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[PMID]:28083689
[Au] Autor:Chen Q; Zhang Y; Hou H; Du F; Wu S; Chen L; Shen Y; Chao F; Chung JK; Zhang H; Tian M
[Ad] Endereço:Department of Psychiatry, The Second Affiliated Hospital of Zhejiang University School of Medicine, Hangzhou, China.
[Ti] Título:Neural correlates of the popular music phenomenon: evidence from functional MRI and PET imaging.
[So] Source:Eur J Nucl Med Mol Imaging;44(6):1033-1041, 2017 Jun.
[Is] ISSN:1619-7089
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Music can induce different emotions. However, its neural mechanism remains unknown. The aim of this study was to use functional magnetic resonance imaging (fMRI) and position emission tomography (PET) imaging for mapping of neural changes under the most popular music in healthy volunteers. METHODS: Blood-oxygen-level-dependent (BOLD) fMRI and monoamine receptor PET imaging with C-N-methylspiperone ( C-NMSP) were conducted under the popular music Gangnam Style and light music A Comme Amour in healthy subjects. PET and fMRI images were analyzed by using the Statistical Parametric Mapping software (SPM). RESULTS: Significantly increased fMRI BOLD signals were found in the bilateral superior temporal cortices, left cerebellum, left putamen and right thalamus cortex. Monoamine receptor availability was increased significantly in the left superior temporal gyrus and left putamen, but decreased in the bilateral superior occipital cortices under the Gangnam Style compared with the light music condition. Significant positive correlation was found between C-NMSP binding and fMRI BOLD signals in the left temporal cortex. Furthermore, increased C-NMSP binding in the left putamen was positively correlated with the mood arousal level score under the Gangnam Style condition. CONCLUSION: Popular music Gangnam Style can arouse pleasure experience and strong emotional response. The left putamen is positively correlated with the mood arousal level score under the Gangnam Style condition. Our results revealed characteristic patterns of brain activity associated with Gangnam Style, and may also provide more general insights into the music-induced emotional processing.
[Mh] Termos MeSH primário: Mapeamento Encefálico
Imagem por Ressonância Magnética
Imagem Multimodal
Música
Tomografia Computadorizada por Raios X
[Mh] Termos MeSH secundário: Adulto
Radioisótopos de Carbono
Emoções
Voluntários Saudáveis
Seres Humanos
Masculino
Espiperona/análogos & derivados
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbon Radioisotopes); 4X6E73CJ0Q (Spiperone); 87539-19-3 (3-N-methylspiperone)
[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:170114
[St] Status:MEDLINE
[do] DOI:10.1007/s00259-017-3614-7


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[PMID]:27265677
[Au] Autor:Borhani K; Mohabati Mobarez A; Khabiri AR; Behmanesh M; Khoramabadi N
[Ad] Endereço:Department of Bacteriology, Faculty of Medical Sciences, Tarbiat Modares University, Tehran, Iran.
[Ti] Título:Inhibitory effects of rHP-NAP IgY against Helicobacter pylori attachment to AGS cell line.
[So] Source:Microb Pathog;97:231-5, 2016 Aug.
[Is] ISSN:1096-1208
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Helicobacter pylori is a major human pathogen related to gastric adenocarcinoma and gastroduodenal diseases. Treatment of H. pylori infections is complicated by the rise of antibiotic resistance, necessitating investigation of alternative therapies. One such alternative is passive immunization by oral administration of antibacterial immunoglobulin. In the present study, chicken immunoglobulin (IgY) was used for passive immunotherapy against a major virulence factor of H. pylori, namely recombinant HP-Nap protein. Recombinant HP-Nap was prepared and used to immunize hens. IgY was purified from the eggs by polyethylene glycol precipitation method with a total IgY-HP-NAP yield of 30 mg per egg. The inhibitory effect of specific IgY on H. pylori attachment was investigated in AGS cell line infected by the bacteria. The results demonstrate the potent effect of IgY- HP-NAP in inhibition of H. pylori attachment to the AGS cells.
