Abstract:
:The estrogenic and antiestrogenic actions of the geometric isomers of tamoxifen and 4-hydroxytamoxifen were determined in a PRL synthesis assay using primary cultures of dispersed immature rat pituitary gland cells. 4-Hydroxytamoxifen was 100 times more potent as an antiestrogen than tamoxifen. The cis isomer of tamoxifen was a weak estrogen, but the cis isomer of 4-hydroxytamoxifen was converted to the trans isomer during the 6-day assay. This made an accurate determination of the properties of cis-(E)4-hydroxytamoxifen impossible. A series of fixed ring derivatives of the compounds were evaluated in the PRL synthesis assay in vitro to determine their estrogenic and antiestrogenic activities. The fixed ring derivatives of tamoxifen, cis-tamoxifen and trans-(Z)4-hydroxytamoxifen all had properties that were the same as those of the original triphenylethylenes. The fixed ring derivative of the cis-(E) isomer of 4-hydroxytamoxifen was a weak competitive antagonist of estrogen action with only very slight estrogenic properties. This contrasted with the other cis isomers of triphenylethylenes. We propose that the hydroxyl group on the molecule may orient the ligand at the binding site of the estrogen receptor to place the alkylaminoethoxy side-chain in a position to produce antiestrogen action.
journal_name
Endocrinologyjournal_title
Endocrinologyauthors
Jordan VC,Koch R,Langan S,McCague Rdoi
10.1210/endo-122-4-1449subject
Has Abstractpub_date
1988-04-01 00:00:00pages
1449-54issue
4eissn
0013-7227issn
1945-7170journal_volume
122pub_type
杂志文章相关文献
ENDOCRINOLOGY文献大全abstract::Transfer of corticosterone from serum to milk was studied in lactating rats after ether and pentobarbital anesthesia. Two minutes after the onset of anesthesia stress, total serum and milk corticosterone concentrations were not significantly different. By 30 min, corticosterone concentrations in serum increased to a p...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-115-4-1364
更新日期:1984-10-01 00:00:00
abstract::Previous studies from this laboratory have demonstrated the presence of two populations of rat Leydig cells (I and II), which differ in their capacity for hCG- or cAMP-stimulated testosterone production. In the present study, we examined the metabolism of 25-hydroxycholesterol in primary cultures of both populations o...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-117-3-1184
更新日期:1985-09-01 00:00:00
abstract::Recently, a subset of neurons was identified in the arcuate nucleus of the hypothalamus that colocalize three neuropeptides, kisspeptin, neurokinin B, and dynorphin, each of which has been shown to play a critical role in the central control of reproduction. Growing evidence suggests that these neurons, abbreviated as...
journal_title:Endocrinology
pub_type: 杂志文章,评审
doi:10.1210/en.2010-0022
更新日期:2010-08-01 00:00:00
abstract::Steady state levels of plasma membrane receptors (measured in radioligand assays) result from processes that contribute to the production of receptors (synthesis, recycling, and unmasking) as well as those that contribute to the loss of receptors (degradation, internalization, and inactivation). Accordingly, we have p...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-126-5-2577
更新日期:1990-05-01 00:00:00
abstract::Nuclear binding of cytoplasmic estrogen receptors was measured in an in vitro cell-free system, using various mixtures of cytosols and nuclei from uteri of mature (6-9 month old) and senescent (24-25 month old) Wistar rats. Both nuclei and cytoplasmic receptors from senescent uteri were 25-35% less efficient in suppor...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-116-2-547
更新日期:1985-02-01 00:00:00
abstract::LH receptor (LHR) expression in the ovary is regulated by the RNA binding protein, (LHR mRNA binding protein [LRBP]), which has been identified as being mevalonate kinase. This study examined the role of microRNA miR-122 in LRBP-mediated LHR mRNA expression. Real-time PCR analysis of ovaries from pregnant mare serum g...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2013-1619
更新日期:2013-12-01 00:00:00
abstract::Endometriosis-associated infertility has a multifactorial etiology. We tested the hypothesis that the endometrial response to the early embryonic signal, human chorionic gonadotropin (hCG), alters over time in a nonhuman primate model of endometriosis. Animals with experimental or spontaneous endometriosis were treate...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2010-0275
更新日期:2010-10-01 00:00:00
abstract::Progesterone (P4) inhibits apoptosis of rat granulosa cells and spontaneously immortalized granulosa cells (SIGCs), which were derived from rat granulosa cells. Defining the mechanism through which P4 mediates its action has been difficult because these cells do not express the classic nuclear P4 receptor. Previous st...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2004-0067
