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Pesquisa : D02.455.426.100.080 [Categoria DeCS]
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[PMID]:29233651
[Au] Autor:Gong H; Weinstein DS; Lu Z; Duan JJ; Stachura S; Haque L; Karmakar A; Hemagiri H; Raut DK; Gupta AK; Khan J; Camac D; Sack JS; Pudzianowski A; Wu DR; Yarde M; Shen DR; Borowski V; Xie JH; Sun H; D'Arienzo C; Dabros M; Galella MA; Wang F; Weigelt CA; Zhao Q; Foster W; Somerville JE; Salter-Cid LM; Barrish JC; Carter PH; Dhar TGM
[Ad] Endereço:Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543-4000, United States.
[Ti] Título:Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
[So] Source:Bioorg Med Chem Lett;28(2):85-93, 2018 01 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor α (LXRα). Structure-based drug design (SBDD) led to the identification of benzothiazine and tetrahydroquinoline sulfonamide analogs which completely dialed out LXRα activity and were less potent at PXR. Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Y in the PXR assay for long term preclinical pharmacokinetic (PK) studies.
[Mh] Termos MeSH primário: Compostos Bicíclicos com Pontes/farmacologia
Desenho de Drogas
Propanóis/farmacologia
Receptores do Ácido Retinoico/agonistas
Receptores de Esteroides/agonistas
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Animais
Compostos Bicíclicos com Pontes/síntese química
Compostos Bicíclicos com Pontes/química
Cristalografia por Raios X
Relação Dose-Resposta a Droga
Seres Humanos
Receptores X do Fígado/agonistas
Masculino
Camundongos
Camundongos Endogâmicos BALB C
Modelos Moleculares
Estrutura Molecular
Propanóis/síntese química
Propanóis/química
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); 0 (Liver X Receptors); 0 (Propanols); 0 (Receptors, Retinoic Acid); 0 (Receptors, Steroid); 0 (Sulfonamides); 0 (pregnane X receptor); 0 (retinoic acid receptor gamma); 3D632GYQ50 (hexafluoroisopropanol)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171214
[St] Status:MEDLINE


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[PMID]:29272360
[Au] Autor:Hasan MK; Friedman TC; Sims C; Lee DL; Espinoza-Derout J; Ume A; Chalfant V; Lee ML; Sinha-Hikim I; Lutfy K; Liu Y; Mahata SK; Sinha-Hikim AP
[Ad] Endereço:Division of Endocrinology, Metabolism and Molecular Medicine, Department of Internal Medicine, Charles R. Drew University of Medicine and Science, Los Angeles, California.
[Ti] Título:α7-Nicotinic Acetylcholine Receptor Agonist Ameliorates Nicotine Plus High-Fat Diet-Induced Hepatic Steatosis in Male Mice by Inhibiting Oxidative Stress and Stimulating AMPK Signaling.
[So] Source:Endocrinology;159(2):931-944, 2018 02 01.
[Is] ISSN:1945-7170
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:α7-Nicotinic acetylcholine receptor (α7nAChR) agonists confer protection against a wide variety of cytotoxic insults and suppress oxidative stress and apoptosis in various cell systems, including hepatocytes. We recently demonstrated that nicotine, when combined with a high-fat diet (HFD), triggers oxidative stress, activates hepatocyte apoptosis, and exacerbates HFD-induced hepatic steatosis in male mice. This study evaluates whether PNU-282987 (PNU), a specific α7nAChR agonist, is effective in preventing nicotine plus HFD-induced hepatic steatosis. Adult C57BL6 male mice were fed a normal chow diet or HFD with 60% of calories derived from fat and received twice-daily intraperitoneal injections of 0.75 mg/kg body weight (BW) of nicotine, PNU (0.26 mg/kg BW), PNU plus nicotine, or saline for 10 weeks. PNU treatment was effective in attenuating nicotine plus HFD-induced increase in hepatic triglyceride levels, hepatocyte apoptosis, and hepatic steatosis. The preventive effects of PNU on nicotine plus HFD-induced hepatic steatosis were mediated by suppression of oxidative stress and activation of adenosine 5'-monophosphate-activated protein kinase (AMPK) together with inhibition of its downstream target sterol regulatory element binding protein 1c (SREBP1c), fatty acid synthase (FAS), and acetyl-coenzyme A-carboxylase (ACC). We conclude that the α7nAChR agonist PNU protects against nicotine plus HFD-induced hepatic steatosis in obese mice. PNU appears to work at various steps of signaling pathways involving suppression of oxidative stress, activation of AMPK, and inhibition of SREBP1c, FAS, and ACC. α7nAChR agonists may be an effective therapeutic strategy for ameliorating fatty liver disease, especially in obese smokers.
