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[PMID]:28450244
[Au] Autor:El-Naggar AWM; Senna MM; Mostafa TA; Helal RH
[Ad] Endereço:Radiation Chemistry Department, National Center for Radiation Research and Technology, Nasr City, Atomic Energy Authority, Cairo, Egypt. Electronic address: ab_nagga@yahoo.com.
[Ti] Título:Radiation synthesis and drug delivery properties of interpenetrating networks (IPNs) based on poly(vinyl alcohol)/ methylcellulose blend hydrogels.
[So] Source:Int J Biol Macromol;102:1045-1051, 2017 Sep.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Gamma radiation was used to prepare blend hydrogels from poly(vinyl alcohol) (PVA) and low ratios of methylcellulose (MC). The structure-property behavior was characterized by IR spectroscopy, gel fraction, differential scanning calorimetry (DSC) and swelling at room temperature and different pH values. The PVA/MC hydrogels were used as a carrier for doxycycline hyclate (DOX-h) drug. The results showed that the gel fraction of PVA/MC hydrogels decreased greatly with increasing the ratio of MC in the initial feeding solution. The PVA/MC hydrogels displayed pH-sensitive swelling character. The drug uptake-release study indicated that PVA/MC hydrogels possessed controlled release behavior and that the release process depends on pH. In this respect, the release of DOX-h drug was significant in alkaline medium.
[Mh] Termos MeSH primário: Portadores de Fármacos/química
Portadores de Fármacos/síntese química
Hidrogéis/química
Hidrogéis/síntese química
Metilcelulose/química
Álcool de Polivinil/química
[Mh] Termos MeSH secundário: Técnicas de Química Sintética
Doxiciclina/química
Liberação Controlada de Fármacos
Raios gama
Concentração de Íons de Hidrogênio
Radioquímica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Hydrogels); 9002-89-5 (Polyvinyl Alcohol); 9004-67-5 (Methylcellulose); N12000U13O (Doxycycline)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE


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[PMID]:28456080
[Au] Autor:Tang C; Nie D; Tang G; Gao S; Liu S; Wen F; Tang X
[Ad] Endereço:Guangdong Engineering Research Center for Medical Radiopharmaceuticals Translational Application PET-CT Center and Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080, China; Department of Nuclear Medicine, The Fifth Affiliated Hospital, Sun Yat-Se
[Ti] Título:Radiosynthesis and biological evaluation of N-(2-[ F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine as a PET tracer for oncologic imaging.
[So] Source:Nucl Med Biol;50:39-46, 2017 Jul.
[Is] ISSN:1872-9614
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Several C and F labeled 3,4-dihydroxy-l-phenylalanine (l-DOPA) analogues have been used for neurologic and oncologic diseases, especially for brain tumors and neuroendocrine tumors PET imaging. However, F-labeled N-substituted l-DOPA analogues have not been reported so far. In the current study, radiosynthesis and biological evaluation of a new F-labeled l-DOPA analogue, N-(2-[ F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine ([ F]FPDOPA) for tumor PET imaging are performed. METHODS: The synthesis of [ F]FPDOPA was via a two-step reaction sequence from 4-nitrophenyl-2-[ F]fluoropropionate ([ F]NFP). The biodistribution of [ F]FPDOPA was determined in normal Kunming mice. In vitro competitive inhibition and protein incorporation experiments were performed with SPC-A-1 lung adenocarcinoma cell lines. PET/CT studies of [ F]FPDOPA were conducted in C6 rat glioma and SPC-A-1 human lung adenocarcinoma and H460 human large cell lung cancer-bearing nude mice. RESULTS: [ F]FPDOPA was prepared with a decay-corrected radiochemical yield of 28±5% and a specific activity of 50±15GBq/µmol (n=10) within 125min. In vitro cell experiments showed that [ F]FPDOPA uptake in SPC-A-1 cells was primarily transported through Na -independent system L, with Na -dependent system B and system ASC partly involved in it. Biodistribution data in mice showed that renal-bladder route was the main excretory system of [ F]FPDOPA. PET imaging demonstrated intense accumulation of [ F]FPDOPA in several tumor xenografts, with (8.50±0.40)%ID/g in C6 glioma, (6.30±0.12)%ID/g in SPC-A-1 lung adenocarcinoma, and (6.50±0.10)%ID/g in H460 large cell lung cancer, respectively. CONCLUSION: A novel N-substituted F-labeled L-DOPA analogue [ F]FPDOPA is synthesized and evaluated in vitro and in vivo. The results support that [ F]FPDOPA seems to be a potential PET tracer for tumor imaging, especially be a better potential PET tracer than [ F]fluoro-2-deoxy-d-glucose ([ F]FDG) for brain tumor imaging.
