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[PMID]:28442581
[Au] Autor:Hiranita T; Hong WC; Kopajtic T; Katz JL
[Ad] Endereço:Psychobiology Section, Molecular Neuropsychiatry Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health (T.H., T.K., J.L.K.), and Department of Pharmaceutical Sciences, Butler University (W.C.H.), Indianapolis, Indiana.
[Ti] Título:σ Receptor Effects of N-Substituted Benztropine Analogs: Implications for Antagonism of Cocaine Self-Administration.
[So] Source:J Pharmacol Exp Ther;362(1):2-13, 2017 Jul.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Several N-substituted benztropine (BZT) analogs are atypical dopamine transport inhibitors as they have affinity for the dopamine transporter (DAT) but have minimal cocaine-like pharmacologic effects and can block numerous effects of cocaine, including its self-administration. Among these compounds, -methyl (AHN1-055), -allyl (AHN2-005), and -butyl (JHW007) analogs of 3 -[bis(4'-fluorophenyl)methoxy]-tropane were more potent in antagonizing self-administration of cocaine and -methamphetamine than in decreasing food-maintained responding. The antagonism of cocaine self-administration (0.03-1.0 mg/kg per injection) with the above BZT analogs was reproduced in the present study. Further, the stimulant-antagonist effects resembled previously reported effects of pretreatments with combinations of standard DAT inhibitors and -receptor ( R) antagonists. Therefore, the present study examined binding of the BZT analogs to Rs, as well as their in vivo R antagonist effects. Each of the BZT analogs displaced radiolabeled R ligands with nanomolar affinity. Further, self-administration of the R agonist DTG (0.1-3.2 mg/kg/injection) was dose dependently blocked by AHN2-005 and JHW007 but potentiated by AHN1-055. In contrast, none of the BZT analogs that were active against DTG self-administration was active against the self-administration of agonists at dopamine D -like [ (+)-SKF 81297, (±)-SKF 82958 (0.00032-0.01 mg/kg per injection each)], D -like [ (-)-NPA (0.0001-0.0032 mg/kg per injection), (-)-quinpirole (0.0032-0.1 mg/kg per injection)], or -opioid (remifentanil, 0.0001-0.0032 mg/kg per injection) receptors. The present results indicate that behavioral antagonist effects of the -substituted BZT analogs are specific for abused drugs acting at the DAT and further suggest that R antagonism contributes to those actions.
[Mh] Termos MeSH primário: Benzotropina/análogos & derivados
Benzotropina/farmacologia
Transtornos Relacionados ao Uso de Cocaína/tratamento farmacológico
Receptores sigma/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Química Encefálica/efeitos dos fármacos
Cocaína/farmacologia
Transtornos Relacionados ao Uso de Cocaína/psicologia
Condicionamento Operante/efeitos dos fármacos
Dopaminérgicos/farmacologia
Relação Dose-Resposta a Droga
Técnicas In Vitro
Masculino
Camundongos
Ensaio Radioligante
Ratos
Ratos Sprague-Dawley
Autoadministração
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dopamine Agents); 0 (Receptors, sigma); 0 (sigma-1 receptor); 0 (sigma-2 receptor); 1NHL2J4X8K (Benztropine); I5Y540LHVR (Cocaine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170714
[Lr] Data última revisão:
170714
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170427
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.117.241109


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[PMID]:28176326
[Au] Autor:Cheng Q; Shah N; Bröer A; Fairweather S; Jiang Y; Schmoll D; Corry B; Bröer S
[Ad] Endereço:Research School of Biology, The Australian National University, Canberra, Australia.
[Ti] Título:Identification of novel inhibitors of the amino acid transporter B AT1 (SLC6A19), a potential target to induce protein restriction and to treat type 2 diabetes.
[So] Source:Br J Pharmacol;174(6):468-482, 2017 Mar.