[Mh] Termos MeSH primário: Benzamidas/farmacologia
Compostos Bicíclicos com Pontes/farmacologia
Fígado Gorduroso/tratamento farmacológico
Estresse Oxidativo/efeitos dos fármacos
[Mh] Termos MeSH secundário: Proteínas Quinases Ativadas por AMP/metabolismo
Animais
Benzamidas/uso terapêutico
Compostos Bicíclicos com Pontes/uso terapêutico
Dieta Hiperlipídica/efeitos adversos
Fígado Gorduroso/etiologia
Fígado Gorduroso/metabolismo
Fígado Gorduroso/patologia
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Obesos
Nicotina/toxicidade
Transdução de Sinais/efeitos dos fármacos
Receptor Nicotínico de Acetilcolina alfa7/agonistas
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Benzamides); 0 (Bridged Bicyclo Compounds); 0 (PNU-282987); 0 (alpha7 Nicotinic Acetylcholine Receptor); 6M3C89ZY6R (Nicotine); EC 2.7.11.31 (AMP-Activated Protein Kinases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180215
[Lr] Data última revisão:
180215
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171223
[St] Status:MEDLINE
[do] DOI:10.1210/en.2017-00594


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[PMID]:29227073
[Au] Autor:Uspenska KR; Gergalova GL; Lykhmus OY; Skok MV
[Ti] Título:The effect of amixin and agmatine on cytochrome C release from isolated mitochondria
[So] Source:Ukr Biochem J;88(1):5-10, 2016 Jan-Feb.
[Is] ISSN:2409-4943
[Cp] País de publicação:Ukraine
[La] Idioma:eng
[Ab] Resumo:Mitochondrial nicotinic acetylcholine receptors (nAChRs) control permeability transition pore formation and cytochrome c release in the presence of apoptogenic factors. This study demonstrates that pharmacological agents amixin and agmatine affect mitochondrial nAChR functioning: they slightly suppress cytochrome c release from mouse brain and liver mitochondria stimulated with apoptogenic dose of Са2+ and prevent the effect of α7 nAChR agonist PNU282987. We conclude that mitochondria may be one of therapeutic targets of amixin and agmatine.
[Mh] Termos MeSH primário: Agmatina/farmacologia
Indutores de Interferon/farmacologia
Mitocôndrias/efeitos dos fármacos
Tilorona/farmacologia
Receptor Nicotínico de Acetilcolina alfa7/metabolismo
[Mh] Termos MeSH secundário: Animais
Benzamidas/antagonistas & inibidores
Benzamidas/farmacologia
Encéfalo/efeitos dos fármacos
Compostos Bicíclicos com Pontes/antagonistas & inibidores
Compostos Bicíclicos com Pontes/farmacologia
Cálcio/farmacologia
Fracionamento Celular
Citocromos c/antagonistas & inibidores
Citocromos c/secreção
Fígado/efeitos dos fármacos
Fígado/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
Mitocôndrias/metabolismo
Agonistas Nicotínicos/farmacologia
Especificidade de Órgãos
Receptor Nicotínico de Acetilcolina alfa7/agonistas
Receptor Nicotínico de Acetilcolina alfa7/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzamides); 0 (Bridged Bicyclo Compounds); 0 (Interferon Inducers); 0 (Nicotinic Agonists); 0 (PNU-282987); 0 (alpha7 Nicotinic Acetylcholine Receptor); 70J407ZL5Q (Agmatine); 9007-43-6 (Cytochromes c); O6W7VEW6KS (Tilorone); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE
[do] DOI:10.15407/ubj88.01.005


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[PMID]:29216268
[Au] Autor:Muñoz-Gutiérrez C; Cáceres-Rojas D; Adasme-Carreño F; Palomo I; Fuentes E; Caballero J
[Ad] Endereço:Centro de Bioinformática y Simulación Molecular (CBSM), Universidad de Talca, Talca, Chile.
[Ti] Título:Docking and quantitative structure-activity relationship of bi-cyclic heteroaromatic pyridazinone and pyrazolone derivatives as phosphodiesterase 3A (PDE3A) inhibitors.