[Mh] Termos MeSH primário: Neoplasias/diagnóstico por imagem
Fenilalanina/análogos & derivados
Fenilalanina/síntese química
Fenilalanina/farmacocinética
Tomografia por Emissão de Pósitrons
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Técnicas de Química Sintética
Estabilidade de Medicamentos
Seres Humanos
Camundongos
Neoplasias/metabolismo
Fenilalanina/química
Traçadores Radioativos
Radioquímica
Ratos
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Radioactive Tracers); 47E5O17Y3R (Phenylalanine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180126
[Lr] Data última revisão:
180126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170430
[St] Status:MEDLINE


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[PMID]:28961587
[Au] Autor:Tian C; Guo H; Lv N; Xu P; Lv W
[Ad] Endereço:*Xi'an Research Institute of Hi-Tech, Xi'an 710025, China.
[Ti] Título:Analysis on Enrichment and Mass of Uranium Materials With Time-Correlated Measurement.
[So] Source:Health Phys;113(5):387-391, 2017 Nov.
[Is] ISSN:1538-5159
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Effective determination for enrichment of the uranium materials in heavy shielding is technically difficult to solve. Various technical methods so far have been proposed to deal with this problem. With the time-correlated coincidence measurement method, 14 MeV neutrons and fission spectrum neutrons are chosen to interrogate the uranium samples with different masses and enrichments. The fission spectrum neutrons are obtained by slowing down the 14 MeV neutrons. Results have shown that a good linear relationship exists between masses of the uranium materials (≤10% enriched U) that possess the same enrichment. A linear relationship also exists between enrichments of the uranium materials that possess the same mass.
[Mh] Termos MeSH primário: Urânio/química
[Mh] Termos MeSH secundário: Deutério/química
Nêutrons
Radioquímica
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
4OC371KSTK (Uranium); AR09D82C7G (Deuterium)
[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:170930
[St] Status:MEDLINE
[do] DOI:10.1097/HP.0000000000000715


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[PMID]:28961584
[Au] Autor:Misdaq MA; Elouardi B; Ouguidi J
[Ad] Endereço:*Nuclear Physics and Techniques Laboratory, Faculty of Sciences Semlalia, BP.2390, University of Cadi Ayyad, Marrakech, Morocco (URAC-15 Research Unit Associated to the CNRST, Rabat, Morocco).
[Ti] Título:222Rn, 220Rn and Their Progenies Measured in the Air of Different Dwellings and Workplaces and Resulting Alpha Radiation Doses to the Eyes of Individuals.
[So] Source:Health Phys;113(5):363-374, 2017 Nov.
[Is] ISSN:1538-5159
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In order to assess radiation doses to the eyes of individuals, concentrations of Rn, Rn and their decay products were measured in different dwelling rooms, café rooms and vehicle repair shops by using two different types of solid state nuclear track detectors (SSNTDs). The influence of building materials, pollution and ventilation rate on radon and thoron alpha-activities inside the studied locations has been investigated. A new dosimetric model was developed for evaluating radiation doses to the eyes of individuals due to alpha particles emitted by the radon and thoron series in the air of the studied dwelling rooms, café rooms, and vehicle repair shops. The influence of the radon and thoron activities in the air of the studied locations, as well as exposure time on committed equivalent dose to the eyes of individuals, was investigated. A maximum value of the committed equivalent dose to the eyes of individuals due to alpha particles emitted by the radon and thoron series was found equal to 0.1 mSv y cm. Committed equivalent dose to the eyes of individuals due to the diffusion of the Rn and Rn gases present in ambient air of the studied locations has been evaluated.