更新日期:2004-06-01 00:00:00
abstract::Activin A is a member of the transforming growth factor-beta family of growth factors and a potent regulator of cellular activity. A number of binding proteins for activin A have been identified, including alpha 2-macroglobulin (alpha 2M). Alpha 2M has several conformational states that are known to have different gro...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo.136.12.7588280
更新日期:1995-12-01 00:00:00
abstract::In the present study epididymal epithelium was immortalized in transgenic mice by expressing simian virus 40 T antigen under a 5.0-kb mouse glutathione peroxidase 5 promoter (GPX5-Tag1). Epididymal tumorigenesis was associated with an increase in c-Myc expression, and a marked decrease in B-Myc expression, with a 500-...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2003-0831
更新日期:2004-01-01 00:00:00
abstract::Isolated bone cells are often described according to the presence of PTH- and calcitonin (CT)-sensitive adenylate cyclase activities. Osteoblasts are thought to be cells with PTH-sensitive adenylate cyclase but without CT response, and osteoclasts are thought to be CT-sensitive cells. We have studied the adenylate cyc...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-115-6-2342
更新日期:1984-12-01 00:00:00
abstract::The expression of cholesterol side-chain cleavage cytochrome P450 (P450scc), 17 alpha-hydroxylase cytochrome P450 (P45017 alpha), and 3 beta-hydroxysteroid dehydrogenase (3 beta HSD) was studied in bovine placenta and fetal adrenal glands throughout gestation. The levels of expression of these enzymes were much lower ...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo.130.5.1374010
更新日期:1992-05-01 00:00:00
abstract::Hyperactivation of the GHRH receptor or downstream signaling components is associated with hyperplasia of the pituitary somatotrope population, in which adenomas form relatively late in life, with less than 100% penetrance. Hyperplastic and adenomatous pituitaries of metallothionein promoter-human GHRH transgenic (Tg)...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2008-1482
更新日期:2009-07-01 00:00:00
abstract::We recently found that plasma membrane phosphatidylinositol 4,5-bisphosphate (PIP(2))-regulated filamentous actin (F-actin) polymerization was diminished in hyperinsulinemic cell culture models of insulin resistance. Here we delineated whether increased glucose flux through the hexosamine biosynthesis pathway (HBP) ca...
journal_title:Endocrinology
pub_type: 杂志文章,收录出版
doi:10.1210/en.2008-1102
更新日期:2009-04-01 00:00:00
abstract::GnRH neurons form the final common pathway regulating the secretion of gonadotropins from the anterior pituitary. Since the patterns of gonadotropin release display profound sexual dimorphism among mammals including the rodent, we undertook an ultrastructural analysis to determine whether these neurosecretory cells we...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-126-2-695
更新日期:1990-02-01 00:00:00
abstract::The present study was conducted to elucidate the role of activin A in tubulogenesis of vascular endothelial cells. Activin A was produced in bovine aortic endothelial cells (BAEC). These cells also expressed the type I and type II activin receptors. When added to BAEC cultured in a collagen gel, activin A induced capi...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2004-0213
更新日期:2004-08-01 00:00:00
abstract::The steady state concentration of dopamine (DA), norepinephrine (NE), and serotonin (5HT) was determined and turnover estimated in several brain regions of young (3-4 months) and old (21 months) male Wistar rats. An estimate of DA and NE turnover was obtained by determining their depletion rates after treatment with a...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-100-6-1672
更新日期:1977-06-01 00:00:00
abstract::Intracellular cargo transport relies on microtubules and motor proteins such as kinesins and dyneins. Currently we have ample knowledge of the mechanisms by which motor proteins propel themselves along the microtubules, but little is known about intracellular factors that regulate motor speed. Here we show that proadr...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2011-1685
更新日期:2012-04-01 00:00:00
abstract::The control of ACTH secretion by opiates seems to involve stimulatory and inhibitory pathways, since opiate agonists and antagonists are capable of releasing ACTH in conscious rats. To elucidate the role of different opiate receptors in the control of ACTH release, rats were treated with receptor-selective opiate agon...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-116-6-2688
