Abstract:
:Carbon-11-labeled casimiroin analogues were first designed and synthesized as new potential PET agents for imaging of quinone reductase (QR) 2 and aromatase expression in breast cancer. [(11)C]casimiroin (6-[(11)C]methoxy-9-methyl-[1,3]dioxolo[4,5-h]quinolin-8(9H)-one, [(11)C]11) and its carbon-11-labeled analogues 5,6,8-trimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]17), 8-methoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21a), 6,8-dimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21b), and 5,8-dimethoxy-1-[(11)C]methyl-4-methylquinolin-2(1H)-one ([(11)C]21c), were prepared from their corresponding precursors with [(11)C]methyl triflate ([(11)C]CH(3)OTf) under basic conditions (NaH) through either O- or N-[(11)C]methylation and isolated by semi-preparative HPLC method in 40-50% radiochemical yields decay corrected to end of bombardment (EOB), based on [(11)C]CO(2), and 111-185GBq/mumol specific activity at the end of synthesis (EOS).
journal_name
Steroidsjournal_title
Steroidsauthors
Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QHdoi
10.1016/j.steroids.2010.06.004subject
Has Abstractpub_date
2010-12-01 00:00:00pages
967-73issue
12eissn
0039-128Xissn
1878-5867pii
S0039-128X(10)00167-4journal_volume
75pub_type
杂志文章相关文献
STEROIDS文献大全abstract::A radioimmunological method was developed for determining total and free corticosterone in rat plasma. This method was used to determine the dose-response curve of corticosterone and to measure the elimination and study the half-lives of total and free corticosterone in rat plasma with a dose of 5 mg/kg. The eliminati...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(88)90056-6
更新日期:1988-05-01 00:00:00
abstract::Recent reports demonstrate neurotrophic properties of dehydroepiandrosterone sulfate (DHEAS) in men at rest, as well as profound neurotrophic responses to stress in both men and women. Little is known of neuroprotective-neurotrophic effects of DHEAS during stress exposure, either in men or women. This translational st...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2014.05.011
更新日期:2014-09-01 00:00:00
abstract::The properties of 5-ene-3 beta hydroxysteroid oxidoreductase (3 beta-HSD) from human placental homogenates were studied in vitro. The apparent Michaelis constants for 3 beta-HSD with the substrates pregnenolone (delta 5P) and dehydroepiandrosterone (DHA) were 170 nM and nM respectively. The optimal pH for both these s...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(79)80002-1
更新日期:1979-01-01 00:00:00
abstract::Oxidative stress is thought to play a crucial role in the pathogenesis of chronic diabetic complications. We investigated the protective effects of 17 beta-estradiol (E2) on alloxan-induced stress oxidant, hepatic dysfunction and histological changes in male rats liver and pancreas. Our results showed that 17 beta-est...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2007.12.026
更新日期:2008-05-01 00:00:00
abstract::In demyelinating or non-demyelinating neurodegenerative diseases, increased levels of 7-ketocholesterol (7KC), 7β-hydroxycholesterol (7β-OHC) and 24(S)-hydroxycholesterol (24S-OHC) can be observed in brain lesions. In 158N murine oligodendrocytes, 7KC triggers a complex mode of cell death defined as oxiapoptophagy, in...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2015.02.003
更新日期:2015-07-01 00:00:00
abstract::Androgen-binding protein/sex hormone-binding globulin (ABP/SHBG) is an extracellular carrier protein that binds androgens and estrogens with high affinity. In the adult, ABP/SHBG is thought to function in the male reproductive system and the general circulation in both sexes to modulate the actions of sex steroids. Th...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(96)00049-9
更新日期:1996-07-01 00:00:00
abstract::Initial excretion studies with orally administered [monoethyl-1-3H] DES demonstrated the feces to be the principal mode of elimination of DES in the C3H mouse. Metabolic studies with tritiated DES and/or [UL-14C] DES were performed with orally dosed C3H high (MTV+) and low (MTV-) titer MMTV female mice. Extraction and...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(78)90029-6
更新日期:1978-04-01 00:00:00
abstract::To investigate the effects of conjugated bile acid on bacterial growth and cholylglycine hydrolase activity, Clostridium perfringens from human feces was exposed to varying concentrations of taurine- or glycine-conjugated chenodeoxycholic acid. Extracellular enzyme activity was determined by deconjugation of radiolabe...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(94)90062-0
