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Referências encontradas : 704 [refinar]
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[PMID]:26066863
[Au] Autor:Eisenstein SA; Bischoff AN; Gredysa DM; Antenor-Dorsey JA; Koller JM; Al-Lozi A; Pepino MY; Klein S; Perlmutter JS; Moerlein SM; Black KJ; Hershey T
[Ad] Endereço:1] Departments of Psychiatry, Washington University School of Medicine, St. Louis, MO 63110, USA [2] Departments of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
[Ti] Título:Emotional Eating Phenotype is Associated with Central Dopamine D2 Receptor Binding Independent of Body Mass Index.
[So] Source:Sci Rep;5:11283, 2015 Jun 12.
[Is] ISSN:2045-2322
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PET studies have provided mixed evidence regarding central D2/D3 dopamine receptor binding and its relationship with obesity as measured by body mass index (BMI). Other aspects of obesity may be more tightly coupled to the dopaminergic system. We characterized obesity-associated behaviors and determined if these related to central D2 receptor (D2R) specific binding independent of BMI. Twenty-two obese and 17 normal-weight participants completed eating- and reward-related questionnaires and underwent PET scans using the D2R-selective and nondisplaceable radioligand (N-[(11)C]methyl)benperidol. Questionnaires were grouped by domain (eating related to emotion, eating related to reward, non-eating behavior motivated by reward or sensitivity to punishment). Normalized, summed scores for each domain were compared between obese and normal-weight groups and correlated with striatal and midbrain D2R binding. Compared to normal-weight individuals, the obese group self-reported higher rates of eating related to both emotion and reward (p<0.001), greater sensitivity to punishment (p=0.06), and lower non-food reward behavior (p<0.01). Across normal-weight and obese participants, self-reported emotional eating and non-food reward behavior positively correlated with striatal (p<0.05) and midbrain (p<0.05) D2R binding, respectively. In conclusion, an emotional eating phenotype may reflect altered central D2R function better than other commonly used obesity-related measures such as BMI.
[Mh] Termos MeSH primário: Encéfalo
Emoções
Comportamento Alimentar
Obesidade
Tomografia por Emissão de Pósitrons
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Adulto
Bemperidol/administração & dosagem
Bemperidol/farmacocinética
Índice de Massa Corporal
Encéfalo/diagnóstico por imagem
Encéfalo/metabolismo
Feminino
Seres Humanos
Masculino
Obesidade/diagnóstico por imagem
Obesidade/metabolismo
Radiografia
Inquéritos e Questionários
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (DRD2 protein, human); 0 (Receptors, Dopamine D2); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:170301
[Lr] Data última revisão:
170301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150613
[St] Status:MEDLINE
[do] DOI:10.1038/srep11283


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[PMID]:23650017
[Au] Autor:Eisenstein SA; Antenor-Dorsey JA; Gredysa DM; Koller JM; Bihun EC; Ranck SA; Arbeláez AM; Klein S; Perlmutter JS; Moerlein SM; Black KJ; Hershey T
[Ad] Endereço:Department of Psychiatry, Washington University School of Medicine, St. Louis, Missouri, 63110.
[Ti] Título:A comparison of D2 receptor specific binding in obese and normal-weight individuals using PET with (N-[(11)C]methyl)benperidol.
[So] Source:Synapse;67(11):748-56, 2013 Nov.
[Is] ISSN:1098-2396
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Previous PET imaging studies have demonstrated mixed findings regarding dopamine D2/D3 receptor availability in obese relative to nonobese humans. Nonspecific D2/D3 radioligands do not allow for separate estimation of D2 receptor (D2R) and D3 receptor (D3R) subtypes of the D2 receptor family, which may play different roles in behavior and are distributed differently throughout the brain. These radioligands are also displaceable by endogenous dopamine, confounding interpretation of differences in receptor availability with differing levels of dopamine release. The present study used PET imaging with the D2R-selective radioligand (N-[(11)C] methyl)benperidol ([(11)C]NMB), which is nondisplaceable by endogenous dopamine, to estimate D2R specific binding (BPND) and its relationship to body mass index (BMI) and age in 15 normal-weight (mean BMI = 22.6 kg/m(2)) and 15 obese (mean BMI = 40.3 kg/m(2)) men and women. Subjects with illnesses or taking medications that interfere with dopamine signaling were excluded. Striatal D2R BPND was calculated using the Logan graphical method with cerebellum as a reference region. D2R BPND estimates were higher in putamen and caudate relative to nucleus accumbens, but did not differ between normal-weight and obese groups. BMI values did not correlate with D2R BPND . Age was negatively correlated with putamen D2R BPND in both groups. These results suggest that altered D2R specific binding is not involved in the pathogenesis of obesity per se and underscore the need for additional studies evaluating the relationship between D3R, dopamine reuptake, or endogenous dopamine release and human obesity.
