D002478:Cells, Cultured; D003600:Cytosol / Q000378:metabolism*; D004958:Estradiol / Q000378:metabolism / Q000494:pharmacology*; D045166:Estradiol Congeners / Q000494:pharmacology; D005260:Female; D051381:Rats; D011960:Receptors, Estrogen / Q000378:metabolism*; D014599:Uterus / Q000648:ultrastructure*
D045166:Estradiol Congeners; D011960:Receptors, Estrogen; D004958:Estradiol
Sravnitel'noe izuchenie éstrogennoĭ aktivnosti modifitsirovannykh estrogenov po dannym konkurentnogo analiza i bioispytaniĭ.