[So] Source:PLoS One;12(12):e0189213, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PDE3s belong to the phosphodiesterases family, where the PDE3A isoform is the major subtype in platelets involved in the cAMP regulation pathway of platelet aggregation. PDE3A inhibitors have been designed as potential antiplatelet agents. In this work, a homology model of PDE3A was developed and used to obtain the binding modes of bicyclic heteroaromatic pyridazinones and pyrazolones. Most of the studied compounds adopted similar orientations within the PDE3A active site, establishing hydrogen bonds with catalytic amino acids. Besides, the structure-activity relationship of the studied inhibitors was described by using a field-based 3D-QSAR method. Different structure alignment strategies were employed, including template-based and docking-based alignments. Adequate correlation models were obtained according to internal and external validations. In general, QSAR models revealed that steric and hydrophobic fields describe the different inhibitory activities of the compounds, where the hydrogen bond donor and acceptor fields have minor contributions. It should be stressed that structural elements of PDE3A inhibitors are reported here, through descriptions of their binding interactions and their differential affinities. In this sense, the present results could be useful in the future design of more specific and potent PDE3A inhibitors that may be used for the treatment of cardiovascular diseases.
[Mh] Termos MeSH primário: Compostos Bicíclicos com Pontes/química
Compostos Bicíclicos com Pontes/farmacologia
Nucleotídeo Cíclico Fosfodiesterase do Tipo 3/efeitos dos fármacos
Inibidores da Fosfodiesterase 3/farmacologia
Pirazolonas/química
Pirazolonas/farmacologia
Piridonas/química
Piridonas/farmacologia
[Mh] Termos MeSH secundário: Simulação de Acoplamento Molecular
Relação Quantitativa Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); 0 (Phosphodiesterase 3 Inhibitors); 0 (Pyrazolones); 0 (Pyridones); EC 3.1.4.17 (Cyclic Nucleotide Phosphodiesterases, Type 3)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171226
[Lr] Data última revisão:
171226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0189213


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[PMID]:28843869
[Au] Autor:Naik R; Valentine H; Hall A; Mathews WB; Harris JC; Carter CS; Dannals RF; Wong DF; Horti AG
[Ad] Endereço:Department of Radiology, The Johns Hopkins University School of Medicine, Baltimore 21287, USA.
[Ti] Título:Development of a radioligand for imaging V vasopressin receptors with PET.
[So] Source:Eur J Med Chem;139:644-656, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of vasopressin receptor V ligands have been synthesized for positron emission tomography (PET) imaging. The lead compound (1S,5R)-1 ((4-(1H-indol-3-yl)-3-methoxyphenyl) ((1S,5R)-1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)methanone) and its F-ethyl analog 6c exhibited the best combination of high binding affinity and optimal lipophilicity within the series. (1S,5R)-1 was radiolabeled with C for PET studies. [ CH ](1S,5R)-1 readily entered the mouse (4.7% ID/g tissue) and prairie vole brains (∼2% ID/g tissue) and specifically (30-34%) labeled V receptor. The common animal anesthetic Propofol significantly blocked the brain uptake of [ CH ](1S,5R)-1 in the mouse brain, whereas anesthetics Ketamine and Saffan increased the uptake variability. Future PET imaging studies with V radiotracers in non-human primates should be performed in awake animals or using anesthetics that do not affect the V receptor.
[Mh] Termos MeSH primário: Compostos Bicíclicos com Pontes/farmacologia
Sondas Moleculares/farmacologia
Tomografia por Emissão de Pósitrons
Receptores de Vasopressinas/metabolismo
[Mh] Termos MeSH secundário: Animais
Compostos Bicíclicos com Pontes/síntese química
Compostos Bicíclicos com Pontes/química
Isótopos de Carbono
Relação Dose-Resposta a Droga
Ligantes
Camundongos
Sondas Moleculares/síntese química
Sondas Moleculares/química
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); 0 (Carbon Isotopes); 0 (Ligands); 0 (Molecular Probes); 0 (Receptors, Vasopressin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170828
[St] Status:MEDLINE


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[PMID]:28802219
[Au] Autor:Gaudette F; Hamadjida A; Bédard D; Nuara SG; Beaudry F; Huot P
[Ad] Endereço:CRCHUM, Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montreal, Quebec, Canada. Electronic address: fleur.gaudette.chum@ssss.gouv.qc.ca.