[Mh] Termos MeSH primário: Partículas alfa
Olho/efeitos da radiação
Habitação
Exposição Ocupacional/análise
Radônio/análise
Radônio/química
Local de Trabalho
[Mh] Termos MeSH secundário: Poluição do Ar em Ambientes Fechados/análise
Difusão
Seres Humanos
Radioquímica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
Q74S4N8N1G (Radon)
[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:170930
[St] Status:MEDLINE
[do] DOI:10.1097/HP.0000000000000710


  5 / 2486 MEDLINE  
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[PMID]:28931274
[Au] Autor:Damont A; Boisgard R; Dollé F; Hollocou M; Kuhnast B
[Ad] Endereço:IMIV, Service Hospitalier Frédéric Joliot, CEA, Inserm, Université Paris Sud, CNRS, Université Paris-Saclay , Orsay, France.
[Ti] Título:Avidin/Biotin Bioinspired Platform for Dual In Vivo F-PET/NIRF Molecular Imaging.
[So] Source:Bioconjug Chem;28(10):2524-2529, 2017 Oct 18.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The complementary nature of positron emission tomography (PET) and near-infrared fluorescence (NIRF) imaging makes the development of innovative multimodal PET/NIRF probes a very exciting prospect. Herein, the bioinspired design of novel platform exploiting the strength and specificity of interactions between radioactive and fluorescent biotin derivatives and an avidin core is reported. The combination of an original [ F]fluoropyridinylated-biotin derivative and commercially available fluorescent biotin derivatives (Atto-425 and Atto-680) is investigated. The in vivo distribution of such a customized platform is also reported, for the first time, in healthy rodent using PET and ex vivo fluorescence imaging.
[Mh] Termos MeSH primário: Avidina/metabolismo
Biomimética/métodos
Biotina/metabolismo
Radioisótopos de Flúor
Raios Infravermelhos
Imagem Óptica/métodos
Tomografia por Emissão de Pósitrons/métodos
[Mh] Termos MeSH secundário: Radioquímica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fluorine Radioisotopes); 1405-69-2 (Avidin); 6SO6U10H04 (Biotin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171107
[Lr] Data última revisão:
171107
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170922
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.7b00536


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[PMID]:28864619
[Au] Autor:Müller C; van der Meulen NP; Benesová M; Schibli R
[Ad] Endereço:Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institut, Villigen-PSA, Switzerland.
[Ti] Título:Therapeutic Radiometals Beyond Lu and Y: Production and Application of Promising α-Particle, ß -Particle, and Auger Electron Emitters.
[So] Source:J Nucl Med;58(Suppl 2):91S-96S, 2017 Sep.
[Is] ISSN:1535-5667
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In recent years, new α-particle-, ß -particle-, and Auger electron-emitting radiometals-such as Cu, Sc, Ho, Tb, Tb, Pb/ Bi, Ac, and Bi-have been produced and evaluated (pre)clinically for therapeutic purposes. In this short review article, the most important routes of production of these radiometals are critically discussed, as are examples of their application in preclinical and clinical studies.
[Mh] Termos MeSH primário: Partículas alfa/uso terapêutico
Partículas beta/uso terapêutico
Elétrons
Metais/química
Radioquímica/métodos
Radioisótopos/química
Radioisótopos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Metals); 0 (Radioisotopes)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170903
[St] Status:MEDLINE
[do] DOI:10.2967/jnumed.116.186825


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[PMID]:28767228
[Au] Autor:Heskamp S; Raavé R; Boerman O; Rijpkema M; Goncalves V; Denat F
[Ad] Endereço:Department of Radiology and Nuclear Medicine, Radboud University Medical Center , Geert Grooteplein-Zuid 10, 6525 HP Nijmegen, The Netherlands.