[Is] ISSN:1476-5381
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND PURPOSE: The neutral amino acid transporter B AT1 (SLC6A19) has recently been identified as a possible target to treat type 2 diabetes and related disorders. B AT1 mediates the Na -dependent uptake of all neutral amino acids. For surface expression and catalytic activity, B AT1 requires coexpression of collectrin (TMEM27). In this study, we established tools to identify and evaluate novel inhibitors of B AT1. EXPERIMENTAL APPROACH: A CHO-based cell line was generated, stably expressing collectrin and B AT1. Using this cell line, a high-throughput screening assay was developed, which uses a fluorescent dye to detect depolarisation of the cell membrane during amino acid uptake via B AT1. In parallel to these functional assays, we ran a computational compound screen using AutoDock4 and a homology model of B AT1 based on the high-resolution structure of the highly homologous Drosophila dopamine transporter. KEY RESULTS: We characterized a series of novel inhibitors of the B AT1 transporter. Benztropine was identified as a competitive inhibitor of the transporter showing an IC of 44 ± 9 µM. The compound was selective with regard to related transporters and blocked neutral amino acid uptake in inverted sections of mouse intestine. CONCLUSION AND IMPLICATIONS: The tools established in this study can be widely used to identify new transport inhibitors. Using these tools, we were able to identify compounds that can be used to study epithelial transport, to induce protein restriction, or be developed further through medicinal chemistry.
[Mh] Termos MeSH primário: Sistemas de Transporte de Aminoácidos Neutros/antagonistas & inibidores
Benzotropina/farmacologia
Diabetes Mellitus Tipo 2/tratamento farmacológico
[Mh] Termos MeSH secundário: Sistemas de Transporte de Aminoácidos/química
Sistemas de Transporte de Aminoácidos/metabolismo
Sistemas de Transporte de Aminoácidos Neutros/metabolismo
Animais
Benzotropina/química
Células CHO
Cricetulus
Diabetes Mellitus Tipo 2/metabolismo
Relação Dose-Resposta a Droga
Drosophila
Feminino
Ensaios de Triagem em Larga Escala
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Simulação de Acoplamento Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acid Transport Systems); 0 (Amino Acid Transport Systems, Neutral); 0 (SLC6A19 protein, mouse); 1NHL2J4X8K (Benztropine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170209
[St] Status:MEDLINE
[do] DOI:10.1111/bph.13711


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[PMID]:27599508
[Au] Autor:Kudriaeva AA; Khaustova NA; Maltseva DV; Kuzina ES; Glagoleva IS; Surina EA; Knorre VD; Belogurov AA; Tonevitsky AG; Gabibov AG
[Ad] Endereço:Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow, 117997, Russia.
[Ti] Título:mRNA expression profile of mouse oligodendrocytes in inflammatory conditions.
[So] Source:Dokl Biochem Biophys;469(1):264-8, 2016 Jul.
[Is] ISSN:1608-3091
[Cp] País de publicação:Russia (Federation)
[La] Idioma:eng
[Ab] Resumo:In this study, we performed transcriptome profiling of oligodendrocyte culture of mice treated with the remyelinating therapeutic agent benztropine in the presence and absence of interferon gamma (IFNγ). The results of this work are important for understanding the expression profile of oligodendrocytes under conditions of systemic inflammation in the central nervous system in multiple sclerosis as well as the mechanisms of cellular response to benztropine in light of its possible use for the treatment of multiple sclerosis.
[Mh] Termos MeSH primário: Oligodendroglia/imunologia
RNA Mensageiro/imunologia
Transcriptoma/imunologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/farmacologia
Benzotropina/farmacologia
Células Cultivadas
Perfilação da Expressão Gênica
Fatores Imunológicos/farmacologia
Interferon gama/farmacologia
Camundongos Endogâmicos C3H
Oligodendroglia/efeitos dos fármacos
Complexo de Endopeptidases do Proteassoma/efeitos dos fármacos
Complexo de Endopeptidases do Proteassoma/imunologia
Transcriptoma/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Immunologic Factors); 0 (RNA, Messenger); 1NHL2J4X8K (Benztropine); 82115-62-6 (Interferon-gamma); EC 3.4.25.1 (Proteasome Endopeptidase Complex)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160908
[St] Status:MEDLINE
[do] DOI:10.1134/S1607672916040086


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[PMID]:26383155
[Au] Autor:Thornton SL; Farnaes L; Minns A
[Ad] Endereço:From the *Poison Control Center, University of Kansas Hospital, Kansas City, KS; †Department of Medicine/Pediatrics, and ‡Division of Medical Toxicology, Department of Emergency Medicine, University of California San Diego, San Diego, CA.
[Ti] Título:Prolonged Antimuscarinic Delirium in a Child Due to Benztropine Exposure Treated With Multiple Doses of Physostigmine.
[So] Source:Pediatr Emerg Care;32(4):243-5, 2016 Apr.