[Mh] Termos MeSH primário: Aderência Bacteriana/efeitos dos fármacos
Células Epiteliais/microbiologia
Helicobacter pylori/efeitos dos fármacos
Helicobacter pylori/imunologia
Imunoglobulinas/metabolismo
Fatores Imunológicos/metabolismo
Fatores de Virulência/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Galinhas
Seres Humanos
Imunoglobulinas/isolamento & purificação
Fatores Imunológicos/isolamento & purificação
Espiperona/análogos & derivados
Fatores de Virulência/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (IgY); 0 (Immunoglobulins); 0 (Immunologic Factors); 0 (Virulence Factors); 4X6E73CJ0Q (Spiperone); 93801-18-4 (N-(4-aminophenethyl)spiroperidol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170327
[Lr] Data última revisão:
170327
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160607
[St] Status:MEDLINE


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[PMID]:27193322
[Au] Autor:Liu X; Grove JC; Hirano AA; Brecha NC; Barnes S
[Ad] Endereço:Biomaterials and Live Cell Imaging Institute, Chongqing University of Science and Technology, Chongqing, People's Republic of China; Department of Neurobiology and Jules Stein Eye Institute, David Geffen School of Medicine, University of California, Los Angeles, California;
[Ti] Título:Dopamine D1 receptor modulation of calcium channel currents in horizontal cells of mouse retina.
[So] Source:J Neurophysiol;116(2):686-97, 2016 Aug 01.
[Is] ISSN:1522-1598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Horizontal cells form the first laterally interacting network of inhibitory interneurons in the retina. Dopamine released onto horizontal cells under photic and circadian control modulates horizontal cell function. Using isolated, identified horizontal cells from a connexin-57-iCre × ROSA26-tdTomato transgenic mouse line, we investigated dopaminergic modulation of calcium channel currents (ICa) with whole cell patch-clamp techniques. Dopamine (10 µM) blocked 27% of steady-state ICa, an action blunted to 9% in the presence of the L-type Ca channel blocker verapamil (50 µM). The dopamine type 1 receptor (D1R) agonist SKF38393 (20 µM) inhibited ICa by 24%. The D1R antagonist SCH23390 (20 µM) reduced dopamine and SKF38393 inhibition. Dopamine slowed ICa activation, blocking ICa by 38% early in a voltage step. Enhanced early inhibition of ICa was eliminated by applying voltage prepulses to +120 mV for 100 ms, increasing ICa by 31% and 11% for early and steady-state currents, respectively. Voltage-dependent facilitation of ICa and block of dopamine inhibition after preincubation with a Gßγ-blocking peptide suggested involvement of Gßγ proteins in the D1R-mediated modulation. When the G protein activator guanosine 5'-O-(3-thiotriphosphate) (GTPγS) was added intracellularly, ICa was smaller and showed the same slowed kinetics seen during D1R activation. With GTPγS in the pipette, additional block of ICa by dopamine was only 6%. Strong depolarizing voltage prepulses restored the GTPγS-reduced early ICa amplitude by 36% and steady-state ICa amplitude by 3%. These results suggest that dopaminergic inhibition of ICa via D1Rs is primarily mediated through the action of Gßγ proteins in horizontal cells.
[Mh] Termos MeSH primário: Canais de Cálcio/fisiologia
Potenciais da Membrana/fisiologia
Receptores de Dopamina D1/metabolismo
Células Horizontais da Retina/fisiologia
[Mh] Termos MeSH secundário: 2,3,4,5-Tetra-Hidro-7,8-Di-Hidroxi-1-Fenil-1H-3-Benzazepina/farmacologia
Animais
Fenômenos Biofísicos/efeitos dos fármacos
Fenômenos Biofísicos/genética
Cálcio/metabolismo
Bloqueadores dos Canais de Cálcio/farmacologia
Conexinas/genética
Conexinas/metabolismo
Dopamina/farmacologia
Agonistas de Dopamina/farmacologia
Antagonistas de Dopamina/farmacologia
Potenciais da Membrana/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Lectinas de Plantas/genética
Lectinas de Plantas/metabolismo
RNA não Traduzido/genética
RNA não Traduzido/metabolismo
Retina/citologia
Células Horizontais da Retina/efeitos dos fármacos
Espiperona/farmacologia
ômega-Conotoxina GVIA/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Calcium Channels); 0 (Connexins); 0 (Dopamine Agonists); 0 (Dopamine Antagonists); 0 (Gja10 protein, mouse); 0 (Gt(ROSA)26Sor non-coding RNA, mouse); 0 (Plant Lectins); 0 (RNA, Untranslated); 0 (Receptors, Dopamine D1); 0 (tomato lectin); 4X6E73CJ0Q (Spiperone); 67287-49-4 (2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine); 92078-76-7 (omega-Conotoxin GVIA); SY7Q814VUP (Calcium); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170907
[Lr] Data última revisão:
170907
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160520
[St] Status:MEDLINE
[do] DOI:10.1152/jn.00990.2015


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[PMID]:26601885
[Au] Autor:Robert B; Perrin MA; Coquerel G; Céolin R; Rietveld IB
[Ad] Endereço:EA 3233, crystal genesis unit, IMR 4114, UR, laboratoire SMS, Normandie université, 76821 Mont-Saint-Aignan cedex, France; Sanofi R&D, lead generation & compound realization/analytical sciences/solid state group, 13, quai Jules-Guesde, 94400 Vitry-sur-Seine, France.
