Base de dados : MEDLINE
Pesquisa : D02.092.471 [Categoria DeCS]
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[PMID]:28866249
[Au] Autor:Akincioglu A; Kocaman E; Akincioglu H; Salmas RE; Durdagi S; Gülçin I; Supuran CT; Göksu S
[Ad] Endereço:Atatürk University, Faculty of Science, Department of Chemistry, Erzurum, Turkey; Agri Ibrahim Çeçen University, Central Researching Laboratory, Agri, Turkey.
[Ti] Título:The synthesis of novel sulfamides derived from ß-benzylphenethylamines as acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase enzymes inhibitors.
[So] Source:Bioorg Chem;74:238-250, 2017 Oct.
[Is] ISSN:1090-2120
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In this study, a series of novel ß-benzylphenethylamines and their sulfamide derivatives were synthesized starting from (Z)-2,3-diphenylacrylonitriles. Pd-C catalysed hydrogenation of diphenylacrylonitriles, reduction of propanenitriles with LiAlH in the presence of AlCl followed by addition of conc. HCl afforded ß-benzylphenethylamine hydrochloride salts. The reactions of these amine hydrochloride salts with chlorosulfonyl isocyanate (CSI) in the presence of tert-BuOH and excess Et N gave sulfamoylcarbamates. Removing of Boc group from the synthesized sulfamoylcarbamates with trifluoroacetic acid (TFA) yielded novel sulfamides in good yields. These novel sulfamides derived from ß-benzylphenethylamines were effective inhibitors of the cytosolic carbonic anhydrase I and II isoenzymes (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with K values in the range of 0.278-2.260nM for hCA I, 0.187-1.478nM for hCA II, 0.127-2.452nM for AChE and 0.494-1.790nM for BChE. The inhibitory effects of the synthesized novel sulfamides derived from ß-benzylphenethylamines were compared to those of acetazolamide and dorzolamide as clinical hCA I and II isoenzymes inhibitors and tacrine as a clinical AChE and BChE enzymes inhibitors. In addition to in vitro tests, molecular modeling approaches are implemented not only for prediction of the binding affinities of the compounds but also to study their inhibition mechanisms in atomic level at the catalytic domains.
[Mh] Termos MeSH primário: Compostos de Benzil/farmacologia
Inibidores da Anidrase Carbônica/farmacologia
Inibidores da Colinesterase/farmacologia
Etilaminas/farmacologia
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/metabolismo
Compostos de Benzil/química
Butirilcolinesterase/metabolismo
Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Etilaminas/química
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzyl Compounds); 0 (Carbonic Anhydrase Inhibitors); 0 (Cholinesterase Inhibitors); 0 (Ethylamines); 0 (Sulfonamides); 0 (beta-benzylphenethylamine); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170904
[St] Status:MEDLINE


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[PMID]:28800452
[Au] Autor:Sakauchi N; Furukawa H; Shirai J; Sato A; Kuno H; Saikawa R; Yoshida M
[Ad] Endereço:Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan. Electronic address: nobuki.sakauchi@takeda.com.
[Ti] Título:Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective α adrenoceptor antagonists.
[So] Source:Eur J Med Chem;139:114-127, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of phenoxyethylamine derivatives was designed and synthesized to discover potent and selective human α adrenoceptor (α adrenergic receptor; α -AR) antagonists. Compound 7 was taken from our internal compound collection as an attractive starting point and exhibited moderate binding affinity for α -AR and high selectivity against α - and α -ARs. We focused on modifying the 2-methylsulfonylbenzyl group of 7 to discover novel compounds structurally distinct from other reported α -AR antagonists containing the phenoxyethylamine motif. Study of structure activity relationship guided by a targeted ligand-lipophilicity efficiency score led to the discovery of a novel scaffold of 3,4-dihydro-2H-thiochromene 1,1-dioxide for selective α -AR antagonists. Further optimization studies resulted in the identification of (4S)-N -[2-(2,5-difluorophenoxy)ethyl]-N -methyl-3,4-dihydro-2H-thiochromene-4,6-diamine 1,1-dioxide, (S)-41, as a novel, highly potent and selective α -AR antagonist. Herein, we provide details of the structure activity relationship of the phenoxyethylamine analog for the potency and selectivity.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos alfa 1/farmacologia
Benzopiranos/farmacologia
Inibidores Enzimáticos/farmacologia
Etilaminas/farmacologia
Receptores Adrenérgicos alfa 1/metabolismo
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos alfa 1/síntese química
Antagonistas de Receptores Adrenérgicos alfa 1/química
Benzopiranos/síntese química
Benzopiranos/química
Citocromo P-450 CYP3A/metabolismo
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Etilaminas/química
Seres Humanos
Microssomos Hepáticos/efeitos dos fármacos
Microssomos Hepáticos/metabolismo
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-1 Receptor Antagonists); 0 (Benzopyrans); 0 (Enzyme Inhibitors); 0 (Ethylamines); 0 (Receptors, Adrenergic, alpha-1); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE


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[PMID]:28413169
[Au] Autor:Zarei F; Rezazadeh Azari M; Salehpour S; Khodakarim S; Omidi L; Tavakol E
[Ad] Endereço:Department of Occupational Health Engineering, School of Public Health, Shahid Beheshti University of Medical Science, Tehran, Iran.
