title: Progestin binds to the glucocorticoid receptor and mediates antiglucocorticoid effect in rat adipose precursor cells.
abstract: The binding of progestin and glucocorticoid hormones was examined in the cytosol of rat adipose precursor cells. Progestin binding sites of high affinity and limited capacity were present in the cytosol of adipose precursor cells from female rats, but not from male rats, by using [3H]R5020 as radioligand. Glucocorticoid binding sites of high affinity and limited capacity were present in the cytosol of these cells from both male and female rats by using [3H]dexamethasone and [3H]triamcinolone acetonide as radioligands. The dissociation constants were in the physiological concentration range. Studies of competitive binding showed that progestin could compete with glucocorticoids at glucocorticoid binding sites. In a serum free medium glucocorticoid effect on cellular differentiation, monitored by glycerophosphate dehydrogenase (GPDH), was effectively counteracted by progesterone which by itself had no effect. These results demonstrate that progestin receptor exists only in rat adipose precursor cells from female rats, while glucocorticoid receptor exists in rat adipose precursor cells of both sexes. Glucocorticoid effects on cellular differentiation in these cells are mediated by the glucocorticoid receptor. Progestin binds to the glucocorticoid receptor and antagonizes glucocorticoid effect on cellular differentiation in these cells.
authors.affiliation: Wallenberg Laboratory, Sahlgren's Hospital, University of Göteborg, Sweden.
authors.forename: X F
authors.initials: XF
authors.lastname: Xu
authors.forename: J
authors.initials: J
authors.lastname: Hoebeke
authors.forename: P
authors.initials: P
authors.lastname: Björntorp
mesh_terms: D000273:Adipose Tissue / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D000818:Animals; D002478:Cells, Cultured; D003600:Cytosol / Q000378:metabolism; D003907:Dexamethasone / Q000378:metabolism* / Q000494:pharmacology; D004958:Estradiol / Q000494:pharmacology; D005260:Female; D007700:Kinetics; D008297:Male; D010052:Ovariectomy; D011374:Progesterone / Q000494:pharmacology*; D011397:Promegestone / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011965:Receptors, Glucocorticoid / Q000187:drug effects / Q000378:metabolism*; D013739:Testosterone / Q000494:pharmacology; D014222:Triamcinolone Acetonide / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D011965:Receptors, Glucocorticoid; D013739:Testosterone; D011374:Progesterone; D004958:Estradiol; D003907:Dexamethasone; D011397:Promegestone; D014222:Triamcinolone Acetonide