更新日期:1985-06-01 00:00:00
abstract::The effects of rat CRF, arginine vasopressin (VP), oxytocin (OXY), and isoproterenol (ISO) on the biosynthesis and release of pro-ACTH/endorphin-derived peptides by monolayer cultures of rat anterior pituitary cells in complete serum-free medium (CSFM) were studied. When cells were exposed to hormone for 3 h, CRF, VP,...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-120-3-953
更新日期:1987-03-01 00:00:00
abstract::Experiments were carried out in castrate adult male rats to further examine whether endogenous opioids are involved in CRF-induced suppression of LH secretion. Serum LH levels in rats castrated 5 days earlier were significantly reduced by intracerebroventricular administration of homologous (rat) CRF (0.02-2 nmol) wit...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-122-3-1034
更新日期:1988-03-01 00:00:00
abstract::Task3 K(+) channels are highly expressed in the adrenal cortex and contribute to the angiotensin II and K(+) sensitivity of aldosterone-producing glomerulosa cells. Adult Task3(-/-) mice display a partially autonomous aldosterone secretion, subclinical hyperaldosteronism, and salt-sensitive hypertension. Here, we inve...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2013-1101
更新日期:2013-08-01 00:00:00
abstract::The plasma osteocalcin (OC) concentration correlates with histological parameters of bone formation and has been used as an index of osteoblast activity. Although the rate of OC synthesis is likely to be a major determinant of the plasma OC level, the contribution of other processes, for example, OC plasma clearance, ...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-124-6-2785
更新日期:1989-06-01 00:00:00
abstract::The primary culture of rat luteal cells and their long-term maintenance have been difficult. Low cellular yields have limited the possibility for the study of gene regulation in luteal cells. The goal of this study was to develop a cell line to serve as a model by which to study the expression and regulation of variou...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo.139.4.5929
更新日期:1998-04-01 00:00:00
abstract::GH3 cells are a PRL-secreting adenoma cell line derived from pituitary lactotropes. These cells have been stably transfected with rat GnRH receptor complementary DNA to produce four cell lines: GGH(3)1', GGH(3)2', GGH(3)6', and GGH(3)12'. In response to either GnRH or Buserelin (a metabolically stable GnRH agonist), t...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo.137.3.8603570
更新日期:1996-03-01 00:00:00
abstract::Insulin resistance and type 2 diabetes mellitus are associated with impaired postprandial secretion of glucagon-like peptide-1 (GLP-1), a potent insulinotropic hormone. The direct effects of insulin and insulin resistance on the L cell are unknown. We therefore hypothesized that the L cell is responsive to insulin and...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/en.2008-0726
更新日期:2009-02-01 00:00:00
abstract::Aside from studies of a possible synergism between T3 and glucocorticoids in regulating GH mRNA, there have been few previous studies of the modulation by hormones and other factors of glucocorticoid hormone regulation of pituitary cell GH gene expression. We have employed a serum-free medium containing no exogenously...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-120-5-1986
更新日期:1987-05-01 00:00:00
abstract::To determine the basis for the marked daily variability in circulating luteinizing hormone (LH) in the female lamb shortly after birth and to determine whether circulating follicle-stimulating hormone (FSH) exhibits similar variability during this period of life, serum levels of both gonadotropins were monitored frequ...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-96-1-15
更新日期:1975-01-01 00:00:00
abstract::We studied the role of calcium in dopaminergic control of the neuroendocrine effects of neurotensin. In primary cultures of dispersed normal female rat anterior pituitary cells the interactions of dopamine and neurotensin were examined with reference to the rate of PRL release, the magnitude of 45Ca2+ uptake, the rate...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-127-4-1948
更新日期:1990-10-01 00:00:00
abstract::The purpose of these studies was to determine whether changes in FSH receptors correlated with FSH-induced attenuation of FSH-responsive adenylyl cyclase in immature porcine granulosa cells. Cells were incubated with FSH (1-1000 ng/ml) for up to 24 h, treated with acidified medium (pH 3.5) to remove FSH bound to cells...
journal_title:Endocrinology
pub_type: 杂志文章
doi:10.1210/endo-123-5-2374
更新日期:1988-11-01 00:00:00