[Ti] Título:Zr-Immuno-Positron Emission Tomography in Oncology: State-of-the-Art Zr Radiochemistry.
[So] Source:Bioconjug Chem;28(9):2211-2223, 2017 Sep 20.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Immuno-positron emission tomography (immunoPET) with Zr-labeled antibodies has shown great potential in cancer imaging. It can provide important information about the pharmacokinetics and tumor-targeting properties of monoclonal antibodies and may help in anticipating on toxicity. Furthermore, it allows accurate dose planning for individualized radioimmunotherapy and may aid in patient selection and early-response monitoring for targeted therapies. The most commonly used chelator for Zr is desferrioxamine (DFO). Preclinical studies have shown that DFO is not an ideal chelator because the Zr-DFO complex is partly unstable in vivo, which results in the release of Zr from the chelator and the subsequent accumulation of Zr in bone. This bone accumulation interferes with accurate interpretation and quantification of bone uptake on PET images. Therefore, there is a need for novel chelators that allow more stable complexation of Zr. In this Review, we will describe the most recent developments in Zr radiochemistry, including novel chelators and site-specific conjugation methods.
[Mh] Termos MeSH primário: Quelantes/química
Imunoconjugados/química
Neoplasias/diagnóstico
Tomografia por Emissão de Pósitrons/métodos
Zircônio/química
[Mh] Termos MeSH secundário: Animais
Quelantes/farmacocinética
Desferroxamina/química
Desferroxamina/farmacocinética
Sistemas de Liberação de Medicamentos/métodos
Descoberta de Drogas/métodos
Seres Humanos
Imunoconjugados/farmacocinética
Neoplasias/tratamento farmacológico
Neoplasias/terapia
Radioquímica/métodos
Radioisótopos/química
Radioisótopos/farmacocinética
Zircônio/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Chelating Agents); 0 (Immunoconjugates); 0 (Radioisotopes); C6V6S92N3C (Zirconium); J06Y7MXW4D (Deferoxamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170803
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.7b00325


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[PMID]:28420176
[Au] Autor:Xie Q; Zhu H; Wang F; Meng X; Ren Q; Xia C; Yang Z
[Ad] Endereço:College of Chemistry, Sichuan University, Chengdu 610064, China. qinghxie@163.com.
[Ti] Título:Establishing Reliable Cu-64 Production Process: From Target Plating to Molecular Specific Tumor Micro-PET Imaging.
[So] Source:Molecules;22(4), 2017 Apr 17.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Copper-64 is a useful radioisotope for positron emission tomography (PET). Due to the wide range of applications, the demand of Cu with low metallic impurities is increasing. Here we report a simple method for the efficient production of high specific activity Cu using a cyclotron for biomedical application. We designed new equipment based on the plating of enriched Ni as the target, and used automated ion exchange chromatography to purify copper-64 efficiently after irradiation and dissolution of the target in good radiochemical and chemical yield and purity. The Cu radionuclide produced using 99.32% enriched Ni with a density of 61.4 ± 5.0 mg/cm², reaching a total radioactivity greater than 200 mCi, with specific activity up to 5.6 GBq/µmoL. It was further incorporated into modified monoclonal antibody DOTA-rituximab to synthesize Cu-DOTA-rituximab, which was used successfully for micro-PET imaging.
[Mh] Termos MeSH primário: Radioisótopos de Cobre/química
Tomografia por Emissão de Pósitrons
Radioquímica
Compostos Radiofarmacêuticos/química
[Mh] Termos MeSH secundário: Animais
Radioisótopos de Cobre/isolamento & purificação
Camundongos
Neoplasias/diagnóstico por imagem
Tomografia por Emissão de Pósitrons/métodos
Radioquímica/instrumentação
Radioquímica/métodos
Compostos Radiofarmacêuticos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Copper Radioisotopes); 0 (Radiopharmaceuticals)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170531
[Lr] Data última revisão:
170531
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170420
[St] Status:MEDLINE


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[PMID]:28360209
[Au] Autor:Toczek J; Ye Y; Gona K; Kim HY; Han J; Razavian M; Golestani R; Zhang J; Wu TL; Jung JJ; Sadeghi MM
[Ad] Endereço:Cardiovascular Molecular Imaging Laboratory, Section of Cardiovascular Medicine and Yale Cardiovascular Research Center, Yale University School of Medicine, New Haven, Connecticut.
