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Pesquisa : D04.210.500.365.415.050 [Categoria DeCS]
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  1 / 110 MEDLINE  
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PMID:21590729
Autor:Aspers RL; Geutjes PE; Honing M; Jaeger M
Endereço:MSD, Merck Research Laboratories, Medicinal Chemistry Oss, Molenstraat 110, 5342 CC Oss, The Netherlands.
Título:Using indirect covariance processing for structure elucidation of small molecules in cases of spectral crowding.
Fonte:Magn Reson Chem; 49(7):425-36, 2011 Jul.
ISSN:1097-458X
País de publicação:England
Idioma:eng
Resumo:Indirect and unsymmetrical indirect covariance NMR provide powerful tools to compute and visualize correlation information by transforming component spectra into combined spectral data matrices. Sensitive component spectra such as TOCSY, HSQC and NOESY can be quickly converted into experimentally insensitive or time-consuming correlation spectra such as HSQC-NOESY. The comparison of illustrative series of spectra from four steroids, dexamethasone, testosterone, allylestrenol and tibolone, renders the effects of resonance overlap on the ease of interpretation visible. The compounds are selected such that signal overlap increases systematically in the proton and carbon domain. Spectra are defined as light, moderate and heavy signal overlap, based on signal density. The investigation suggests that moderate spectral congestion in either proton or carbon domain leads to a number of artifacts that does not hamper signal assignment but lowers the level of confidence on de novo structure elucidation. Since the number of correlations usually increases through covariance processing, component spectra with severe spectral congestion in both dimensions are not suitable for covariance processing and the resulting spectra do not support structure confirmation or structure elucidation. The calculated spectra are compared with the corresponding experimental spectra with respect to their application in structure elucidation laboratory environments.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Norpregnenes); 0 (Steroids); 3XMK78S47O (Testosterone); 7S5I7G3JQL (Dexamethasone); FF9X0205V2 (tibolone); I47VB5DZ8O (Allylestrenol)


  2 / 110 MEDLINE  
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PMID:18639502
Autor:Shi X; Wu Y; Hang T; Xu X; Ding L; Tian Y; Wen A
Endereço:Department of Pharmacy, Xijing Hospital, The Fourth Military Medical University, Xi'an, Shaanxi, China.
Título:Application of a sensitive liquid chromatographic/tandem mass spectrometric method to a pharmacokinetic study of allylestrenol in healthy Chinese female volunteers.
Fonte:J Chromatogr B Analyt Technol Biomed Life Sci; 871(1):90-4, 2008 Aug 01.
ISSN:1570-0232
País de publicação:Netherlands
Idioma:eng
Resumo:A sensitive, specific and rapid liquid chromatographic/tandem mass spectrometric (LC/MS/MS) assay for the determination of allylestrenol in human plasma was established. Plasma samples were extracted by tert-butyl ether and separated by LC/MS/MS using a Phenomenex Curosil-PFP column (250 mm x 4.6 mm ID, dp 5 microm) with a mobile phase of methanol-water (95:5, v/v). The analytes were monitored with atmospheric pressure chemical ionization (APCI) by selected reaction monitoring (SRM) mode. The linear calibration curves covered a concentration range of 0.04-20.0 ng/mL with lower limit of quantification (LLOQ) at 0.04 ng/mL. The mean extraction recovery of allylestrenol was greater than 81.8%. The intra- and inter-day precisions were less than 1.3% and 3.1% respectively, determined from quality control (QC) samples of three representative concentrations. The method has been successfully applied to determining the plasma concentration of allylestrenol and a clinical pharmacokinetics study in healthy Chinese female volunteers.
Tipo de publicação: JOURNAL ARTICLE; VALIDATION STUDIES
Nome de substância:I47VB5DZ8O (Allylestrenol)


