Antiestrogens are partial estrogen agonists for prolactin production in primary pituitary cultures.
The antiestrogens Ly-117018 and tamoxifen increased prolactin production about 2-fold in primary cultures of male rat anterior pituitary cells. The dose-response relationship was biphasic; 10(-10) M Ly-117018 and 10(-7) M tamoxifen caused maximal stimulation, but higher concentrations caused no stimulation and completely antagonized the 5-fold stimulation caused by estrogen. The calmodulin antagonists, trifluoperazine, pimozide and W7 also prevented estrogen induction of prolactin production. Increasing concentrations of estradiol reversed inhibition by tamoxifen but not by pimozide. These results indicate that, in normal pituitary cells, estrogen antagonists may behave as partial agonists at low concentrations and as full antagonists at higher concentrations (tamoxifen, prolactin, calmodulin, 17 beta-estradiol).
D000818:Animals; D002478:Cells, Cultured; D004958:Estradiol / Q000494:pharmacology*; D004965:Estrogen Antagonists / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D010903:Pituitary Gland, Anterior / Q000187:drug effects / Q000378:metabolism*; D011388:Prolactin / Q000096:biosynthesis*; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013629:Tamoxifen / Q000494:pharmacology*; D013876:Thiophenes / Q000494:pharmacology*
D004965:Estrogen Antagonists; D011759:Pyrrolidines; D013876:Thiophenes; D013629:Tamoxifen; D004958:Estradiol; C025430:LY 117018; D011388:Prolactin