[Is] ISSN:1535-1815
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:An 11-year-old boy presented with an antimuscarinic toxidrome due to benztropine and risperidone ingestion. His delirium was prolonged and difficult to treat with benzodiazepines. Multiple doses of physostigmine successfully treated it. Benztropine is a potent antimuscarinic agent, whereas risperidone has not been reported to cause antimuscarinic toxicity. The use of physostigmine to treat benztropine intoxication in a pediatric patient has not previously been described. In this case, multiple doses were used and were well tolerated.
[Mh] Termos MeSH primário: Benzotropina/efeitos adversos
Inibidores da Colinesterase/administração & dosagem
Delírio/induzido quimicamente
Antagonistas Muscarínicos/efeitos adversos
Fisostigmina/administração & dosagem
[Mh] Termos MeSH secundário: Criança
Delírio/tratamento farmacológico
Seres Humanos
Masculino
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Muscarinic Antagonists); 1NHL2J4X8K (Benztropine); 9U1VM840SP (Physostigmine)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170113
[Lr] Data última revisão:
170113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150919
[St] Status:MEDLINE
[do] DOI:10.1097/PEC.0000000000000503


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[PMID]:26202243
[Au] Autor:Cheng H; Lear-Rooney CM; Johansen L; Varhegyi E; Chen ZW; Olinger GG; Rong L
[Ad] Endereço:Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, Illinois, USA.
[Ti] Título:Inhibition of Ebola and Marburg Virus Entry by G Protein-Coupled Receptor Antagonists.
[So] Source:J Virol;89(19):9932-8, 2015 Oct.
[Is] ISSN:1098-5514
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:UNLABELLED: Filoviruses, consisting of Ebola virus (EBOV) and Marburg virus (MARV), are among the most lethal infectious threats to mankind. Infections by these viruses can cause severe hemorrhagic fevers in humans and nonhuman primates with high mortality rates. Since there is currently no vaccine or antiviral therapy approved for humans, there is an urgent need to develop prophylactic and therapeutic options for use during filoviral outbreaks and bioterrorist attacks. One of the ideal targets against filoviral infection and diseases is at the entry step, which is mediated by the filoviral glycoprotein (GP). In this report, we screened a chemical library of small molecules and identified numerous inhibitors, which are known G protein-coupled receptor (GPCR) antagonists targeting different GPCRs, including histamine receptors, 5-HT (serotonin) receptors, muscarinic acetylcholine receptor, and adrenergic receptor. These inhibitors can effectively block replication of both infectious EBOV and MARV, indicating a broad antiviral activity of the GPCR antagonists. The time-of-addition experiment and microscopic studies suggest that GPCR antagonists block filoviral entry at a step following the initial attachment but prior to viral/cell membrane fusion. These results strongly suggest that GPCRs play a critical role in filoviral entry and GPCR antagonists can be developed as an effective anti-EBOV/MARV therapy. IMPORTANCE: Infection of Ebola virus and Marburg virus can cause severe illness in humans with a high mortality rate, and currently there is no FDA-approved vaccine or therapeutic treatment available. The 2013-2015 epidemic in West Africa underscores a lack of our understanding in the infection and pathogenesis of these viruses and the urgency of drug discovery and development. In this study, we have identified numerous inhibitors that are known G protein-coupled receptor (GPCR) antagonists targeting different GPCRs. These inhibitors can effectively block replication of both infectious EBOV and MARV, indicating a broad antiviral activity of the GPCR antagonists. Our results strongly suggest that GPCRs play a critical role in filoviral entry and GPCR antagonists can be developed as an effective anti-EBOV/MARV therapy.
[Mh] Termos MeSH primário: Ebolavirus/efeitos dos fármacos
Ebolavirus/fisiologia
Marburgvirus/efeitos dos fármacos
Marburgvirus/fisiologia
Receptores Acoplados a Proteínas-G/antagonistas & inibidores
Internalização do Vírus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Antivirais/farmacologia
Benzotropina/farmacologia
Linhagem Celular
Cercopithecus aethiops
Ciproeptadina/farmacologia
Ebolavirus/patogenicidade
Células HEK293
Doença pelo Vírus Ebola/tratamento farmacológico
Heparina/farmacologia
Ensaios de Triagem em Larga Escala
Seres Humanos
Macrolídeos/farmacologia
Doença do Vírus de Marburg/tratamento farmacológico
Marburgvirus/patogenicidade
Receptores Acoplados a Proteínas-G/fisiologia
Bibliotecas de Moléculas Pequenas
Células Vero
Zidovudina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Macrolides); 0 (Receptors, G-Protein-Coupled); 0 (Small Molecule Libraries); 1NHL2J4X8K (Benztropine); 2YHB6175DO (Cyproheptadine); 4B9XT59T7S (Zidovudine); 88899-55-2 (bafilomycin A1); 9005-49-6 (Heparin)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150724
[St] Status:MEDLINE
[do] DOI:10.1128/JVI.01337-15


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[PMID]:26132170
[Au] Autor:Cook TB; Reeves GM; Teufel J; Postolache TT
[Ad] Endereço:Department of Public Health, Mercyhurst Institute of Public Health, Mercyhurst University, Erie, PA, USA.