[Ti] Título:Respiratory Effects of Simultaneous Exposure to Respirable Crystalline Silica Dust, Formaldehyde, and Triethylamine of a Group of Foundry Workers.
[So] Source:J Res Health Sci;17(1):e00371, 2017 03 04.
[Is] ISSN:2228-7809
[Cp] País de publicação:Iran
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Foundry workers are occupationally exposed to hazardous substances such as silica dusts and toxic gases. The aim of this study was to examine the effects of simultaneous exposure to complex mixtures of silica dust, formaldehyde, and triethylamine on lung function parameters. STUDY DESIGN: A cross-sectional study. METHODS: This study was conducted on 55 male workers of core making unit of a foundry plant (the case group) and 55 workers in a food industry were enrolled as a control group in 2015. Workers were monitored for personal exposure to crystalline silica respirable dust, according the NIOSH method No.7602. The concentrations of formaldehyde and triethylamine were measured using a PID instrument. Lung function tests were performed according to the ERS/ATS standards. RESULTS: The mean concentrations of personal exposure to silica dust, formaldehyde, and triethylamine in the core making workers were 0.23 mg/m3, 2.85 ppm, and 5.55 ppm and respective exposures of control subjects were less than the LOD (limit of detection). There were significant associations between exposure to silica dust and decreases in FVC (Forced vital capacity) values (P<0.05). The findings showed a statistically significant synergistic effect of silica dust and triethylamine on FVC values (P<0.05). CONCLUSIONS: The mean exposure of all studied substances was higher than occupational exposure limits. Synergistic effects of exposure to silica dust and triethylamine on some lung function parameters were observed. Simultaneous exposure of foundry workers to silica dust and triethylamine could impair lung function.
[Mh] Termos MeSH primário: Poluentes Atmosféricos/efeitos adversos
Etilaminas/efeitos adversos
Formaldeído/efeitos adversos
Pulmão/efeitos dos fármacos
Indústria Manufatureira
Exposição Ocupacional/efeitos adversos
Dióxido de Silício/efeitos adversos
[Mh] Termos MeSH secundário: Adulto
Poluentes Atmosféricos/análise
Misturas Complexas/efeitos adversos
Estudos Transversais
Poeira/análise
Monitoramento Ambiental/métodos
Etilaminas/análise
Formaldeído/análise
Seres Humanos
Pulmão/fisiologia
Masculino
Exposição Ocupacional/análise
Ocupações
Testes de Função Respiratória
Dióxido de Silício/análise
Capacidade Vital
Trabalho
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Air Pollutants); 0 (Complex Mixtures); 0 (Dust); 0 (Ethylamines); 1HG84L3525 (Formaldehyde); 7631-86-9 (Silicon Dioxide); VOU728O6AY (triethylamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171022
[Lr] Data última revisão:
171022
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170418
[St] Status:MEDLINE


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[PMID]:28325450
[Au] Autor:Onay A; Onay M; Abul O
[Ad] Endereço:Department of Computer Engineering, TOBB University of Economics & Technology, 06560, Ankara, Turkey.
[Ti] Título:Classification of nervous system withdrawn and approved drugs with ToxPrint features via machine learning strategies.