[Ti] Título:Development and validation of a high-performance liquid chromatography-tandem mass spectrometry method to quantify LY-354,740 in rat and marmoset plasma.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1061-1062:392-398, 2017 Sep 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:LY-354,740 (eglumegad) is a selective and potent agonist of the metabotropic glutamate group II receptors (mGluR2,3) that has already entered clinical trials as a potential anti-psychotic agent and therefore has well-documented pharmacokinetic (PK), safety and tolerability profiles in human. Whereas its development as an anti-psychotic agent has not been pursued, LY-354,740 may have potential in other neuroscience-related fields, notably anxiety and neuro-protection. The common marmoset is a small primate that has long been used in neuroscience. However, given its small size and small circulating blood volume, conducting PK studies to determine the therapeutic effectiveness of LY-354,740 at clinically-relevant doses is challenging. Here, we have developed and validated a simple, sensitive and selective analytical method that enables quantification of LY-354,740 using a small volume of plasma. The analytical method consisted of protein precipitation followed by high-performance liquid chromatography with heat assisted electrospray ionisation mass spectrometry (UHPLC-HESI-MS/MS). The chromatographic separation was achieved using gradient elution with a mobile phase consisting of acetonitrile and 10mM ammonium formate (pH 3) on a Thermo Scientific Acclaim Trinity P1 analytical column (100x3.0mm I.D., 3µm) operating at 45°C and at a flow rate of 900µl/min. The method displays a linear relationship ranging from 20.0 to 5000ng/ml. Intra- and inter-day relative standard deviations are less than 5.7% and 7.0%, respectively and the accuracy ranged from 91.0 to 106.0%. The UHPLC-HESI-MS/MS analytical method we describe here is simple, sensitive, specific and capable of quantifying LY-354,740 in both rat and marmoset plasma, and is suitable to conduct PK studies after a single sub-cutaneous dose of 1.0mg/kg or lower in both species.
[Mh] Termos MeSH primário: Compostos Bicíclicos com Pontes/sangue
Cromatografia Líquida de Alta Pressão/métodos
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Compostos Bicíclicos com Pontes/química
Compostos Bicíclicos com Pontes/farmacocinética
Callithrix
Estabilidade de Medicamentos
Limite de Detecção
Modelos Lineares
Ratos
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); ONU5A67T2S (eglumetad)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170813
[St] Status:MEDLINE


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[PMID]:28701654
[Au] Autor:Asakawa Y; Tomiyama K; Sakurai K; Kawakami Y; Yaguchi Y
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Tokushima Bunri University.
[Ti] Título:Volatile Compounds from the Different Organs of Houttuynia cordata and Litsea cubeba (L. citriodora).
[So] Source:J Oleo Sci;66(8):889-895, 2017 Aug 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The volatile compounds obtained from the different organs of Houttuynia cordata (Saururaceae) and Litsea cubeba (Lauraceae) were analyzed by Gas Chromatography/Mass Spectrometry (GC/MS), Headspace Solid Phase Micro Extraction-Gas Chromatography/Mass Spectrometry (HS-SPME-GC/MS), and GC/olfactometry (GC/O). The major component of all parts of H. cordata is assigned as 4-tridecanone. Each organ produces myrcene as the major monoterpenoid. The major monoterpene in the rhizomes and roots was ß-pinene instead of myrcene. 1-Decanal which was responsible for the unpleasant odor of this plant, was the predominant polyketide in both leaves and stems. The presence of 1-decanal was very poor in flowers, stem collected in summer, rhizomes, and roots. GC/MS analyses were very simple in case of the crude extracts of flowers. The content of sesquiterpenoids was extremely poor. (8Z)-Heptadecene, geranial, and neral were detected as the major components in Litsea cubeba. Odor-contributing components by GC/O analysis of the ether extract of the fresh flowers of L. cubeba were neral and geranial which played an important role in sweet-lemon fragrance of the flowers. The role of a high content of (8Z)-heptadecene was still unknown but it might play a significant role in the dispersion of the volatile monoterpene hydrocarbons and aldehydes. The flower volatiles of the Japanese L. cubeba were chemically quite different from those of the Chinese same species.