[Ti] Título:Persistence of racial disparities in prescription of first-generation antipsychotics in the USA.
[So] Source:Pharmacoepidemiol Drug Saf;24(11):1197-206, 2015 Nov.
[Is] ISSN:1099-1557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: The aim of this study was to estimate the prevalence of first-generation antipsychotics (FGA) prescribed for treatment of psychiatric and neurological conditions and use of benztropine to reduce extrapyramidal side effects (EPS) by patient race/ethnicity in a nationally representative sample of adult outpatient visits. METHODS: The study sample included all outpatient visits (N = 8154) among patients aged 18-69 years where a prescription for one or more antipsychotics was recorded across 6 years of the National Ambulatory Medical Care Survey and National Hospital Ambulatory Medical Care Survey (2005-2010). Use of FGA was compared by race/ethnicity using multiple logistic regression models accounting for patient and clinical characteristics stratified by neighborhood poverty rate. Frequency of EPS was determined by use of benztropine to reduce or prevent EPS. RESULTS: Black patients were significantly more likely than White patients to use FGA (odds ratio = 1.48, p = 0.040) accounting for psychiatric and neurological diagnoses, treatment setting, metabolic factors, neighborhood poverty, and payer source. Black patients were more than twice as likely as White patients to receive higher-potency FGA (haloperidol or fluphenazine), particularly in higher-poverty areas (odds ratio = 2.50, p < 0.001). Use of FGA, higher among Black than White patients, was positively associated with use of benztropine to reduce EPS. CONCLUSIONS: Racial disparities in the pharmacological treatment of severe mental disorders persist 30 years after the introduction of second-generation antipsychotics. The relatively high frequency of FGA of use among Black patients compared with White patients despite more Food and Drug Administration-approved indications and lower EPS risk for second-generation antipsychotics requires additional research.
[Mh] Termos MeSH primário: Assistência Ambulatorial/estatística & dados numéricos
Antipsicóticos/uso terapêutico
Disparidades em Assistência à Saúde
Transtornos Mentais/tratamento farmacológico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Afroamericanos/estatística & dados numéricos
Idoso
Assistência Ambulatorial/normas
Antipsicóticos/administração & dosagem
Antipsicóticos/efeitos adversos
Benzotropina/administração & dosagem
Benzotropina/uso terapêutico
Grupos de Populações Continentais/estatística & dados numéricos
Grupo com Ancestrais do Continente Europeu/estatística & dados numéricos
Feminino
Pesquisas sobre Serviços de Saúde
Seres Humanos
Modelos Logísticos
Masculino
Meia-Idade
Áreas de Pobreza
Padrões de Prática Médica/normas
Padrões de Prática Médica/estatística & dados numéricos
Estados Unidos
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 1NHL2J4X8K (Benztropine)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:151104
[Lr] Data última revisão:
151104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150702
[St] Status:MEDLINE
[do] DOI:10.1002/pds.3819


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[PMID]:25548026
[Au] Autor:Reith ME; Blough BE; Hong WC; Jones KT; Schmitt KC; Baumann MH; Partilla JS; Rothman RB; Katz JL
[Ad] Endereço:Department of Psychiatry, New York University School of Medicine, New York, NY 10016, USA; Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine, New York, NY 10016, USA. Electronic address: Maarten.Reith@nyumc.org.
[Ti] Título:Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporter.
[So] Source:Drug Alcohol Depend;147:1-19, 2015 Feb 01.