[Ti] Título:The topological pressure-temperature phase diagram and crystal structures of the dimorphic system spiperone.
[So] Source:Ann Pharm Fr;74(2):129-36, 2016 Mar.
[Is] ISSN:0003-4509
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The topological pressure-temperature phase diagram for the dimorphism of spiperone, a potent neuroleptic drug, has been constructed using literature data and improved crystal structures obtained with new crystallographic data from single-crystal X-ray diffraction at various temperatures. It is inferred that form II, which is the more dense form and exhibits the lower melting temperature, becomes the more stable phase under pressure. Under ambient conditions, form I is more stable.
[Mh] Termos MeSH primário: Antipsicóticos/química
Espiperona/química
[Mh] Termos MeSH secundário: Cristalização
Modelos Moleculares
Temperatura Ambiente
Termodinâmica
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 4X6E73CJ0Q (Spiperone)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170209
[Lr] Data última revisão:
170209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151126
[St] Status:MEDLINE


  5 / 2805 MEDLINE  
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[PMID]:25927611
[Au] Autor:Skurikhin EG; Pershina OV; Reztsova AM; Ermakova NN; Khmelevskaya ES; Krupin VA; Stepanova IE; Artamonov AV; Bekarev AA; Madonov PG; Dygai AM
[Ad] Endereço:Department of Pathophysiology and Regenerative Medicine, Research Institute of Pharmacology and Regenerative Medicine named after E.D. Goldberg, Tomsk, Russia.
[Ti] Título:Modulation of bleomycin-induced lung fibrosis by pegylated hyaluronidase and dopamine receptor antagonist in mice.
[So] Source:PLoS One;10(4):e0125065, 2015.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Hyaluronidases are groups of enzymes that degrade hyaluronic acid (HA). To stop enzymatic hydrolysis we modified testicular hyaluronidase (HYAL) by activated polyethylene oxide with the help of electron-beam synthesis. As a result we received pegylated hyaluronidase (pegHYAL). Spiperone is a selective D2 dopamine receptor antagonist. It was demonstrated on the model of a single bleomycin damage of alveolar epithelium that during the inflammatory phase monotherapy by pegHYAL or spiperone reduced the populations of hematopoietic stem /progenitor cells in the lung parenchyma. PegHYAL also reduced the levels of transforming growth factor (TGF)-ß, interleukin (IL)-1ß, tumor necrosis factor (TNF)-α in the serum and lungs, while spiperone reduced the level of the serum IL-1ß. Polytherapy by spiperone and pegHYAL caused the increase of the quantity of hematopoietic stem/ progenitor cells in the lungs. Such an influx of blood cell precursors was observed on the background of considerable fall level of TGF-ß and the increase level of TNF-α in the serum and lungs. These results show pegHYAL reduced the bleomycin-induced fibrosis reaction (production and accumulation of collagen) in the lung parenchyma. This effect was observed at a single and repetitive bleomycin damage of alveolar epithelium, the antifibrotic activity of pegHYAL surpassing the activity of testicular HYAL. The antifibrotic effect of pegHYAL is enhanced by an additional instillation of spiperone. Therapy by pegHYAL causes the flow of CD31‒ CD34‒ CD45‒ CD44+ CD73+ CD90+ CD106+-cells into the fibrous lungs. These cells are incapable of differentiating into fibroblast cells. Spiperone instillation separately or together with pegHYAL reduced the MSC-like cells considerably. These data enable us to assume, that pegHYAL is a new and promising instrument both for preventive and therapy of toxic pneumofibrosis. The blockage of D2 dopamine receptors with the following change of hyaluronan matrix can be considered as a new strategy in treatment of pneumofibrosis.