  3 / 110 MEDLINE  
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PMID:17373727
Autor:Urushibara M; Ishioka J; Hyochi N; Kihara K; Hara S; Singh P; Isaacs JT; Kageyama Y
Endereço:Department of Urology, Graduate School, Tokyo Medical and Dental University, Tokyo, Japan.
Título:Effects of steroidal and non-steroidal antiandrogens on wild-type and mutant androgen receptors.
Fonte:Prostate; 67(8):799-807, 2007 Jun 01.
ISSN:0270-4137
País de publicação:United States
Idioma:eng
Resumo:BACKGROUND: Molecular basis for secondary antiandrogen therapy in prostate cancer with mutant androgen receptors (ARs) is not fully elucidated. MATERIALS AND METHODS: Effects of steroidal and non-steroidal antiandrogens on transcriptional activities of wild-type and mutant (W741C, T877A, and W741C+T877A) ARs were measured. Crystal structure analysis and docking studies were performed using Molecular Operating Environment (MOE) package. RESULTS: DHT-induced transcriptional activity of the T877A mutant and the W741C mutant was suppressed by bicalutamide and hydroxyflutamide, respectively. Nilutamide suppressed the W741C mutant and the double mutant. Cyproterone acetate modestly inhibited the W741C mutant and the double mutant. The structural studies suggested that nilutamide and cyproterone acetate retain their antiandrogenic properties against both the W741C mutant and the double mutant due to fact that mutation W741C does not permit formation of key hydrophobic interaction between ligand and AR ligand binding domain, which is necessary for their conversion into agonists. CONCLUSIONS: Switching antiandrogens may be reasonable in prostate cancer with mutant ARs.
Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Nome de substância:0 (Androgen Antagonists); 0 (Androgen Receptor Antagonists); 0 (Androgens); 0 (Anilides); 0 (Imidazolidines); 0 (Nitriles); 0 (RNA, Neoplasm); 0 (Receptors, Androgen); 0 (Tosyl Compounds); 31D90UKP5Y (hydroxyflutamide); 3XMK78S47O (Testosterone); 4KM2BN5JHF (Cyproterone Acetate); 51G6I8B902 (nilutamide); 5H7I2IP58X (boldenone); 76W6J0943E (Flutamide); A0Z3NAU9DP (bicalutamide); EC 3.4.21.77 (Prostate-Specific Antigen); I47VB5DZ8O (Allylestrenol)


  4 / 110 MEDLINE  
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PMID:16910584
Autor:Noguchi K; Suzuki K; Teranishi J; Kondo K; Kishida T; Saito K; Uemura H; Kubota Y
Endereço:Department of Urology, Yokohama City University Medical Center.
Título:Recovery of serum prostate specific antigen value after interruption of antiandrogen therapy with allylestrenol for benign prostatic hyperplasia.
Fonte:Hinyokika Kiyo; 52(7):527-30, 2006 Jul.
ISSN:0018-1994
País de publicação:Japan
Idioma:eng
Resumo:Decrease in serum prostate specific antigen (PSA) concentration is inevitably associated with antiandrogen therapy for benign prostatic hyperplasia (BPH), and might mask the presence of prostate cancer or delay its diagnosis. To determine the appropriate timepoint for determination of correct PSA value, we sequentially measured serum PSA and testosterone levels after discontinuation of antiandrogen therapy for BPH. With informed consent, 12 patients (72.8 +/- 12.2* years old) with BPH were treated with allylestrenol 50 mg/day for 4 months. Serum testosterone and PSA concentrations were determined before and just after treatment, as well as every month after treatment up to 3 months. After treatment with allylestrenol for 4 months, mean serum testosterone and PSA levels were significantly decreased from 408 +/- 136* to 87.9 +/- 76.2* ng/dl, and from 2.81 +/- 0.87* to 2.04 +/- 0.82* ng/ml, respectively. The mean serum PSA level recovered to the pretreatment level within 2 months and mean serum testosterone concentration within one month after discontinuation of administration. In conclusion, during treatment of BPH with antiandrogen allylestrenol, a two-month washout is adequate for determination of correct PSA value (*: M +/- SD).
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Androgen Antagonists); 0 (Progesterone Congeners); 3XMK78S47O (Testosterone); EC 3.4.21.77 (Prostate-Specific Antigen); I47VB5DZ8O (Allylestrenol)


  5 / 110 MEDLINE  
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PMID:12094708
Autor:Noguchi K; Takeda M; Hosaka M; Kubota Y
Endereço:Department of Urology, Yokohama City University, School of Medicine.
Título:[Clinical effects of allylestrenol on patients with benign prostatic hyperplasia (BPH) evaluated with criteria for treatment efficacy in BPH].
Fonte:Hinyokika Kiyo; 48(5):269-73, 2002 May.
ISSN:0018-1994
País de publicação:Japan
Idioma:jpn
Resumo:One hundred and twenty-nine patients with benign prostatic hypertrophy (BPH) were registered and treated with allylestrenol. Allylestrenol was administered at a dose of 50 mg/day given twice a day for 16 weeks. Out of 129 patients with a mean age of 67.8 years old, 92 cases completed the study and 48 cases with moderate symptoms were objectively evaluated with "Criteria for Treatment Efficacy in BPH" proposed by The Japanese Urological Association in 1997. Prostate volume was significantly decreased from 32.7 +/- 11.9 to 27.4 +/- 11.2 ml (mean +/- SD), and maximum flow rate was significantly increased from 8.4 +/- 3.4 to 10.8 +/- 5.0 ml/sec. Residual urine volume was significantly decreased from 62.4 +/- 57.4 to 37.0 +/- 38.7 ml. IPSS was significantly decreased from 15.3 +/- 4.9 to 9.9 +/- 4.0, and QOL index was significantly decreased from 4.4 +/- 0.8 to 2.7 +/- 1.2. The efficacy of allylestrenol was shown by its effects on prostate volume (anatomy), maximum urinary flow rate (function), and symptom scores (symptom) at the end of 16 weeks of treatment. The rates of improvement for symptoms, QOL, function, and anatomy are 68.7% (N = 48), 79.2% (N = 48), 50.0% (N = 48), and 61.0% (N = 41), respectively. Overall efficacy (Good and Fair) was 70.9% (N = 48). During this study, 5 patients (3.9%) complained of loss of libido and 2 patients dropped out. In conclusion, allylestrenol was demonstrated to be a quite effective and safe medical treatment for patients with symptomatic BPH based on the criteria for treatment efficacy in BPH.
Tipo de publicação: CLINICAL TRIAL; ENGLISH ABSTRACT; JOURNAL ARTICLE; MULTICENTER STUDY
Nome de substância:0 (Progesterone Congeners); I47VB5DZ8O (Allylestrenol)