[Mh] Termos MeSH primário: Obesidade/metabolismo
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Adulto
Fatores Etários
Bemperidol/administração & dosagem
Bemperidol/análogos & derivados
Índice de Massa Corporal
Encéfalo/diagnóstico por imagem
Encéfalo/metabolismo
Estudos de Casos e Controles
Feminino
Seres Humanos
Masculino
Obesidade/diagnóstico por imagem
Obesidade/etiologia
Especificidade de Órgãos
Tomografia por Emissão de Pósitrons
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Receptors, Dopamine D2); 133066-70-3 (N-methylbenperidol); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:1405
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130508
[St] Status:MEDLINE
[do] DOI:10.1002/syn.21680


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[PMID]:22535514
[Au] Autor:Eisenstein SA; Koller JM; Piccirillo M; Kim A; Antenor-Dorsey JA; Videen TO; Snyder AZ; Karimi M; Moerlein SM; Black KJ; Perlmutter JS; Hershey T
[Ad] Endereço:Department of Psychiatry, Washington University School of Medicine in St. Louis, St. Louis, Missouri 63110, USA.
[Ti] Título:Characterization of extrastriatal D2 in vivo specific binding of [¹8F](N-methyl)benperidol using PET.
[So] Source:Synapse;66(9):770-80, 2012 Sep.
[Is] ISSN:1098-2396
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PET imaging studies of the role of the dopamine D2 receptor family in movement and neuropsychiatric disorders are limited by the use of radioligands that have near-equal affinities for D2 and D3 receptor subtypes and are susceptible to competition with endogenous dopamine. By contrast, the radioligand [¹8F]N-methylbenperidol ([¹8F]NMB) has high selectivity and affinity for the D2 receptor subtype (D2R) and is not sensitive to endogenous dopamine. Although [¹8F]NMB has high binding levels in striatum, its utility for measuring D2R in extrastriatal regions is unknown. A composite MR-PET image was constructed across 14 healthy adult participants representing average NMB uptake 60 to 120 min after [¹8F]NMB injection. Regional peak radioactivity was identified using a peak-finding algorithm. FreeSurfer and manual tracing identified a priori regions of interest (ROI) on each individual's MR image and tissue activity curves were extracted from coregistered PET images. [¹8F]NMB binding potentials (BP(ND) s) were calculated using the Logan graphical method with cerebellum as reference region. In eight unique participants, extrastriatal BP(ND) estimates were compared between Logan graphical methods and a three-compartment kinetic tracer model. Radioactivity and BP(ND) levels were highest in striatum, lower in extrastriatal subcortical regions, and lowest in cortical regions relative to cerebellum. Age negatively correlated with striatal BP(ND) s. BP(ND) estimates for extrastriatal ROIs were highly correlated across kinetic and graphical methods. Our findings indicate that PET with [¹8F]NMB measures specific binding in extrastriatal regions, making it a viable radioligand to study extrastriatal D2R levels in healthy and diseased states.