[Mh] Termos MeSH primário: Bleomicina/toxicidade
Antagonistas de Dopamina/uso terapêutico
Hialuronoglucosaminidase/uso terapêutico
Fibrose Pulmonar/induzido quimicamente
Fibrose Pulmonar/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Ensaio de Imunoadsorção Enzimática
Citometria de Fluxo
Hialuronoglucosaminidase/química
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Espiperona/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dopamine Antagonists); 11056-06-7 (Bleomycin); 4X6E73CJ0Q (Spiperone); EC 3.2.1.35 (Hyaluronoglucosaminidase)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150501
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0125065


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[PMID]:25840364
[Au] Autor:Zhen J; Antonio T; Ali S; Neve KA; Dutta AK; Reith ME
[Ad] Endereço:Department of Psychiatry, New York University School of Medicine, New York, NY, USA. Electronic address: juan.zhen@nyumc.org.
[Ti] Título:Use of radiolabeled antagonist assays for assessing agonism at D2 and D3 dopamine receptors: comparison with functional GTPγS assays.
[So] Source:J Neurosci Methods;248:7-15, 2015 Jun 15.
[Is] ISSN:1872-678X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Cell-based drug screening assays are essential tools for drug discovery and development targeting G protein-coupled receptors, which include dopamine D3 receptors. D3 is notorious for its poor coupling to G protein in most heterologous cell lines, and therefore D3 agonist-stimulated binding of [(35)S]GTPγS to G protein cannot be observed in many "non-functional" D3 expressing cell lines. NEW METHOD: The present work explores the use of an alternate method for assessing agonist activity, consisting of measuring the difference in agonist competition between [(3)H]spiperone bound to low-affinity states of the receptor and that with radioligand bound to high-affinity states (GTP shift assay). COMPARISON WITH EXISTING METHOD: The current study describes the determination of GTP shifts in [(3)H]spiperone binding assays for the assessment of agonists' potencies (at D2 and D3) and efficacies (at D3). Compared with GTPγ(35)S binding assays, the new method removes the cumbersome need of functional D3 cell lines and limited project duration due to short half-life of isotope (35)S. CONCLUSION: The new method allows the estimation of potency (D2 and D3) and efficacy (D3) at the level of receptor and G protein activation in a simple fashion from shifts in monophasic-inhibition curves. Moreover, it does not require [(35)S]GTPγS binding assays with functional D3 cells. This method will have wide applicability for D3-selective agonist screening. It may also be useful for other GPCRs circumventing the need for functional assays and offering the ability to detect agonist activity regardless of the particular signaling pathway.
[Mh] Termos MeSH primário: Agonistas de Dopamina/farmacologia
Avaliação Pré-Clínica de Medicamentos/métodos
Guanosina 5´-O-(3-Tiotrifosfato)/farmacologia
Receptores de Dopamina D2/agonistas
Receptores de Dopamina D3/agonistas
[Mh] Termos MeSH secundário: Animais
Células CHO
Cricetulus
Células HEK293
Seres Humanos
Receptores de Dopamina D2/genética
Receptores de Dopamina D3/genética
Espiperona/farmacologia
Radioisótopos de Enxofre
Transfecção
Trítio
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Dopamine Agonists); 0 (Receptors, Dopamine D2); 0 (Receptors, Dopamine D3); 0 (Sulfur Radioisotopes); 10028-17-8 (Tritium); 37589-80-3 (Guanosine 5'-O-(3-Thiotriphosphate)); 4X6E73CJ0Q (Spiperone)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150502
[Lr] Data última revisão:
150502
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150404
[St] Status:MEDLINE


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[PMID]:25371112
[Au] Autor:Jatana N; Thukral L; Latha N
[Ad] Endereço:Bioinformatics Infrastructure Facility, Sri Venkateswara College (University of Delhi), Benito Juarez Road, Dhaula Kuan, New Delhi, 110 021, India.