[So] Source:Comput Methods Programs Biomed;142:9-19, 2017 Apr.
[Is] ISSN:1872-7565
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND OBJECTIVES: Early-phase virtual screening of candidate drug molecules plays a key role in pharmaceutical industry from data mining and machine learning to prevent adverse effects of the drugs. Computational classification methods can distinguish approved drugs from withdrawn ones. We focused on 6 data sets including maximum 110 approved and 110 withdrawn drugs for all and nervous system diseases to distinguish approved drugs from withdrawn ones. METHODS: In this study, we used support vector machines (SVMs) and ensemble methods (EMs) such as boosted and bagged trees to classify drugs into approved and withdrawn categories. Also, we used CORINA Symphony program to identify Toxprint chemotypes including over 700 predefined chemotypes for determination of risk and safety assesment of candidate drug molecules. In addition, we studied nervous system withdrawn drugs to determine the key fragments with The ParMol package including gSpan algorithm. RESULTS: According to our results, the descriptors named as the number of total chemotypes and bond CN_amine_aliphatic_generic were more significant descriptors. The developed Medium Gaussian SVM model reached 78% prediction accuracy on test set for drug data set including all disease. Here, bagged tree and linear SVM models showed 89% of accuracies for phycholeptics and psychoanaleptics drugs. A set of discriminative fragments in nervous system withdrawn drug (NSWD) data sets was obtained. These fragments responsible for the drugs removed from market were benzene, toluene, N,N-dimethylethylamine, crotylamine, 5-methyl-2,4-heptadiene, octatriene and carbonyl group. CONCLUSION: This paper covers the development of computational classification methods to distinguish approved drugs from withdrawn ones. In addition, the results of this study indicated the identification of discriminative fragments is of significance to design a new nervous system approved drugs with interpretation of the structures of the NSWDs.
[Mh] Termos MeSH primário: Simulação por Computador
Sistema Nervoso/efeitos dos fármacos
Retirada de Medicamento Baseada em Segurança/estatística & dados numéricos
Máquina de Vetores de Suporte
[Mh] Termos MeSH secundário: Algoritmos
Área Sob a Curva
Benzeno/toxicidade
Carbono
Mineração de Dados
Aprovação de Drogas
Monitoramento de Medicamentos
Etilaminas/toxicidade
Reações Falso-Positivas
Seres Humanos
Modelos Lineares
Segurança do Paciente
Reconhecimento Automatizado de Padrão/métodos
Preparações Farmacêuticas/química
Vigilância de Produtos Comercializados/normas
Risco
Sensibilidade e Especificidade
Tolueno/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ethylamines); 0 (Pharmaceutical Preparations); 3FPU23BG52 (Toluene); 7440-44-0 (Carbon); 9N5384XVEM (N,N-dimethylethylamine); J64922108F (Benzene)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170323
[St] Status:MEDLINE


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[PMID]:28287460
[Au] Autor:Brenner AK; Reikvam H; Rye KP; Hagen KM; Lavecchia A; Bruserud Ø
[Ad] Endereço:Section for Hematology, Department of Clinical Science, Faculty of Medicine and Dentistry, University of Bergen, Bergen 5021, Norway. annette.brenner@uib.no.
[Ti] Título:CDC25 Inhibition in Acute Myeloid Leukemia-A Study of Patient Heterogeneity and the Effects of Different Inhibitors.
[So] Source:Molecules;22(3), 2017 Mar 11.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Cell division cycle 25 (CDC25) protein phosphatases regulate cell cycle progression through the activation of cyclin-dependent kinases (CDKs), but they are also involved in chromatin modulation and transcriptional regulation. CDC25 inhibition is regarded as a possible therapeutic strategy for the treatment of human malignancies, including acute myeloid leukemia (AML). We investigated the in vitro effects of CDC25 inhibitors on primary human AML cells derived from 79 unselected patients in suspension cultures. Both the previously well-characterized CDC25 inhibitor NSC95397, as well as five other inhibitors (BN82002 and the novel small molecular compounds ALX1, ALX2, ALX3, and ALX4), only exhibited antiproliferative effects for a subset of patients when tested alone. These antiproliferative effects showed associations with differences in genetic abnormalities and/or AML cell differentiation. However, the responders to CDC25 inhibition could be identified by analysis of global gene expression profiles. The differentially expressed genes were associated with the cytoskeleton, microtubules, and cell signaling. The constitutive release of 28 soluble mediators showed a wide variation among patients and this variation was maintained in the presence of CDC25 inhibition. Finally, NSC95397 had no or only minimal effects on AML cell viability. In conclusion, CDC25 inhibition has antiproliferative effects on primary human AML cells for a subset of patients, and these patients can be identified by gene expression profiling.