[Mh] Termos MeSH primário: Houttuynia/química
Litsea/química
Estruturas Vegetais
Compostos Orgânicos Voláteis/análise
[Mh] Termos MeSH secundário: Alcanos/análise
Alcenos/análise
Compostos Bicíclicos com Pontes/análise
Álcoois Graxos/análise
Cromatografia Gasosa-Espectrometria de Massas/métodos
Litsea/anatomia & histologia
Monoterpenos/análise
Olfatometria
Policetídeos/análise
Sesquiterpenos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkanes); 0 (Alkenes); 0 (Bridged Bicyclo Compounds); 0 (Fatty Alcohols); 0 (Monoterpenes); 0 (Polyketides); 0 (Sesquiterpenes); 0 (Volatile Organic Compounds); 3M39CZS25B (myrcene); 4MS8VHZ1HJ (beta-pinene); 89V4LX791F (n-decyl alcohol); A3LZF0L939 (tridecane); H7C0J39XUM (heptadecane); T7EU0O9VPP (citral)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170714
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17049


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[PMID]:28609696
[Au] Autor:Wang M; Gu D; Li H; Wang Q; Kang J; Chu T; Guo H; Yang Y; Tian J
[Ad] Endereço:School of Biological Engineering, Dalian Polytechnic University, Dalian 116034, China.
[Ti] Título:Rapid prediction and identification of lipase inhibitors in volatile oil from Pinus massoniana L. needles.
[So] Source:Phytochemistry;141:114-120, 2017 Sep.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A facile method based on gas chromatography-mass spectrometry (GC-MS) and molecular docking was established to analyze, identify, and predict lipase inhibitors in volatile oil from Pinus massoniana L. needles (PMLN). The volatile oil, with an IC value of 15.25 ± 0.06 µg/mL, exhibited potential inhibitory activity against lipase in vitro. In total, 33 compounds were identified from the volatile oil through GC-MS analysis. The major compounds in the volatile oil were ß-pinene (39.24%), α-pinene (14.68%), germacrene D (9.08%), caryophyllene (6.94%), α-terpineol (5.39%), ß-phellandrene (4.82%), and D-limonene (3.93%). The identified compounds were individually docked with lipase as the target through molecular docking. Among the compounds, longifolene characterized by preferable binding energy and the good inhibition constant exhibited potential lipase inhibitory activity. The IC value of longifolene was 25.10 ± 0.49 µM, indicating that this compound is the active ingredient responsible for the lipase inhibitory activity of PMLN volatile oil.
[Mh] Termos MeSH primário: Lipase/antagonistas & inibidores
Óleos Voláteis/química
Pinus/química
Óleos Vegetais/química
Sesquiterpenos/química
[Mh] Termos MeSH secundário: Compostos Bicíclicos com Pontes/química
Compostos Bicíclicos com Pontes/isolamento & purificação
Cicloexenos/química
Cicloexenos/isolamento & purificação
Inibidores Enzimáticos/química
Inibidores Enzimáticos/isolamento & purificação
Cromatografia Gasosa-Espectrometria de Massas
Simulação de Acoplamento Molecular
Monoterpenos/química
Monoterpenos/isolamento & purificação
Folhas de Planta/química
Sesquiterpenos/isolamento & purificação
Sesquiterpenos de Germacrano/química
Sesquiterpenos de Germacrano/isolamento & purificação
Terpenos/química
Terpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); 0 (Cyclohexenes); 0 (Enzyme Inhibitors); 0 (Monoterpenes); 0 (Oils, Volatile); 0 (Plant Oils); 0 (Sesquiterpenes); 0 (Sesquiterpenes, Germacrane); 0 (Terpenes); 21334LVV8W (alpha-terpineol); 2KK225M001 (beta-phellandrene); 3YXH7YY8WM (longifolene); 4MS8VHZ1HJ (beta-pinene); 9MC3I34447 (limonene); BHW853AU9H (caryophyllene); EC 3.1.1.3 (Lipase); JPF3YI7O34 (alpha-pinene); V2I9ATG34E (germacrene D)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170721
[Lr] Data última revisão:
170721
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE


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[PMID]:28606623
[Au] Autor:Donvito G; Bagdas D; Toma W; Rahimpour E; Jackson A; Meade JA; AlSharari S; Kulkarni AR; Ivy Carroll F; Lichtman AH; Papke RL; Thakur GA; Imad Damaj M
[Ad] Endereço:Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, VA, USA. Electronic address: giulia.donvito@vcuhealth.org.
[Ti] Título:The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.
[So] Source:Exp Neurol;295:194-201, 2017 Sep.