[Ti] Título:Structure and dynamics of DRD4 bound to an agonist and an antagonist using in silico approaches.
[So] Source:Proteins;83(5):867-80, 2015 May.
[Is] ISSN:1097-0134
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Human dopamine receptor D4 (DRD4), a member of G-protein coupled receptor (GPCR) family, plays a central role in cell signaling and trafficking. Dysfunctional activity of DRD4 can lead to several psychiatric conditions and, therefore, represents target for many neurological disorders. However, lack of atomic structure impairs our understanding of the mechanism regulating its activity. Here, we report the modeled structure of DRD4 alone and in complex with dopamine and spiperone, its natural agonist and antagonist, respectively. To assess the conformational dynamics induced upon ligand binding, all-atom explicit solvent molecular dynamics simulations in membrane environment were performed. Comprehensive analyses of simulations reveal that agonist binding triggers a series of conformational changes in the transmembrane region, including rearrangement of residues, characteristic of transmission and tyrosine toggle molecular switches. Further, the trajectories indicate that a loop region in the intracellular region--ICL3, is significantly dynamic in nature, mainly due to the side-chain movements of conserved proline residues involved in SH3 binding domains. Interestingly, in dopamine-bound receptor simulation, ICL3 represents an open conformation ideal for G protein binding. The structural and dynamical information presented here suggest a mode of activation of DRD4, upon ligand binding. Our study will help in further understanding of receptor activation, as acquiring structural information is crucial for the design of highly selective DRD4 ligands.
[Mh] Termos MeSH primário: Agonistas de Dopamina/química
Antagonistas de Dopamina/química
Receptores de Dopamina D4/química
[Mh] Termos MeSH secundário: Sítios de Ligação
Dopamina/química
Seres Humanos
Ligações de Hidrogênio
Simulação de Acoplamento Molecular
Simulação de Dinâmica Molecular
Ligação Proteica
Estrutura Secundária de Proteína
Estrutura Terciária de Proteína
Receptores de Dopamina D4/agonistas
Receptores de Dopamina D4/antagonistas & inibidores
Espiperona/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (DRD4 protein, human); 0 (Dopamine Agonists); 0 (Dopamine Antagonists); 137750-34-6 (Receptors, Dopamine D4); 4X6E73CJ0Q (Spiperone); VTD58H1Z2X (Dopamine)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:150415
[Lr] Data última revisão:
150415
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141106
[St] Status:MEDLINE
[do] DOI:10.1002/prot.24716


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[PMID]:24913578
[Au] Autor:Skurikhin EG; Khmelevskaya ES; Ermakova NN; Pershina OV; Reztsova AM; Krupin VA; Stepanova IE; Reztsova VM; Reikhart DV; Dygai AM
[Ad] Endereço:Research Institute of Pharmacology, Siberian Division of the Russian Academy of Medical Sciences, Tomsk, Russia.
[Ti] Título:Effect of spiperone on mesenchymal multipotent stromal and hemopoietic stem cells under conditions of pulmonary fibrosis.
[So] Source:Bull Exp Biol Med;157(1):132-7, 2014 May.
[Is] ISSN:1573-8221
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The antifibrotic properties of spiperone and its effect on stem and progenitor cells were studied on the model of reversible bleomycin-induced pulmonary fibrosis in C57Bl/6 mice. Spiperone reduced infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevented the growth of the connective tissue in the parenchyma of bleomycin lungs. Apart from anti-inflammatory effect, spiperone suppressed bone marrow hemopoietic cells (CD3, CD45R (B220), Ly6C, Ly6G (Gr1), CD11b (Mac1), TER-119)-, Sca-1+, c-Kit+, CD34- and progenitor hemopoietic cells (granulocyte-erythroid-macrophage-megakaryocytic and granulocyte CFU). Spiperone-induced disturbances of fi brogenesis were paralleled by restoration of endothelial cells in the lung parenchyma, reduction of the number of circulating bone marrow cells and lung mesenchymopoietic cells (mesenchymal multipotent stromal cells (CD31-, CD34-, CD45-, CD44+, CD73+, CD90+, CD106+) and progenitor fi broblast cells), and suppression of multilineage differentiation of multipotent mesenchymal stromal cells (including fi broblast-lineage cells).