[Mh] Termos MeSH primário: Bemperidol/análogos & derivados
Encéfalo/diagnóstico por imagem
Tomografia por Emissão de Pósitrons
Receptores de Dopamina D2/metabolismo
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Bemperidol/análise
Cerebelo/diagnóstico por imagem
Córtex Cerebral/diagnóstico por imagem
Corpo Estriado/diagnóstico por imagem
Antagonistas de Dopamina/farmacologia
Antagonistas dos Receptores de Dopamina D2
Feminino
Radioisótopos de Flúor/análise
Seres Humanos
Imagem por Ressonância Magnética
Masculino
Meia-Idade
Especificidade de Órgãos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Dopamine Antagonists); 0 (Dopamine D2 Receptor Antagonists); 0 (Fluorine Radioisotopes); 0 (Receptors, Dopamine D2); 133066-70-3 (N-methylbenperidol); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:1211
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120427
[St] Status:MEDLINE
[do] DOI:10.1002/syn.21566


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[PMID]:21956608
[Au] Autor:Kreuzer P; Landgrebe M; Wittmann M; Schecklmann M; Poeppl TB; Hajak G; Langguth B
[Ad] Endereço:Department of Psychiatry, Psychotherapy and Psychosomatics, University of Regensburg, Regensburg, Germany. peter.kreuzer@medbo.de
[Ti] Título:Hypothermia associated with antipsychotic drug use: a clinical case series and review of current literature.
[So] Source:J Clin Pharmacol;52(7):1090-7, 2012 Jul.
[Is] ISSN:1552-4604
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Hypothermia as an adverse reaction of antipsychotic drug use represents a potentially life-threatening complication. However, the mechanisms by which antipsychotic drugs alter thermoregulatory processes in the human body are far from being fully understood. Here we present a case series of 5 patients developing severe hypothermia after administration of olanzapine and benperidol. Controlled by a network of neural structures, body temperature is physiologically regulated in far more narrow boundaries than are other vital functions, and its homeostasis is critical for survival. The preoptic region in the ventral hypothalamus is assumed to act as a coordinating center that is endowed with thermosensory units that constantly compare actual body temperature with target values and initiate regulatory and compensatory mechanisms in case of mismatch. Hypothermia risk seems to increase in the first days after initiation of antipsychotic drug therapy or increases in the daily dose. Schizophrenic patients bear a higher risk than nonschizophrenic patients treated with antipsychotic drugs (such as patients with dementia or depression). Antipsychotic drugs with strong 5-HT2 antagonism seem to be more frequently associated with hypothermia. These cases demonstrate the clinical relevance of hypothermia as an adverse reaction to antipsychotic treatment and the importance of careful monitoring of body temperature.
[Mh] Termos MeSH primário: Antipsicóticos/efeitos adversos
Hipotermia/induzido quimicamente
Esquizofrenia/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Idoso
Antipsicóticos/administração & dosagem
Antipsicóticos/uso terapêutico
Bemperidol/efeitos adversos
Bemperidol/uso terapêutico
Benzodiazepinas/efeitos adversos
Benzodiazepinas/uso terapêutico
Regulação da Temperatura Corporal/efeitos dos fármacos
Regulação da Temperatura Corporal/fisiologia
Relação Dose-Resposta a Droga
Feminino
Seres Humanos
Hipotermia/fisiopatologia
Masculino
Meia-Idade
Fatores de Risco
Antagonistas do Receptor 5-HT2 de Serotonina/efeitos adversos
Antagonistas do Receptor 5-HT2 de Serotonina/uso terapêutico
Índice de Gravidade de Doença
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Serotonin 5-HT2 Receptor Antagonists); 12794-10-4 (Benzodiazepines); 97O6X78C53 (Benperidol); N7U69T4SZR (olanzapine)
[Em] Mês de entrada:1211
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110930
[St] Status:MEDLINE
[do] DOI:10.1177/0091270011409233


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[PMID]:18355689
[Au] Autor:Antenor-Dorsey JA; Markham J; Moerlein SM; Videen TO; Perlmutter JS
[Ad] Endereço:Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, MO, USA.
[Ti] Título:Validation of the reference tissue model for estimation of dopaminergic D2-like receptor binding with [18F](N-methyl)benperidol in humans.
[So] Source:Nucl Med Biol;35(3):335-41, 2008 Apr.