  6 / 110 MEDLINE  
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PMID:11999805
Autor:Csaba G; Karabélyos C; Inczefi-Gonda A
Endereço:Department of Genetics, Cell- and Immunobiology, Semmelweis University, Budapest, Hungary. csagyor@dgci.sote.hu
Título:Effect of tamoxifen treatment at adolescent age on the sexual behaviour and steroid hormone receptor binding of adult female rats.
Fonte:Acta Physiol Hung; 88(2):131-7, 2001.
ISSN:0231-424X
País de publicação:Hungary
Idioma:eng
Resumo:Hormonal imprinting takes place perinatally, at the first encounter between the target hormone and its developing receptor. However, there is a secondary critical period of imprinting at puberty. In these periods molecules similar to the hormones (members of the same hormone family, antagonists, certain environmental pollutants, etc.) can cause faulty imprinting with lifelong consequences. In the present experiments 5+2 days of tamoxifen treatment (120 microg/day) at adolescent age dramatically (from approx. 40% to 10%) reduced the sexual activity (Meyerson index and lordosis quotient) of female rats, soon after the finishment of the treatment and between four to six weeks after treatment. Similar results were observed in animals neonatally treated with allylestrenol and tamoxifen treated at puberty. Thymic glucocorticoid receptor and uterine estrogen receptor binding capacity were not influenced.
Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Nome de substância:0 (Estrogen Antagonists); 0 (Progesterone Congeners); 0 (Receptors, Estrogen); 0 (Receptors, Glucocorticoid); 094ZI81Y45 (Tamoxifen); I47VB5DZ8O (Allylestrenol)


  7 / 110 MEDLINE  
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PMID:11107528
Autor:Noguchi K; Uemura H; Takeda M; Sekiguchi Y; Ogawa K; Hosaka M
Endereço:Department of Urology, Yokohama City University, School of Medicine.
Título:[Rebound of prostate specific antigen after discontinuation of antiandrogen therapy for benign prostatic hyperplasia].
Fonte:Hinyokika Kiyo; 46(9):605-7, 2000 Sep.
ISSN:0018-1994
País de publicação:Japan
Idioma:jpn
Resumo:We compared the prostate specific antigen (PSA) levels in benign prostatic hyperplasia (BPH) patients with antiandrogen chlormadinone acetate (CMA) or allylestrenol (AE) before and during the treatment. We also investigated the serial change of PSA levels before, during and after discontinuation of antiandrogen therapy. Fifty-one BPH patients with normal PSA levels were treated with CMA or AE for 16 weeks. The mean serum PSA level significantly decreased after the treatment from 1.9 +/- 1.0 ng/ml to 1.1 +/- 0.7 ng/ml (M +/- SD). We discontinued medication with informed consent and the patients were carefully monitored for another 16 weeks. Nineteen patients were followed for 32 weeks. The mean serum PSA level decreased significantly from 2.0 +/- 1.0 ng/ml to 1.1 +/- 0.5 ng/ml (M +/- SD) and recovered approximately to the pretreatment level (1.7 +/- 1.1 ng/ml) at the end of this study. We found only one patient whose PSA was slightly elevated to a subnormal range (4.3 ng/ml) after discontinuation of therapy. The other BPH patients with normal PSA levels showed no excessive increase in PSA levels beyond the normal limit after discontinuation of antiandrogen therapy compared with the pretreatment baseline. In conclusion, BPH patients with a marked increase in PSA after discontinuation of antiandrogen therapy should be checked for prostate cancer.
Tipo de publicação: ENGLISH ABSTRACT; JOURNAL ARTICLE
Nome de substância:0 (Androgen Antagonists); 0 (Progesterone Congeners); 0SY050L61N (Chlormadinone Acetate); EC 3.4.21.77 (Prostate-Specific Antigen); I47VB5DZ8O (Allylestrenol)