[Mh] Termos MeSH primário: Antagonistas de Dopamina/farmacologia
Fibroblastos/efeitos dos fármacos
Células Mesenquimais Estromais/efeitos dos fármacos
Alvéolos Pulmonares/efeitos dos fármacos
Fibrose Pulmonar/tratamento farmacológico
Espiperona/farmacologia
[Mh] Termos MeSH secundário: Animais
Antígenos CD/metabolismo
Biomarcadores/metabolismo
Bleomicina
Células da Medula Óssea/citologia
Células da Medula Óssea/efeitos dos fármacos
Células da Medula Óssea/metabolismo
Linhagem da Célula/efeitos dos fármacos
Células Endoteliais/citologia
Células Endoteliais/efeitos dos fármacos
Células Endoteliais/metabolismo
Fibroblastos/metabolismo
Fibroblastos/patologia
Expressão Gênica
Granulócitos/citologia
Granulócitos/efeitos dos fármacos
Granulócitos/metabolismo
Células-Tronco Hematopoéticas/citologia
Células-Tronco Hematopoéticas/efeitos dos fármacos
Células-Tronco Hematopoéticas/metabolismo
Macrófagos/citologia
Macrófagos/efeitos dos fármacos
Macrófagos/metabolismo
Megacariócitos/citologia
Megacariócitos/efeitos dos fármacos
Megacariócitos/metabolismo
Células Mesenquimais Estromais/citologia
Células Mesenquimais Estromais/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
Infiltração de Neutrófilos/efeitos dos fármacos
Alvéolos Pulmonares/metabolismo
Alvéolos Pulmonares/patologia
Fibrose Pulmonar/induzido quimicamente
Fibrose Pulmonar/metabolismo
Fibrose Pulmonar/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, CD); 0 (Biomarkers); 0 (Dopamine Antagonists); 11056-06-7 (Bleomycin); 4X6E73CJ0Q (Spiperone)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140611
[St] Status:MEDLINE
[do] DOI:10.1007/s10517-014-2508-y


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[PMID]:24910074
[Au] Autor:Quelch DR; Withey SL; Nutt DJ; Tyacke RJ; Parker CA
[Ad] Endereço:Centre for Neuropsychopharmacology, Division of Brain Sciences, Imperial College London, UK. Electronic address: d.quelch09@imperial.ac.uk.
[Ti] Título:The influence of different cellular environments on PET radioligand binding: an application to D2/3-dopamine receptor imaging.
[So] Source:Neuropharmacology;85:305-13, 2014 Oct.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Various D2/3 receptor PET radioligands are sensitive to endogenous dopamine release in vivo. The Occupancy Model is generally used to interpret changes in binding observed in in vivo competition binding studies; an Internalisation Hypothesis may also contribute to these changes in signal. Extension of in vivo competition imaging to other receptor systems has been relatively unsuccessful. A greater understanding of the cellular processes underlying signal changes following endogenous neurotransmitter release may help translate this imaging paradigm to other receptor systems. To investigate the Internalisation Hypothesis we assessed the effects of different cellular environments, representative of those experienced by a receptor following agonist-induced internalisation, on the binding of three D2/3 PET ligands with previously reported sensitivities to endogenous dopamine in vivo, namely [3H]spiperone, [3H]raclopride and [3H]PhNO. Furthermore, we determined the contribution of each cellular compartment to total striatal binding for these D2/3 ligands. These studies suggest that sensitivity to endogenous dopamine release in vivo is related to a decrease in affinity in the endosomal environment compared with those found at the cell surface. In agreement with these findings we also demonstrate that ∼25% of total striatal binding for [3H]spiperone originates from sub-cellular, microsomal receptors, whereas for [3H]raclopride and [3H]PhNO, this fraction is lower, representing ∼14% and 17%, respectively. This pharmacological approach is fully translatable to other receptor systems. Assessment of affinity shifts in different cellular compartments may play a crucial role for understanding if a radioligand is sensitive to endogenous release in vivo, for not just the D2/3, but other receptor systems.