[Is] ISSN:0969-8051
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Positron emission tomography measurements of dopaminergic D2-like receptors may provide important insights into disorders such as Parkinson's disease, schizophrenia, dystonia and Tourette's syndrome. The positron emission tomography (PET) radioligand [18F](N-methyl)benperidol ([18F]NMB) has high affinity and selectivity for D2-like receptors and is not displaced by endogenous dopamine. The goal of this study is to evaluate the use of a graphical method utilizing a reference tissue region for [18F]-NMB PET analysis by comparisons to an explicit three-compartment tracer kinetic model and graphical method that use arterial blood measurements. We estimated binding potential (BP) in the caudate and putamen using all three methods in 16 humans and found that the three-compartment tracer kinetic method provided the highest BP estimates while the graphical method using a reference region yielded the lowest estimates (P<.0001 by repeated-measures ANOVA). However, the three methods yielded highly correlated BP estimates for the two regions of interest. We conclude that the graphical method using a reference region still provides a useful estimate of BP comparable to methods using arterial blood sampling, especially since the reference region method is less invasive and computationally more straightforward, thereby simplifying these measurements.
[Mh] Termos MeSH primário: Bemperidol/análogos & derivados
Ensaio Radioligante/normas
Receptores de Dopamina D2/química
Processamento de Sinais Assistido por Computador
Técnica de Subtração
[Mh] Termos MeSH secundário: Adulto
Bemperidol/sangue
Bemperidol/química
Bemperidol/farmacocinética
Calibragem
Núcleo Caudado/diagnóstico por imagem
Interpretação Estatística de Dados
Feminino
Radioisótopos de Flúor/sangue
Radioisótopos de Flúor/química
Radioisótopos de Flúor/farmacocinética
Seres Humanos
Análise dos Mínimos Quadrados
Masculino
Taxa de Depuração Metabólica
Meia-Idade
Modelos Teóricos
Tomografia por Emissão de Pósitrons/métodos
Tomografia por Emissão de Pósitrons/normas
Putamen/diagnóstico por imagem
Artéria Radial/diagnóstico por imagem
Ensaio Radioligante/métodos
Compostos Radiofarmacêuticos/sangue
Compostos Radiofarmacêuticos/química
Compostos Radiofarmacêuticos/farmacocinética
Receptores de Dopamina D2/análise
Padrões de Referência
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Fluorine Radioisotopes); 0 (Radiopharmaceuticals); 0 (Receptors, Dopamine D2); 133066-70-3 (N-methylbenperidol); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:0808
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080322
[St] Status:MEDLINE
[do] DOI:10.1016/j.nucmedbio.2007.12.004


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[PMID]:18071701
[Au] Autor:Antenor-Dorsey JA; Laforest R; Moerlein SM; Videen TO; Perlmutter JS
[Ad] Endereço:Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
[Ti] Título:Radiation dosimetry of N-([11C]methyl)benperidol as determined by whole-body PET imaging of primates.
[So] Source:Eur J Nucl Med Mol Imaging;35(4):771-8, 2008 Apr.
[Is] ISSN:1619-7070
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: N-([(11)C]methyl)benperidol ([(11)C]NMB) can be used for positron emission tomography (PET) measurements of D(2)-like dopamine receptor binding in vivo. We report the absorbed radiation dosimetry of i.v.-administered (11)C-NMB, a critical step before applying this radioligand to imaging studies in humans. MATERIALS AND METHODS: Whole-body PET imaging with a CTI/Siemens ECAT 953B scanner was done in a male and a female baboon. After i.v. injection of 444-1221 MBq of (11)C-NMB, sequential images taken from the head to the pelvis were collected for 3 h. Volumes of interest (VOIs) were identified that entirely encompassed small organs (whole brain, striatum, eyes, and myocardium). Large organs (liver, lungs, kidneys, lower large intestine, and urinary bladder) were sampled by drawing representative regions within the organ volume. Time-activity curves for each VOI were extracted from the PET, and organ residence times were calculated by analytical integration of a multi-exponential fit of the time-activity curves. Human radiation doses were estimated using OLINDA/EXM 1.0 and the standard human model. RESULTS: Highest retention was observed in the blood and liver, each with total residence times of 1.5 min. The highest absorbed radiation doses were to the heart (10.5 µGy/MBq) [DOSAGE ERROR CORRECTED] and kidney (9.19 µGy/MBq), [DOSAGE ERROR CORRECTED] making these the critical organs for [(11)C]NMB. A heart absorption of 50 mGy would result from an injected dose of 4,762 MBq [(11)C]NMB. CONCLUSIONS: Thus, this study suggests that up to 4,762 MBq of [(11)C]NMB can be safely administered to human subjects for PET studies. Total body dose and effective dose for [(11)C]NMB are 2.82 µGy/MBq [DOSAGE ERROR CORRECTED] and 3.7 mSv/kBq, respectively.