[Mh] Termos MeSH primário: Proteínas do Citoesqueleto/genética
Regulação Leucêmica da Expressão Gênica
Leucemia Mieloide Aguda/genética
Proteínas dos Microtúbulos/genética
Células Mieloides/metabolismo
Fosfatases cdc25/antagonistas & inibidores
[Mh] Termos MeSH secundário: Antineoplásicos/farmacologia
Biomarcadores Farmacológicos/metabolismo
Sobrevivência Celular/efeitos dos fármacos
Biologia Computacional
Proteínas do Citoesqueleto/metabolismo
Inibidores Enzimáticos/farmacologia
Etilaminas/farmacologia
Perfilação da Expressão Gênica
Heterogeneidade Genética
Seres Humanos
Leucemia Mieloide Aguda/metabolismo
Leucemia Mieloide Aguda/patologia
Proteínas dos Microtúbulos/metabolismo
Células Mieloides/efeitos dos fármacos
Células Mieloides/patologia
Naftoquinonas/farmacologia
Nitrocompostos/farmacologia
Farmacogenética
Cultura Primária de Células
Transdução de Sinais
Bibliotecas de Moléculas Pequenas/farmacologia
Fosfatases cdc25/genética
Fosfatases cdc25/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2,3-bis(2-hydroxyethylsulfanyl)-(1,4)naphthoquinone); 0 (Antineoplastic Agents); 0 (BN82002); 0 (Biomarkers, Pharmacological); 0 (Cytoskeletal Proteins); 0 (Enzyme Inhibitors); 0 (Ethylamines); 0 (Microtubule Proteins); 0 (Naphthoquinones); 0 (Nitro Compounds); 0 (Small Molecule Libraries); EC 3.1.3.48 (cdc25 Phosphatases)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170515
[Lr] Data última revisão:
170515
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170314
[St] Status:MEDLINE


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[PMID]:28120383
[Au] Autor:Pícha J; Budesínský M; Machácková K; Collinsová M; Jirácek J
[Ad] Endereço:Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, v.v.i., Flemingovo nám. 2, 166 10, Prague 6, Czech Republic.
[Ti] Título:Optimized syntheses of Fmoc azido amino acids for the preparation of azidopeptides.
[So] Source:J Pept Sci;23(3):202-214, 2017 Mar.
[Is] ISSN:1099-1387
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The rise of CuI-catalyzed click chemistry has initiated an increased demand for azido and alkyne derivatives of amino acid as precursors for the synthesis of clicked peptides. However, the use of azido and alkyne amino acids in peptide chemistry is complicated by their high cost. For this reason, we investigated the possibility of the in-house preparation of a set of five Fmoc azido amino acids: ß-azido l-alanine and d-alanine, γ-azido l-homoalanine, δ-azido l-ornithine and ω-azido l-lysine. We investigated several reaction pathways described in the literature, suggested several improvements and proposed several alternative routes for the synthesis of these compounds in high purity. Here, we demonstrate that multigram quantities of these Fmoc azido amino acids can be prepared within a week or two and at user-friendly costs. We also incorporated these azido amino acids into several model tripeptides, and we observed the formation of a new elimination product of the azido moiety upon conditions of prolonged couplings with 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate/DIPEA. We hope that our detailed synthetic protocols will inspire some peptide chemists to prepare these Fmoc azido acids in their laboratories and will assist them in avoiding the too extensive costs of azidopeptide syntheses. Experimental procedures and/or analytical data for compounds 3-5, 20, 25, 26, 30 and 43-47 are provided in the supporting information. © 2017 The Authors Journal of Peptide Science published by European Peptide Society and John Wiley & Sons Ltd.