更新日期:1994-08-01 00:00:00
abstract::Estrogen results in the suppression of experimental allergic encephalomyelitis (EAE), a frequently used experimental animal model of multiple sclerosis (MS). The mechanism by which estrogen acts in diseases with an autoimmune background is less clear. Here, we used splenic dendritic cells (DC) from the Lewis rats EAE ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2004.05.019
更新日期:2004-09-01 00:00:00
abstract::Fingernail clipping is expected to be a specimen for steroid testing, because it has several advantages over blood; i.e., noninvasive collection, ease of storage, portability and handling, and possibility for an assessment of the steroid status over a relatively long and retrospective time window. In this study, we ex...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.02.013
更新日期:2016-05-01 00:00:00
abstract::The importance of computer-aided drug design and development is clear nowadays. These approaches smooth the way of designing some efficient candidates based on drugs in use. At this place, we studied the mechanism of D4-abiraterone (D4A), the active metabolite of Abiraterone (Abi), binding to CYP17A1 compared with Abi...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2021.108799
更新日期:2021-01-17 00:00:00
abstract::Progesterone and its polar metabolite(s) trigger the meiotic divisions in the amphibian oocyte through a non-genomic signaling system at the plasma membrane. Published site-directed mutagenesis studies of ouabain binding and progesterone-ouabain competition studies indicate that progesterone binds to a 23 amino acid e...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2012.04.012
更新日期:2012-09-01 00:00:00
abstract::The steroid receptor-positive human ovarian cancer (BG-1) was evaluated to determine its usefulness as a tumor model. This tumor grows in intact male and female nude mice without hormone supplements. Moreover, its growth was significantly accelerated in ovariectomized mice, and the increased growth rate could be rever...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(89)90083-4
更新日期:1989-12-01 00:00:00
abstract::Inhibition of 5alpha-reduction of testosterone by an anti-androgen TSAA-291 (16beta-ethyl-17beta-hydroxy-4-estren-3-one) was studied in rat ventral prostates and the metabolic conversion of 3H-TSAA-291 was examined both in vitro and in vivo. In the in vitro experiment using nuclear 5alpha-reductase of the prostate, 5a...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(81)90021-0
更新日期:1981-07-01 00:00:00
abstract::To identify new pathways of estrogen action and novel estrogen receptor α (ERα) biomodulators, we performed high throughput screening and used follow on assays and bioinformatics to identify small molecule ERα inhibitors with a novel mode of action. These studies led to identification of rapid extranuclear activation ...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2016.03.014
更新日期:2016-10-01 00:00:00
abstract::Sleep apnea is a disorder, which increasingly affects people worldwide. Whether the associated hypoxic events during sleep are central or obstructive in origin, the end result is excessive daytime sleepiness and an increased risk for several comorbidities, such as cardiovascular and neurodegenerative disorders. Sleep ...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2017.12.006
更新日期:2018-05-01 00:00:00
abstract::Chick kidney and brain were analyzed for the subcellular distribution (if any) of a putative plasma membrane receptor for 1,25-dihydroxyvitamin D3 [1,25(OH)2D3]. Fractionation protocols were found to be based not only on differential centrifugation conditions, but also gentleness of resuspension procedures, and suffic...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(99)00030-6
更新日期:1999-08-01 00:00:00
abstract::Guinea pig adrenal estrogen sulfotransferase from either sex was eluted as a single peak, irrespective of buffer salt concentration, when subjected to fast protein liquid chromatography on gel filtration columns. The same enzyme was consistently eluted in two distinct peaks during chromatofocusing. Adrenal pregnenolon...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(92)90063-f
更新日期:1992-06-01 00:00:00
abstract::Labeled beta-muricholic acid was obtained from germfree rats given [24-14C]-chenodeoxycholic acid. It was crystallized with the same unlabeled bile acid extracted from germfree rat pooled biles. Five patients fitted with a T-tube after cholecystectomy were given orally 100 mg of the bile acid. Metabolites of beta-muri...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(85)90006-6
更新日期:1985-05-01 00:00:00