[Mh] Termos MeSH primário: Bemperidol/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Bemperidol/administração & dosagem
Bemperidol/farmacocinética
Encéfalo/diagnóstico por imagem
Encéfalo/metabolismo
Feminino
Coração/diagnóstico por imagem
Injeções Intravenosas
Fígado/diagnóstico por imagem
Fígado/metabolismo
Masculino
Modelos Animais
Miocárdio/metabolismo
Papio
Tomografia por Emissão de Pósitrons
Receptores de Dopamina D2/metabolismo
Distribuição Tecidual
Irradiação Corporal Total
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Receptors, Dopamine D2); 133066-70-3 (N-methylbenperidol); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:0808
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071212
[St] Status:MEDLINE


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[PMID]:17477341
[Au] Autor:Bender A; Scheiber J; Glick M; Davies JW; Azzaoui K; Hamon J; Urban L; Whitebread S; Jenkins JL
[Ad] Endereço:Lead Finding Platform, Novartis Institutes for BioMedical Research Inc. 250 Massachusetts Ave., Cambridge, Massachusetts 02139, USA. andreas.bender@novartis.com
[Ti] Título:Analysis of pharmacology data and the prediction of adverse drug reactions and off-target effects from chemical structure.
[So] Source:ChemMedChem;2(6):861-73, 2007 Jun.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Preclinical Safety Pharmacology (PSP) attempts to anticipate adverse drug reactions (ADRs) during early phases of drug discovery by testing compounds in simple, in vitro binding assays (that is, preclinical profiling). The selection of PSP targets is based largely on circumstantial evidence of their contribution to known clinical ADRs, inferred from findings in clinical trials, animal experiments, and molecular studies going back more than forty years. In this work we explore PSP chemical space and its relevance for the prediction of adverse drug reactions. Firstly, in silico (computational) Bayesian models for 70 PSP-related targets were built, which are able to detect 93% of the ligands binding at IC(50) < or = 10 microM at an overall correct classification rate of about 94%. Secondly, employing the World Drug Index (WDI), a model for adverse drug reactions was built directly based on normalized side-effect annotations in the WDI, which does not require any underlying functional knowledge. This is, to our knowledge, the first attempt to predict adverse drug reactions across hundreds of categories from chemical structure alone. On average 90% of the adverse drug reactions observed with known, clinically used compounds were detected, an overall correct classification rate of 92%. Drugs withdrawn from the market (Rapacuronium, Suprofen) were tested in the model and their predicted ADRs align well with known ADRs. The analysis was repeated for acetylsalicylic acid and Benperidol which are still on the market. Importantly, features of the models are interpretable and back-projectable to chemical structure, raising the possibility of rationally engineering out adverse effects. By combining PSP and ADR models new hypotheses linking targets and adverse effects can be proposed and examples for the opioid mu and the muscarinic M2 receptors, as well as for cyclooxygenase-1 are presented. It is hoped that the generation of predictive models for adverse drug reactions is able to help support early SAR to accelerate drug discovery and decrease late stage attrition in drug discovery projects. In addition, models such as the ones presented here can be used for compound profiling in all development stages.