[Mh] Termos MeSH primário: Aminoácidos/síntese química
Azidas/química
Química Click/métodos
Fluorenos/síntese química
Peptídeos/síntese química
[Mh] Termos MeSH secundário: Alquinos/química
Etilaminas/química
Fluorenos/química
Triazóis/química
Ureia/análogos & derivados
Ureia/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkynes); 0 (Amino Acids); 0 (Azides); 0 (Ethylamines); 0 (Fluorenes); 0 (N(alpha)-fluorenylmethyloxycarbonylamino acids); 0 (Peptides); 0 (Triazoles); 5SIQ15721L (N,N-diisopropylethylamine); 8W8T17847W (Urea); X5I03TZQ8D (2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170324
[Lr] Data última revisão:
170324
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170126
[St] Status:MEDLINE
[do] DOI:10.1002/psc.2968


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[PMID]:28097528
[Au] Autor:Halberstadt AL
[Ad] Endereço:Department of Psychiatry, University of California San Diego, 9500 Gilman Drive, La Jolla, CA, 92093-0804, USA. ahalbers@ucsd.edu.
[Ti] Título:Pharmacology and Toxicology of N-Benzylphenethylamine ("NBOMe") Hallucinogens.
[So] Source:Curr Top Behav Neurosci;32:283-311, 2017.
[Is] ISSN:1866-3370
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Serotonergic hallucinogens induce profound changes in perception and cognition. The characteristic effects of hallucinogens are mediated by 5-HT receptor activation. One class of hallucinogens are 2,5-dimethoxy-substituted phenethylamines, such as the so-called 2C-X compounds 2,5-dimethoxy-4-bromophenethylamine (2C-B) and 2,5-dimethoxy-4-iodophenethylamine (2C-I). Addition of an N-benzyl group to phenethylamine hallucinogens produces a marked increase in 5-HT -binding affinity and hallucinogenic potency. N-benzylphenethylamines ("NBOMes") such as N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (25I-NBOMe) show subnanomolar affinity for the 5-HT receptor and are reportedly highly potent in humans. Several NBOMEs have been available from online vendors since 2010, resulting in numerous cases of toxicity and multiple fatalities. This chapter reviews the structure-activity relationships, behavioral pharmacology, metabolism, and toxicity of members of the NBOMe hallucinogen class. Based on a review of 51 cases of NBOMe toxicity reported in the literature, it appears that rhabdomyolysis is a relatively common complication of severe NBOMe toxicity, an effect that may be linked to NBOMe-induced seizures, hyperthermia, and vasoconstriction.
[Mh] Termos MeSH primário: Alucinógenos/farmacologia
Receptor 5-HT2A de Serotonina/efeitos dos fármacos
Agonistas de Receptores 5-HT2 de Serotonina/farmacologia
[Mh] Termos MeSH secundário: Animais
Dimetoxifeniletilamina/efeitos adversos
Dimetoxifeniletilamina/análogos & derivados
Dimetoxifeniletilamina/química
Dimetoxifeniletilamina/farmacologia
Etilaminas/efeitos adversos
Etilaminas/química
Etilaminas/farmacologia
Febre/induzido quimicamente
Alucinógenos/efeitos adversos
Alucinógenos/química
Seres Humanos
Iodobenzenos/efeitos adversos
Iodobenzenos/química
Iodobenzenos/farmacologia
Camundongos
Receptor 5-HT2C de Serotonina/efeitos dos fármacos
Rabdomiólise/induzido quimicamente
Convulsões/induzido quimicamente
Agonistas de Receptores 5-HT2 de Serotonina/efeitos adversos
Agonistas de Receptores 5-HT2 de Serotonina/química
Relação Estrutura-Atividade
Vasoconstrição/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.; REVIEW
[Nm] Nome de substância:
0 (2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine); 0 (4-iodo-2,5-dimethoxy-beta-phenethylamine); 0 (Dimethoxyphenylethylamine); 0 (Ethylamines); 0 (Hallucinogens); 0 (Iodobenzenes); 0 (N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine); 0 (Receptor, Serotonin, 5-HT2A); 0 (Receptor, Serotonin, 5-HT2C); 0 (Serotonin 5-HT2 Receptor Agonists); V77772N32H (2-(4-bromo-2,5-dimethoxyphenyl)ethylamine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170119
[St] Status:MEDLINE
[do] DOI:10.1007/7854_2016_64


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[PMID]:27889455
[Au] Autor:Prabhakaran J; Solingapuram Sai KK; Zanderigo F; Rubin-Falcone H; Jorgensen MJ; Kaplan JR; Tooke KI; Mintz A; Mann JJ; Kumar JS
[Ad] Endereço:Department of Psychiatry, Columbia University Medical Center, New York, USA; Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA.