[Ti] Título:Preclinical Evaluation of RYM1, a Matrix Metalloproteinase-Targeted Tracer for Imaging Aneurysm.
[So] Source:J Nucl Med;58(8):1318-1323, 2017 Aug.
[Is] ISSN:1535-5667
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Matrix metalloproteinases (MMPs) play a key role in abdominal aortic aneurysm (AAA) development. Accordingly, MMP-targeted imaging provides important information regarding vessel wall biology in the course of aneurysm development. Given the small size of the vessel wall and its proximity with blood, molecular imaging of aneurysm optimally requires highly sensitive tracers with rapid blood clearance. To this end, we developed a novel hydrosoluble zwitterionic MMP inhibitor, RYM, on the basis of which a pan-MMP tracer, RYM1, was designed. Here, we describe the development and preclinical evaluation of RYM1 in comparison with RP805, a commonly used pan-MMP tracer in murine models of aneurysm. The macrocyclic hydroxamate-based pan-MMP inhibitor coupled with 6-hydrazinonicotinamide, RYM1, was synthesized and labeled with Tc. Radiochemical stability of Tc-RYM1 was evaluated by radio-high-performance liquid chromatography analysis. Tracer blood kinetics and biodistribution were compared with Tc-RP805 in C57BL/6J mice ( = 10). Tc-RYM1 binding to aneurysm and specificity were evaluated by quantitative autoradiography in apolipoprotein E-deficient (apoE ) mice with CaCl -induced carotid aneurysm ( = 11). Angiotensin II-infused apoE ( = 16) mice were used for small-animal SPECT/CT imaging. Aortic tissue MMP activity and macrophage marker CD68 expression were assessed by zymography and reverse-transcription polymerase chain reaction. RYM1 showed nanomolar range inhibition constants for several MMPs. Tc-RYM1 was radiochemically stable in mouse blood for 5 h and demonstrated rapid renal clearance and lower blood levels in vivo compared with Tc-RP805. Tc-RYM1 binding to aneurysm and its specificity were shown by autoradiography in carotid aneurysm. Angiotensin II infusion in apoE mice for 4 wk resulted in AAA formation in 36% (4/11) of surviving animals. In vivo Tc-RYM1 small-animal SPECT/CT images showed higher uptake of the tracer in AAA than nondilated aortae. Finally, aortic uptake of Tc-RYM1 in vivo correlated with aortic MMP activity and CD68 expression. The newly developed pan-MMP inhibitor-based tracer Tc-RYM1 displays favorable pharmacokinetics for early vascular imaging and enables specific detection of inflammation and MMP activity in aneurysm.
[Mh] Termos MeSH primário: Aneurisma/diagnóstico por imagem
Aneurisma/metabolismo
Ácidos Hidroxâmicos/metabolismo
Compostos Macrocíclicos/metabolismo
Inibidores de Metaloproteinases de Matriz/metabolismo
Metaloproteinases da Matriz/metabolismo
Imagem Molecular/métodos
Niacina/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Artérias Carótidas/diagnóstico por imagem
Desenho de Drogas
Estabilidade de Medicamentos
Regulação Enzimológica da Expressão Gênica
Ácidos Hidroxâmicos/química
Ácidos Hidroxâmicos/farmacocinética
Compostos Macrocíclicos/química
Compostos Macrocíclicos/farmacocinética
Inibidores de Metaloproteinases de Matriz/química
Inibidores de Metaloproteinases de Matriz/farmacocinética
Camundongos
Niacina/química
Niacina/metabolismo
Niacina/farmacocinética
Traçadores Radioativos
Radioquímica
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hydroxamic Acids); 0 (Macrocyclic Compounds); 0 (Matrix Metalloproteinase Inhibitors); 0 (Radioactive Tracers); 2679MF687A (Niacin); EC 3.4.24.- (Matrix Metalloproteinases)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170825
[Lr] Data última revisão:
170825
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170401
[St] Status:MEDLINE
[do] DOI:10.2967/jnumed.116.188656


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[PMID]:28338530
[Au] Autor:Han J; Liu H; Liu C; Jin H; Perlmutter JS; Egan TM; Tu Z
[Ad] Endereço:Departments of aRadiology bNeurology, Neuroscience, Physical Therapy and Occupational Therapy, Washington University School of Medicine cDepartment of Pharmacological and Physiological Science, Saint Louis University School of Medicine, St. Louis, Missouri, USA.