[Is] ISSN:1879-0046
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Treatment of stimulant-use disorders remains a formidable challenge, and the dopamine transporter (DAT) remains a potential target for antagonist or agonist-like substitution therapies. METHODS: This review focuses on DAT ligands, such as benztropine, GBR 12909, modafinil, and DAT substrates derived from phenethylamine or cathinone that have atypical DAT-inhibitor effects, either in vitro or in vivo. The compounds are described from a molecular mechanistic, behavioral, and medicinal-chemical perspective. RESULTS: Possible mechanisms for atypicality at the molecular level can be deduced from the conformational cycle for substrate translocation. For each conformation, a crystal structure of a bacterial homolog is available, with a possible role of cholesterol, which is also present in the crystal of Drosophila DAT. Although there is a direct relationship between behavioral potencies of most DAT inhibitors and their DAT affinities, a number of compounds bind to the DAT and inhibit dopamine uptake but do not share cocaine-like effects. Such atypical behavior, depending on the compound, may be related to slow DAT association, combined sigma-receptor actions, or bias for cytosol-facing DAT. Some structures are sterically small enough to serve as DAT substrates but large enough to also inhibit transport. Such compounds may display partial DA releasing effects, and may be combined with release or uptake inhibition at other monoamine transporters. CONCLUSIONS: Mechanisms of atypical DAT inhibitors may serve as targets for the development of treatments for stimulant abuse. These mechanisms are novel and their further exploration may produce compounds with unique therapeutic potential as treatments for stimulant abuse.
[Mh] Termos MeSH primário: Proteínas da Membrana Plasmática de Transporte de Dopamina/química
Proteínas da Membrana Plasmática de Transporte de Dopamina/metabolismo
Sistemas de Liberação de Medicamentos
[Mh] Termos MeSH secundário: Animais
Compostos Benzidrílicos/metabolismo
Compostos Benzidrílicos/farmacologia
Benzotropina/metabolismo
Benzotropina/farmacologia
Estimulantes do Sistema Nervoso Central/metabolismo
Estimulantes do Sistema Nervoso Central/farmacologia
Cocaína/farmacologia
Proteínas da Membrana Plasmática de Transporte de Dopamina/antagonistas & inibidores
Sistemas de Liberação de Medicamentos/métodos
Seres Humanos
Ligantes
Ligação Proteica/fisiologia
Estrutura Secundária de Proteína
Estrutura Terciária de Proteína
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, N.I.H., INTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Benzhydryl Compounds); 0 (Central Nervous System Stimulants); 0 (Dopamine Plasma Membrane Transport Proteins); 0 (Ligands); 1NHL2J4X8K (Benztropine); I5Y540LHVR (Cocaine); R3UK8X3U3D (modafinil)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:170624
[Lr] Data última revisão:
170624
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141231
[St] Status:MEDLINE


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[PMID]:25414475
[Au] Autor:Asha SE; Kerr A; Jones K; McAlpine A
[Ad] Endereço:Emergency Department, St George Hospital, Sydney, New South Wales, Australia Faculty of Medicine, University of New South Wales, Sydney, New South Wales, Australia.
[Ti] Título:Benztropine for the relief of acute non-traumatic neck pain (wry neck): a randomised trial.
[So] Source:Emerg Med J;32(8):616-9, 2015 Aug.
[Is] ISSN:1472-0213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: The aim of this study was to determine the effect of intra-muscular benztropine on pain and range of motion in patients presenting to the emergency department with acute, non-traumatic neck pain (wry neck). METHODS: In this two-centre randomised, double-blind, placebo-controlled, parallel-group superiority trial, participants were allocated to receive 2 mg intramuscular benztropine or normal saline. Participants were aged 16-65 years, no history of neck disorders and no use of medication that cause dystonia. Randomisation was computer generated, with allocation concealment by opaque sequentially numbered sealed envelopes. Pain scores and neck range of motion were measured immediately before drug administration, and 30 min after. Pain scores, range of motion and adverse effects were compared between the groups. No funding was received. The trial was registered. RESULTS: Thirty participants were enrolled, 15 randomised to placebo and 15 to benztropine. Pain scores at 30 min were lower in those allocated to benztropine, but the difference was neither statistically nor clinically significant (0.6 points, 95% CI -0.8 to 1.8, p=0.40). The range of motion of the cervical spine was greater in those receiving benztropine, but the differences were very small and not statistically significant. Adverse events were more common in those receiving benztropine. CONCLUSIONS: Benztropine was ineffective for reducing pain or improving range of motion of the cervical spine in patients suffering from acute, non-traumatic neck pain, but frequently caused anticholinergic side effects. However, as the CI for the primary outcome included the minimum difference considered clinically significant, an important effect of benztropine cannot be ruled out. TRIAL REGISTRATION NUMBER: ANZCTR#12612000354886.