[Ti] Título:In vivo evaluation of [ F]FECIMBI-36, an agonist 5-HT receptor PET radioligand in nonhuman primate.
[So] Source:Bioorg Med Chem Lett;27(1):21-23, 2017 01 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We recently reported the radiosynthesis and in vitro evaluation of [ F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([ F]FECIMBI-36) or ([ F]1), an agonist radioligand for 5HT receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [ F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [ F]FECIMBI-36 penetrates the blood-brain barrier and a low retention of radioactivity is observed in monkey brain. Although the time activity curves indicate a somehow heterogeneous distribution of the radioligand in the brain, the low level of [ F]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT receptors by PET.
[Mh] Termos MeSH primário: Etilaminas/farmacologia
Radioisótopos de Flúor/farmacologia
Tomografia por Emissão de Pósitrons
Receptor 5-HT2A de Serotonina/metabolismo
Receptor 5-HT2C de Serotonina/metabolismo
Agonistas de Receptores 5-HT2 de Serotonina/farmacologia
[Mh] Termos MeSH secundário: Animais
Cercopithecus aethiops
Relação Dose-Resposta a Droga
Etilaminas/síntese química
Etilaminas/química
Radioisótopos de Flúor/química
Seres Humanos
Ligantes
Imagem por Ressonância Magnética
Masculino
Estrutura Molecular
Agonistas de Receptores 5-HT2 de Serotonina/síntese química
Agonistas de Receptores 5-HT2 de Serotonina/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (((18)F)-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine); 0 (Ethylamines); 0 (Fluorine Radioisotopes); 0 (Ligands); 0 (Receptor, Serotonin, 5-HT2A); 0 (Receptor, Serotonin, 5-HT2C); 0 (Serotonin 5-HT2 Receptor Agonists)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161128
[St] Status:MEDLINE


  9 / 2514 MEDLINE  
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[PMID]:27862093
[Au] Autor:Talaat W
[Ad] Endereço:Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Damanhour University, Damnhour, Egypt.
[Ti] Título:Bioanalytical method for the estimation of co-administered esomeprazole, leflunomide and ibuprofen in human plasma and in pharmaceutical dosage forms using micellar liquid chromatography.
[So] Source:Biomed Chromatogr;31(5), 2017 May.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The present study represents a connection between basic science and clinical applied science through providing a bioanalytical method for the analysis of certain co-administered drugs used for the treatment of rheumatoid arthritis. The studied drugs are esomeprazole, leflunomide and ibuprofen. The proposed bioanalytical method is a simple reversed phase high performance liquid chromatographic method using micellar mobile phase. The method is conducted using a Shim-pack VP-ODS (150 mm × 4.6 mm ID) stainless steel column at ambient temperature with ultraviolet detection at 285 nm. The micellar mobile phase consisted of 0.1 m sodium dodecyl sulfate, 10% n-propanol, 0.3% triethylamine in 0.02 m orthophosphoric acid (pH 3.5) and is pumped at a flow rate of 1.0 mL/min. The calibration curve was rectilinear over the concentration range of 0.1-5.0, 0.5-10.0 and 1.0-20.0 µg/mL for esomeprazole, leflunomide and ibuprofen respectively. The proposed method was successfully applied to the analysis of these drugs in dosage forms. The method is extended to the in-vitro, in-vivo determination of these drugs in spiked and real human plasma samples.