[Mh] Termos MeSH primário: Simulação por Computador
Sistemas de Liberação de Medicamentos
Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos
Modelos Químicos
Modelos Moleculares
Preparações Farmacêuticas/química
[Mh] Termos MeSH secundário: Antipsicóticos/efeitos adversos
Antipsicóticos/química
Antipsicóticos/farmacologia
Antipsicóticos/uso terapêutico
Arritmias Cardíacas/induzido quimicamente
Bemperidol/efeitos adversos
Bemperidol/química
Bemperidol/farmacologia
Bemperidol/uso terapêutico
Bases de Dados Factuais
Desenho de Drogas
Avaliação Pré-Clínica de Medicamentos
Ligantes
Valor Preditivo dos Testes
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Ligands); 0 (Pharmaceutical Preparations); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:0809
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070505
[St] Status:MEDLINE


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[PMID]:15846648
[Au] Autor:Leucht S; Hartung B
[Ad] Endereço:Klinik für Psychiatrie und Psychotherapie, Klinikum rechts der Isar der TU-München, Ismaningerstr. 22, München, Germany, 81675. Stefan.Leucht@lrz.tu-muenchen.de
[Ti] Título:Benperidol for schizophrenia.
[So] Source:Cochrane Database Syst Rev;(2):CD003083, 2005 Apr 18.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Benperidol is a relatively old antipsychotic drug that has been marketed since 1966. It has been used in Germany for 30 years, but is also available in Belgium, Greece, Italy, the Netherlands and the UK. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade. Those taking it are therefore reputed to be at high risk of extrapyramidal side effects, but benperidol's unusual profile may render it valuable to subgroups of people with schizophrenia. OBJECTIVES: To examine the clinical effects and safety of benperidol for those with schizophrenia and schizophrenia-like psychoses. SEARCH STRATEGY: We searched the Cochrane Schizophrenia Group's register (November 2004) for this update. SELECTION CRITERIA: We included all randomised controlled trials that compared benperidol with other treatments for people with schizophrenia, or schizophrenia-like psychoses. DATA COLLECTION AND ANALYSIS: We reliably selected studies, quality rated them and extracted data. We independently extracted data but excluded data if loss to follow up was greater than 50%. For dichotomous data, we estimated relative risks (RR), with the 95% confidence intervals (CI). Where possible, we calculated the number needed to treat/harm statistic (NNT/H) and used intention-to-treat analysis. MAIN RESULTS: The update yielded no further studies for inclusion in the review. We identified only one unpublished poorly randomised controlled trial (N=40, duration 30 days, comparison perphenazine). Although benperidol was inferior to perphenazine (1 RCT, N=40, global state no better or worse RR 8.0 CI 2.1 to 30, NNH 1.4 CI 1 to 2) poor reporting suggests that an overestimate of effect is likely. It was not possible to report other outcomes. AUTHORS' CONCLUSIONS: Currently, there are insufficient data from randomised trials to assess the clinical effects of benperidol. This compound merits further research interest.
[Mh] Termos MeSH primário: Antipsicóticos/uso terapêutico
Bemperidol/uso terapêutico
Esquizofrenia/tratamento farmacológico
[Mh] Termos MeSH secundário: Seres Humanos
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Antipsychotic Agents); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:0507
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050423
[St] Status:MEDLINE


  9 / 704 MEDLINE  
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[PMID]:14709957
[Au] Autor:Schönfeldt-Lecuona C; Juengling FD; Connemann BJ; Reske SN; Spitzer M; Kassubek J
[Ti] Título:Complete dopamine D2 receptor occupancy without extrapyramidal side effects under benperidol.
[So] Source:J Clin Psychopharmacol;24(1):97-8, 2004 Feb.