[Mh] Termos MeSH primário: Benzotropina/uso terapêutico
Antagonistas Muscarínicos/uso terapêutico
Cervicalgia/tratamento farmacológico
Parassimpatolíticos/uso terapêutico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Método Duplo-Cego
Feminino
Seres Humanos
Injeções Intramusculares
Masculino
Meia-Idade
Cervicalgia/fisiopatologia
Medição da Dor
Amplitude de Movimento Articular/fisiologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Muscarinic Antagonists); 0 (Parasympatholytics); 1NHL2J4X8K (Benztropine)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:150721
[Lr] Data última revisão:
150721
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141122
[St] Status:MEDLINE
[do] DOI:10.1136/emermed-2014-204317


  9 / 663 MEDLINE  
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[PMID]:25392329
[Au] Autor:Green AJ
[Ti] Título:The best basic science paper in MS in 2013: Antimuscarinic therapies in remyelination.
[So] Source:Mult Scler;20(14):1814-6, 2014 Dec.
[Is] ISSN:1477-0970
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Benzotropina/uso terapêutico
Encefalomielite Autoimune Experimental/tratamento farmacológico
Ensaios de Triagem em Larga Escala/métodos
Modelos Biológicos
Esclerose Múltipla/tratamento farmacológico
Antagonistas Muscarínicos/isolamento & purificação
Bainha de Mielina/efeitos dos fármacos
Fibras Nervosas Mielinizadas/efeitos dos fármacos
Oligodendroglia/efeitos dos fármacos
Regeneração/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Feminino
[Pt] Tipo de publicação:COMMENT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Muscarinic Antagonists); 1NHL2J4X8K (Benztropine)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:141218
[Lr] Data última revisão:
141218
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141114
[St] Status:MEDLINE
[do] DOI:10.1177/1352458514558679


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[PMID]:24709263
[Au] Autor:Mingorance L; Friesland M; Coto-Llerena M; Pérez-del-Pulgar S; Boix L; López-Oliva JM; Bruix J; Forns X; Gastaminza P
[Ad] Endereço:Centro Nacional De Biotecnología-Consejo Superior de Investigaciones Científicas (CNB-CSIC), Madrid, Spain.
[Ti] Título:Selective inhibition of hepatitis C virus infection by hydroxyzine and benztropine.
[So] Source:Antimicrob Agents Chemother;58(6):3451-60, 2014 Jun.
[Is] ISSN:1098-6596
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Hepatitis C virus (HCV) infection is a major biomedical problem worldwide as it causes severe liver disease in millions of humans around the world. Despite the recent approval of specific drugs targeting HCV replication to be used in combination with alpha interferon (IFN-α) and ribavirin, there is still an urgent need for pangenotypic, interferon-free therapies to fight this genetically diverse group of viruses. In this study, we used an unbiased screening cell culture assay to interrogate a chemical library of compounds approved for clinical use in humans. This system enables identifying nontoxic antiviral compounds targeting every aspect of the viral life cycle, be the target viral or cellular. The aim of this study was to identify drugs approved for other therapeutic applications in humans that could be effective components of combination therapies against HCV. As a result of this analysis, we identified 12 compounds with antiviral activity in cell culture, some of which had previously been identified as HCV inhibitors with antiviral activity in cell culture and had been shown to be effective in patients. We selected two novel HCV antivirals, hydroxyzine and benztropine, to characterize them by determining their specificity and genotype spectrum as well as by defining the step of the replication cycle targeted by these compounds. We found that both compounds effectively inhibited viral entry at a postbinding step of genotypes 1, 2, 3, and 4 without affecting entry of other viruses.
[Mh] Termos MeSH primário: Antivirais/uso terapêutico
Benzotropina/uso terapêutico
Hepacivirus/efeitos dos fármacos
Hepatite C/tratamento farmacológico
Hidroxizina/uso terapêutico
Interferon-alfa/uso terapêutico
Ribavirina/uso terapêutico
[Mh] Termos MeSH secundário: Bioensaio
Técnicas de Cultura de Células
Quimioterapia Combinada
Genética Populacional
Genótipo
Hepacivirus/genética
Hepatite C/virologia
Seres Humanos
Fígado
Bibliotecas de Moléculas Pequenas
Replicação Viral/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Interferon-alpha); 0 (Small Molecule Libraries); 1NHL2J4X8K (Benztropine); 30S50YM8OG (Hydroxyzine); 49717AWG6K (Ribavirin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140409
[St] Status:MEDLINE
[do] DOI:10.1128/AAC.02619-14



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