[Is] ISSN:1090-2430
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recently, α7 nicotinic acetylcholine receptors (nAChRs), primarily activated by binding of orthosteric agonists, represent a target for anti-inflammatory and analgesic drug development. These receptors may also be modulated by positive allosteric modulators (PAMs), ago-allosteric ligands (ago-PAMs), and α7-silent agonists. Activation of α7 nAChRs has been reported to increase the brain levels of endogenous ligands for nuclear peroxisome proliferator-activated receptors type-α (PPAR-α), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), in a Ca -dependent manner. Here, we investigated potential crosstalk between α7 nAChR and PPAR-α, using the formalin test, a mouse model of tonic pain. Using pharmacological and genetic approaches, we found that PNU282987, a full α7 agonist, attenuated formalin-induced nociceptive behavior in α7-dependent manner. Interestingly, the selective PPAR-α antagonist GW6471 blocked the antinociceptive effects of PNU282987, but did not alter the antinociceptive responses evoked by the α7 nAChR PAM PNU120596, ago-PAM GAT107, and silent agonist NS6740. Moreover, GW6471 administered systemically or spinally, but not via the intraplantar surface of the formalin-injected paw blocked PNU282987-induced antinociception. Conversely, exogenous administration of the naturally occurring PPAR-α agonist PEA potentiated the antinociceptive effects of PNU282987. In contrast, the cannabinoid CB antagonist rimonabant and the CB antagonist SR144528 failed to reverse the antinociceptive effects of PNU282987. These findings suggest that PPAR-α plays a key role in a putative antinociceptive α7 nicotinic signaling pathway.
[Mh] Termos MeSH primário: Nociceptividade/efeitos dos fármacos
PPAR alfa/efeitos dos fármacos
Transdução de Sinais/efeitos dos fármacos
Receptor Nicotínico de Acetilcolina alfa7/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Compostos Azabicíclicos/farmacologia
Benzamidas/farmacologia
Compostos Bicíclicos com Pontes/farmacologia
Antagonistas de Receptores de Canabinoides/farmacologia
Etanolaminas/farmacologia
Furanos/farmacologia
Masculino
Camundongos
Camundongos Endogâmicos ICR
Antagonistas Nicotínicos/farmacologia
Oxazóis/farmacologia
PPAR alfa/antagonistas & inibidores
Medição da Dor/efeitos dos fármacos
Ácidos Palmíticos/farmacologia
Receptor Cross-Talk
Tirosina/análogos & derivados
Tirosina/farmacologia
Receptor Nicotínico de Acetilcolina alfa7/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,4-diazabicyclo(3.2.2)nonan-4-yl(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone); 0 (Azabicyclo Compounds); 0 (Benzamides); 0 (Bridged Bicyclo Compounds); 0 (Cannabinoid Receptor Antagonists); 0 (Ethanolamines); 0 (Furans); 0 (GW 6471); 0 (Nicotinic Antagonists); 0 (Oxazoles); 0 (PNU-282987); 0 (PPAR alpha); 0 (Palmitic Acids); 0 (alpha7 Nicotinic Acetylcholine Receptor); 42HK56048U (Tyrosine); 6R8T1UDM3V (palmidrol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE


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[PMID]:28531857
[Au] Autor:Young B; Delatolla R; Kennedy K; LaFlamme E; Stintzi A
[Ad] Endereço:Department of Civil Engineering, Faculty of Engineering, University of Ottawa, Ottawa, Canada.
[Ti] Título:Post carbon removal nitrifying MBBR operation at high loading and exposure to starvation conditions.
[So] Source:Bioresour Technol;239:318-325, 2017 Sep.
[Is] ISSN:1873-2976
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study investigates the performance of MBBR nitrifying biofilm post carbon removal at high loading and starvation conditions. The nitrifying MBBR, treating carbon removal lagoon effluent, achieved a maximum SARR of 2.13gN/m d with complete conversion of ammonia to nitrate. The results also show the MBBR technology is capable of maintaining a stable biofilm under starvation conditions in systems that nitrify intermittently. The biomass exhibited a higher live fraction of total cells in the high loaded reactors (73-100%) as compared to the reactors operated in starvation condition (26-82%). For both the high loaded and starvation condition, the microbial communities significantly changed with time of operation. The nitrifying community, however, remained steady with the family Nitrosomonadacea as the primary AOBs and Nitrospira as the primary NOB. During starvation conditions, the relative abundance of AOBs decreased and Nitrospira increased corresponding to an NOB/AOB ratio of 5.2-12.1.
[Mh] Termos MeSH primário: Biofilmes
Reatores Biológicos
[Mh] Termos MeSH secundário: Amônia
Compostos Bicíclicos com Pontes
Carbono
Nitrificação
Nitritos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds); 0 (Nitrites); 7440-44-0 (Carbon); 7664-41-7 (Ammonia); V23UK0CYXL (monobromobimane)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170523
[St] Status:MEDLINE



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