[Ti] Título:Pharmacologic characterizations of a P2X7 receptor-specific radioligand, [11C]GSK1482160 for neuroinflammatory response.
[So] Source:Nucl Med Commun;38(5):372-382, 2017 May.
[Is] ISSN:1473-5628
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: The P2X7 receptor (P2X7R) is a key regulatory element in the neuroinflammatory cascade that provides a promising target for imaging neuroinflammation. GSK1482160, a P2X7R modulator with nanomolar binding affinity and high selectivity, has been successfully radiolabeled and utilized for imaging P2X7 levels in a mouse model of lipopolysaccharide-induced systemic inflammation. In the current study, we further characterized its binding profile and determined whether [C]GSK1482160 can detect changes in P2X7R expression in a rodent model of multiple sclerosis. METHODS: [C]GSK1482160 was synthesized with high specific activity and high radiochemical purity. Radioligand saturation and competition binding assays were performed for [C]GSK1482160 using HEK293-hP2X7R living cells. Micro-PET studies were carried out in nonhuman primates. In vitro autoradiography and immunohistochemistry studies were then carried out to evaluate tracer uptake and P2X7 expression in experimental autoimmune encephalomyelitis (EAE) rat lumbar spinal cord at EAE-peak and EAE-remitting stages compared with sham rats. RESULTS: [C]GSK1482160 binds to HEK293-hP2X7R living cells with high binding affinity (Kd=5.09±0.98 nmol/l, Ki=2.63±0.6 nmol/l). Micro-PET studies showed high tracer retention and a homogeneous distribution in the brain of nonhuman primates. In the EAE rat model, tracer uptake of [C]GSK1482160 in rat lumbar spinal cord was the highest at the EAE-peak stage (277.74±79.74 PSL/mm), followed by the EAE-remitting stage(149.00±54.14 PSL/mm) and sham (66.37±1.48 PSL/mm). The tracer uptake correlated strongly with P2X7-positive cell counts, activated microglia numbers, and disease severity. CONCLUSION: We conclude that [C]GSK1482160 has the potential for application in monitoring neuroinflammation.
[Mh] Termos MeSH primário: Radioisótopos de Carbono
Encefalomielite Autoimune Experimental/metabolismo
Ácido Pirrolidonocarboxílico/metabolismo
Receptores Purinérgicos P2X7/metabolismo
[Mh] Termos MeSH secundário: Animais
Transporte Biológico
Encéfalo/diagnóstico por imagem
Encéfalo/metabolismo
Progressão da Doença
Encefalomielite Autoimune Experimental/diagnóstico por imagem
Feminino
Regulação da Expressão Gênica
Células HEK293
Seres Humanos
Ligantes
Macaca fascicularis
Masculino
Camundongos
Tomografia por Emissão de Pósitrons
Ácido Pirrolidonocarboxílico/química
Radioquímica
Ratos
Medula Espinal/diagnóstico por imagem
Medula Espinal/metabolismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbon Radioisotopes); 0 (Ligands); 0 (N-(2-chloro-3-(trifluoromethyl)benzyl)-N-methyl-5-oxopyrrolidine-2-carboxamide); 0 (Receptors, Purinergic P2X7); SZB83O1W42 (Pyrrolidonecarboxylic Acid)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171117
[Lr] Data última revisão:
171117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170325
[St] Status:MEDLINE
[do] DOI:10.1097/MNM.0000000000000660



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