PMID- 6780318 OWN - NLM STAT- MEDLINE DCOM- 19810424 LR - 20181130 IS - 0013-7227 (Print) IS - 0013-7227 (Linking) VI - 108 IP - 1 DP - 1981 Jan TI - Antiestrogens and ovine gonadotrophs: antagonism of estrogen-induced changes in gonadotropin secretions. PG - 96-102 AB - 17 beta-Estradiol (E2) was found to affect gonadotrophs in long term ovine pituitary cell culture in several ways which were easily measured. It inhibited basal FSH secretion and, concomitantly, stimulated LH secretion. High physiological levels of E2 (10(-10) M; 27 pg/ml) were able to elicit about 70% of the maximal responses, and the effects were developed fully between 6-24 h after the addition of E2. In culture, the antiestrogens (AEs) tamoxifen, nafoxidine, and CI-680 antagonized both the inhibitory and stimulatory effects of E2 (10(-10) M) on gonadotropin secretion in a dose-dependent manner, and 10(-6) M AE was fully effective. At concentrations of 10(-6) M or lower, the AEs showed no significant intrinsic estrogenicity. At higher concentrations, the AEs progressively altered gonadotropin secretion in an apparently nonspecific fashion. Preincubations of cultures with AEs (3.3 X 10(-6) M) antagonized E2 action (10(-10) M) for approximately 18-24 h after the removal of AEs. Tamoxifen appeared to be the most potent AE tested. In conclusion, long term ovine pituitary cell cultures have provided a useful in vitro system for testing the biological potencies of AE analogs. AEs appeared to act as pure estrogen antagonists in ovine gonadotrophs. FAU - Miller, W L AU - Miller WL FAU - Huang, E S AU - Huang ES LA - eng GR - HD-10773/HD/NICHD NIH HHS/United States GR - RR-07071/RR/NCRR NIH HHS/United States PT - Journal Article PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - Endocrinology JT - Endocrinology JID - 0375040 RN - 0 (Estrogen Antagonists) RN - 0 (Gonadotropins) RN - 094ZI81Y45 (Tamoxifen) RN - 33515-09-2 (Gonadotropin-Releasing Hormone) RN - 4TI98Z838E (Estradiol) RN - 9002-67-9 (Luteinizing Hormone) RN - 9002-68-0 (Follicle Stimulating Hormone) SB - IM MH - Animals MH - Estradiol/pharmacology MH - Estrogen Antagonists/*pharmacology MH - Female MH - Follicle Stimulating Hormone/metabolism MH - Gonadotropin-Releasing Hormone/pharmacology MH - Gonadotropins/metabolism/*pharmacology MH - Luteinizing Hormone/metabolism MH - Pituitary Gland/metabolism MH - Sheep MH - Tamoxifen/pharmacology EDAT- 1981/01/01 00:00 MHDA- 1981/01/01 00:01 CRDT- 1981/01/01 00:00 PHST- 1981/01/01 00:00 [pubmed] PHST- 1981/01/01 00:01 [medline] PHST- 1981/01/01 00:00 [entrez] AID - 10.1210/endo-108-1-96 [doi] PST - ppublish SO - Endocrinology. 1981 Jan;108(1):96-102. doi: 10.1210/endo-108-1-96.