abstract::(25S)-3-Oxocholesta-1,4-dien-26-oic acid (1) and a new (25S)-18-acetoxy-3-oxocholesta-1,4-dien-26-oic acid (2) were isolated from a soft coral Minabea sp. (cf. aldersladei) collected in North Sulawesi, Indonesia, together with two known cholic-acid-type compounds, 3-oxochol-1,4-dien-24-oic acid (3) and 3-oxochol-4-en-...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2009.04.002
更新日期:2009-09-01 00:00:00
abstract::In this paper, we studied the effect of heme availability on corticosterone and aldosterone synthesis in rat adrenal. We found that hemin stimulated corticosterone and aldosterone production in adrenal homogenates in a dose-dependent fashion. Hemin administration to rats also provoked an increase in both corticosteron...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(97)00074-3
更新日期:1997-12-01 00:00:00
abstract::From the fruiting bodies of Ascomycetes Tuber indicum, a new steroidal glucoside with polyhydroxy ergosterol nucleus, tuberoside (2), has been isolated along with additional four known ergosterol derivatives, (22E, 24R)-ergosta-7, 22-dien-3beta, 5alpha, 6beta-triol (1), 5alpha, 8alpha-epidioxy-(22E, 24R)-ergosta-6, 22...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(01)00105-2
更新日期:2001-10-01 00:00:00
abstract::Novel C6-cyclo secondary amine substituted purine steroid-nucleoside analogues (2-9) were efficiently synthesized through displacement of the C6 chloro on the purine ring of series 1 with versatile cyclic secondary amines, including pyrrolidines, piperidine, morpholine, and piperazines. All the newly-synthesized compo...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2014.03.017
更新日期:2014-07-01 00:00:00
abstract:BACKGROUND:Serum progesterone (P) rises after ovulation in the luteinisation process. OBJECTIVE:To identify an accurate progesterone threshold to confirm ovulation in the assessment of a woman's fertility. METHODS:In a secondary analysis of an observational European multicentre study, this study included 107 women ov...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2015.06.013
更新日期:2015-09-01 00:00:00
abstract::In this paper we report the synthesis of four fluorinated analogues of brassinosteroids in which fluorine was introduced stereoselectively at C-2. The bioactivity of these new compounds was evaluated using the rice lamina inclination test. The results show that two of these analogues elicit high bioactivity, suggestin...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2008.12.006
更新日期:2009-04-01 00:00:00
abstract::The nature of the water-soluble products formed by incubating labelled estradiol with uterine peroxidase in the presence of H2O2 and tyrosine was examined by two-dimensional thin-layer chromatography and high voltage electrophoresis. It was shown that the steroid and amino acid were associated in a 1:2 or 1:3 ratio an...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(77)90072-1
更新日期:1977-04-01 00:00:00
abstract::During our studies of the hepatic androgen receptor in cynomolgus monkeys, tritiated mibolerone +/- a 200-fold excess of unlabeled mibolerone has been used to determine specific binding in cytosol. During time-course studies, high-capacity, unsaturable binding of [3H]mibolerone was noted after short-term incubations (...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(95)00116-8
更新日期:1995-11-01 00:00:00
abstract::Some intermediates in the cholesterol biosynthesis between lanosterol and cholesterol are capable of inducing resumption of meiosis in cultured mouse oocytes without the presence of gonadotropins. The mechanism by which these so-called Meiosis Activating Sterols (MAS) activate the meiotic process is unknown, and it is...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(02)00041-7
更新日期:2002-11-01 00:00:00
abstract::Biotransformation of an orally active contraceptive drug, drospirenone (1), by Cunninghamella elegans ATCC 36114 yielded four new metabolites, 6β,7β,15β,16β-dimethylene-3-oxo-14α-hydroxy-17α-pregn-4-ene-21,17-carbolactone (2), 6β,7β,15β,16β-dimethylene-3,11-dioxo-17α-pregn-4-ene-21,17-carbolactone (3), 6β,7β,15β,16β-d...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2017.07.010
更新日期:2017-10-01 00:00:00
abstract::The peripheral conversion of testosterone (T) into androstenedione (delta 4) and dihydrotestosterone (DHT) were studied in pregnant (days 32, 48 and 67 post coitum) and non-pregnant anesthetized guinea-pigs by constant intravenous infusion of tritium labeled T. Endogenous levels were measured by radioimmunoassay, and ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(83)90157-5
更新日期:1983-08-01 00:00:00