[Mh] Termos MeSH primário: Cromatografia Líquida/métodos
Esomeprazol/sangue
Ibuprofeno/sangue
Isoxazóis/sangue
[Mh] Termos MeSH secundário: Adulto
Calibragem
Quimioterapia Combinada
Esomeprazol/administração & dosagem
Etilaminas/química
Seres Humanos
Ibuprofeno/administração & dosagem
Isoxazóis/administração & dosagem
Limite de Detecção
Masculino
Micelas
Ácidos Fosfóricos/química
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
Dodecilsulfato de Sódio/química
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ethylamines); 0 (Isoxazoles); 0 (Micelles); 0 (Phosphoric Acids); 368GB5141J (Sodium Dodecyl Sulfate); E4GA8884NN (phosphoric acid); G162GK9U4W (leflunomide); N3PA6559FT (Esomeprazole); VOU728O6AY (triethylamine); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170619
[Lr] Data última revisão:
170619
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161119
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.3865


  10 / 2514 MEDLINE  
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[PMID]:27847109
[Au] Autor:Lan H; Rönkkö T; Parshintsev J; Hartonen K; Gan N; Sakeye M; Sarfraz J; Riekkola ML
[Ad] Endereço:Laboratory of Analytical Chemistry, Department of Chemistry, University of Helsinki, P.O. Box 55, 00014 University of Helsinki, Finland.
[Ti] Título:Modified zeolitic imidazolate framework-8 as solid-phase microextraction Arrow coating for sampling of amines in wastewater and food samples followed by gas chromatography-mass spectrometry.
[So] Source:J Chromatogr A;1486:76-85, 2017 Feb 24.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this study, a novel solid phase microextration (SPME) Arrow was prepared for the sampling of volatile low molecular weight alkylamines (trimethylamine (TMA) and triethylamine (TEA)) in wastewater, salmon and mushroom samples before gas chromatographic separation with mass spectrometer as detector. Acidified zeolitic imidazolate framework-8 (A-ZIF-8) was utilized as adsorbent and poly(vinyl chloride) (PVC) as the adhesive. The custom SPME Arrow was fabricated via a physical adhesion: (1) ZIF-8 particles were suspended in a mixture of tetrahydrofuran (THF) and PVC to form a homogeneous suspension, (2) a non-coated stainless steel SPME Arrow was dipped in the ZIF-8/PVC suspension for several times to obtain a uniform and thick coating, (3) the pore size of ZIF-8 was modified by headspace exposure to hydrochloric acid in order to increase the extraction efficiency for amines. The effect of ZIF-8 concentration in PVC solution, dipping cycles and aging temperature on extraction efficiency was investigated. In addition, sampling parameters such as NaCl concentration, sample volume, extraction time, potassium hydroxide concentration, desorption temperature and desorption time were optimized. The Arrow-to-Arrow reproducibilities (RSDs) for five ZIF-8 coated Arrows were 15.6% and 13.3% for TMA and TEA, respectively. The extraction with A-ZIF-8/PVC Arrow was highly reproducible for at least 130 cycles without noticeable decrease of performance (RSD<12.5%). Headspace SPME of 7.5mL sample solution with the fabricated ZIF-8 coated Arrow achieved linear ranges of 1-200ngmL for both TMA and TEA. The limit of quantitation (LOQ) was 1ngmL for both TMA and TEA. The method was successfully applied to the determination of TMA and TEA in wastewater, salmon and mushroom samples giving satisfactory selectivity towards the studied amines.
[Mh] Termos MeSH primário: Aminas/análise
Aminas/química
Análise de Alimentos/métodos
Cromatografia Gasosa-Espectrometria de Massas
Imidazóis/química
Microextração em Fase Sólida/métodos
Águas Residuais/química
Zeolitas/química
[Mh] Termos MeSH secundário: Agaricales/química
Animais
Etilaminas/análise
Etilaminas/química
Metilaminas/análise
Metilaminas/química
Peso Molecular
Cloreto de Polivinila/química
Salmão
Alimentos Marinhos
Cloreto de Sódio/química
Microextração em Fase Sólida/instrumentação
Aço Inoxidável/química
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Ethylamines); 0 (Imidazoles); 0 (Methylamines); 0 (Waste Water); 0 (acidified zeolitic imidazolate framework-8); 12597-68-1 (Stainless Steel); 1318-02-1 (Zeolites); 451W47IQ8X (Sodium Chloride); 9002-86-2 (Polyvinyl Chloride); LHH7G8O305 (trimethylamine); VOU728O6AY (triethylamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161117
[St] Status:MEDLINE



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