  8 / 110 MEDLINE  
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PMID:10664567
Autor:Zivanovic L; Vojvodic L; Ristic P; Zecevic M; Nemcova I
Endereço:Institute of Pharmaceutical Chemistry and Drug Analysis, Faculty of Pharmacy, Belgrade, P.F. 146, Yugoslavia.
Título:Validation and application of the RP-HPLC method for the assay of allylestrenol and alpha-tocopherol in tablets.
Fonte:Biomed Chromatogr; 14(1):56-7, 2000 Feb.
ISSN:0269-3879
País de publicação:England
Idioma:eng
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Tablets); 1406-18-4 (Vitamin E); I47VB5DZ8O (Allylestrenol)


  9 / 110 MEDLINE  
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PMID:10075115
Autor:Karabélyos C; Horváth C; Holló I; Csaba G
Endereço:Department of Genetics, Cell and Immunobiology, Semmelweis University of Medicine, Budapest, Hungary.
Título:Effect of perinatal synthetic steroid hormone (allylestrenol, diethylstilbestrol) treatment (hormonal imprinting) on the bone mineralization of the adult male and female rat.
Fonte:Life Sci; 64(9):PL105-10, 1999.
ISSN:0024-3205
País de publicação:Netherlands
Idioma:eng
Resumo:Neonatal treatment with allylestrenol or diethylstilbestrol (DES) reduced the bone mineral content (BMC/bw) of the adult (four months old) female rats, without influencing bone mineral density (BMD/bw). In males these neonatal treatments elevated BMC and BMD alike. Ovariectomy alone decreased BMC and BMD alike; however the neonatal hormone treatments did not influence this reduced value. Ovariectomy of two months old animals increased body weight without the influence of neonatal hormone treatments. In adult males, the body weight was reduced significantly by neonatal DES and non-significantly by neonatal allylestrenol treatment. The experiments call attention to the possible human bone-effects of allylestrenol, which was used in the last decades as medication protecting endangered pregnancies.
Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Nome de substância:0 (Estrogens, Non-Steroidal); 0 (Progesterone Congeners); 731DCA35BT (Diethylstilbestrol); I47VB5DZ8O (Allylestrenol)


  10 / 110 MEDLINE  
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PMID:9804880
Autor:Martelli A; Mereto E; Ghia M; Orsi P; Allavena A; De Pascalis CR; Brambilla G
Endereço:Department of Internal Medicine, Division of Clinical Pharmacology and Toxicology, University of Genoa, I-16132, Genoa, Italy.
Título:Induction of micronuclei and of enzyme-altered foci in the liver of female rats exposed to progesterone and three synthetic progestins.
Fonte:Mutat Res; 419(1-3):33-41, 1998 Nov 09.
ISSN:0027-5107
País de publicação:Netherlands
Idioma:eng
Resumo:Progesterone (PG) and three structurally similar synthetic progestins-norethisterone (NE), allylestrenol (AE), and dydrogesterone (DG)-have been compared for their ability to induce the formation of micronuclei and of enzyme-altered foci in the liver of female rats. In the micronucleus assay, carried out in rats given a single p.o. dose of 100 mg kg-1 3 days before partial hepatectomy and sacrificed for cell sampling 2 days later, the frequency of micronucleated hepatocytes was 3.5-fold higher than in controls with PG, 2.8-fold with DG, 2.2-fold with NE and 2.1-fold with AE, but the increase was statistically significant only for PG. In the liver foci assay, performed to evaluate the tumor initiating activity of p. o. dosing with 100 mg kg-1 once a week for 6 successive weeks, the values of the number and area of gamma-glutamyltranspeptidase-positive foci were, as compared to controls, 15.9- and 100-fold higher with NE, and 13.9- and 52-fold higher with AE, but only the increase of area produced by NE was statistically significant; PG and DG did not display in this test any activities. Considered together with previous findings, these results suggest that NE might be biotransformed in the liver into reactive species and thus behave as a weak genotoxic agent.
Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Nome de substância:0 (Carcinogens); 0 (Mutagens); 0 (Progesterone Congeners); 4G7DS2Q64Y (Progesterone); 4KM2BN5JHF (Cyproterone Acetate); 90I02KLE8K (Dydrogesterone); EC 2.3.2.2 (gamma-Glutamyltransferase); I47VB5DZ8O (Allylestrenol); T18F433X4S (Norethindrone)



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