[Mh] Termos MeSH primário: Antagonistas dos Receptores de Dopamina D2/metabolismo
Compostos Radiofarmacêuticos/metabolismo
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Animais
Membrana Celular/efeitos dos fármacos
Membrana Celular/metabolismo
Corpo Estriado/efeitos dos fármacos
Corpo Estriado/metabolismo
Antagonistas dos Receptores de Dopamina D2/farmacologia
Endossomos/efeitos dos fármacos
Endossomos/metabolismo
Espaço Extracelular/efeitos dos fármacos
Cinética
Masculino
Tomografia por Emissão de Pósitrons
Racloprida/metabolismo
Racloprida/farmacologia
Ensaio Radioligante
Compostos Radiofarmacêuticos/farmacologia
Ratos Sprague-Dawley
Receptores de Dopamina D3/metabolismo
Espiperona/metabolismo
Espiperona/farmacologia
Frações Subcelulares/efeitos dos fármacos
Frações Subcelulares/metabolismo
Trítio/metabolismo
Trítio/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Dopamine D2 Receptor Antagonists); 0 (Radiopharmaceuticals); 0 (Receptors, Dopamine D2); 0 (Receptors, Dopamine D3); 10028-17-8 (Tritium); 430K3SOZ7G (Raclopride); 4X6E73CJ0Q (Spiperone)
[Em] Mês de entrada:1503
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140610
[St] Status:MEDLINE


  10 / 2805 MEDLINE  
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[PMID]:24520350
[Au] Autor:Black KJ; Snyder AZ; Mink JW; Tolia VN; Revilla FJ; Moerlein SM; Perlmutter JS
[Ad] Endereço:Department of Psychiatry, Washington University School of Medicine, St. Louis, Missouri, United States of America ; Department of Neurology, Washington University School of Medicine, St. Louis, Missouri, United States of America ; Department of Radiology, Washington University School of Medicine, St
[Ti] Título:Spatial reorganization of putaminal dopamine D2-like receptors in cranial and hand dystonia.
[So] Source:PLoS One;9(2):e88121, 2014.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The putamen has a somatotopic organization of neurons identified by correspondence of firing rates with selected body part movements, as well as by complex, but organized, differential cortical projections onto putamen. In isolated focal dystonia, whole putaminal binding of dopamine D2-like receptor radioligands is quantitatively decreased, but it has not been known whether selected parts of the putamen are differentially affected depending upon the body part affected by dystonia. The radioligand [(18)F]spiperone binds predominantly to D2-like receptors in striatum. We hypothesized that the spatial location of [(18)F]spiperone binding within the putamen would differ in patients with dystonia limited to the hand versus the face, and we tested that hypothesis using positron emission tomography and magnetic resonance imaging. To address statistical and methodological concerns, we chose a straightforward but robust image analysis method. An automated algorithm located the peak location of [(18)F]spiperone binding within the striatum, relative to a brain atlas, in each of 14 patients with cranial dystonia and 8 patients with hand dystonia. The mean (left and right) |x|, y, and z coordinates of peak striatal binding for each patient were compared between groups by t test. The location of peak [(18)F]spiperone binding within the putamen differed significantly between groups (cranial dystonia z
[Mh] Termos MeSH primário: Distonia/metabolismo
Mãos/patologia
Receptores de Dopamina D2/metabolismo
Crânio/metabolismo
[Mh] Termos MeSH secundário: Adulto
Idoso
Distonia/diagnóstico por imagem
Distonia/patologia
Feminino
Radioisótopos de Flúor
Mãos/diagnóstico por imagem
Seres Humanos
Imagem por Ressonância Magnética
Masculino
Meia-Idade
Tomografia por Emissão de Pósitrons
Putamen/diagnóstico por imagem
Putamen/metabolismo
Putamen/patologia
Crânio/diagnóstico por imagem
Crânio/patologia
Espiperona
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Fluorine Radioisotopes); 0 (Receptors, Dopamine D2); 4X6E73CJ0Q (Spiperone)
[Em] Mês de entrada:1410
[Cu] Atualização por classe:170304
[Lr] Data última revisão:
170304
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140213
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0088121



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