[Is] ISSN:0271-0749
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Bemperidol/uso terapêutico
Di-Hidroxifenilalanina/análogos & derivados
Discinesia Induzida por Medicamentos/prevenção & controle
Receptores de Dopamina D2/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Gânglios da Base/diagnóstico por imagem
Gânglios da Base/efeitos dos fármacos
Gânglios da Base/fisiopatologia
Bemperidol/sangue
Bemperidol/farmacologia
Radioisótopos de Carbono
Clozapina/sangue
Clozapina/farmacologia
Clozapina/uso terapêutico
Discinesia Induzida por Medicamentos/fisiopatologia
Radioisótopos de Flúor
Seres Humanos
Masculino
Racloprida/farmacocinética
Receptores de Dopamina D2/metabolismo
Esquizofrenia/tratamento farmacológico
Tomografia Computadorizada de Emissão/métodos
Resultado do Tratamento
Ultrassonografia
[Pt] Tipo de publicação:CASE REPORTS; LETTER
[Nm] Nome de substância:
0 (Carbon Radioisotopes); 0 (Fluorine Radioisotopes); 0 (Receptors, Dopamine D2); 2C598205QX (fluorodopa F 18); 430K3SOZ7G (Raclopride); 63-84-3 (Dihydroxyphenylalanine); 97O6X78C53 (Benperidol); J60AR2IKIC (Clozapine)
[Em] Mês de entrada:0406
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040108
[St] Status:MEDLINE


  10 / 704 MEDLINE  
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Fotocópia
[PMID]:12679408
[Au] Autor:Nikolaus S; Larisch R; Beu M; Hamacher K; Forutan F; Vosberg H; Müller HW
[Ad] Endereço:Nuklearmedizinische Klinik, Universitätsklinikum Düsseldorf, Moorenstrasse 5, 40225 Düsseldorf, Germany.
[Ti] Título:In vivo measurement of D2 receptor density and affinity for 18F-(3-N-methyl)benperidol in the rat striatum with a PET system for small laboratory animals.
[So] Source:J Nucl Med;44(4):618-24, 2003 Apr.
[Is] ISSN:0161-5505
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:UNLABELLED: A recent investigation showed that intracerebral radioactivity concentrations can reliably be quantified in vivo with a small-animal PET device. The purpose of the current study was to investigate the binding characteristics of the D(2) receptor radioligand (18)F-(3-N-methyl)benperidol ((18)FMB) in rat striatum by determining receptor density (B(max)) and affinity (K(d)) in vivo. For validation, K(d) and B(max) additionally were determined in vitro using storage phosphor autoradiography. METHODS: Striatal radioactivity was measured with PET in 8 Sprague-Dawley rats after injection of (18)FMB in increasing specific activities. Free radioligand concentrations were estimated from cortical radioactivity concentrations and were subtracted from striatal radioactivity concentrations to obtain specific binding. In vitro saturation experiments were performed on 7 further rats according to the isotopic dilution method. Specific binding was determined by both subtraction of (18)FMB binding in the presence of raclopride and subtraction of cortical radioactivity concentrations from total radioligand binding. Saturation binding curves were obtained by plotting specifically bound radioligand concentrations against free radioligand concentrations and were evaluated with regression analysis. RESULTS: PET yielded a K(d) of 6.2 nmol/L and a B(max) of 16 fmol/mg for the striatal D(2) receptor. In vitro, K(d) and B(max) amounted to 4.4 nmol/L and 84.1 fmol/mg (subtraction of (18)FMB binding in the presence of raclopride), respectively, and 7.9 nmol/L and 70.1 fmol/mg (subtraction of cortical radioactivity concentrations), respectively. CONCLUSION: K(d) values measured with PET and autoradiography agreed and corresponded to inhibition constants obtained in previous in vitro studies. B(max) values lay within the same order of magnitude. The results of in vitro saturation binding analyses also agreed, irrespective of the mode of determination of free radioligand concentrations. Thus, B(max) and K(d) may be determined with PET in analogy to the evaluation of in vitro binding data by regression analysis of bound-versus-free ligand concentrations. Our results show that small-animal tomographs are valuable tools for the in vivo characterization of receptor radioligands as an alternative to autoradiography.
[Mh] Termos MeSH primário: Bemperidol/análogos & derivados
Bemperidol/farmacocinética
Corpo Estriado/diagnóstico por imagem
Corpo Estriado/metabolismo
Radioisótopos de Flúor/farmacocinética
Receptores de Dopamina D2/metabolismo
Tomografia Computadorizada de Emissão/métodos
[Mh] Termos MeSH secundário: Animais
Autorradiografia
Estudos de Viabilidade
Masculino
Ratos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Fluorine Radioisotopes); 0 (Receptors, Dopamine D2); 133066-70-3 (N-methylbenperidol); 97O6X78C53 (Benperidol)
[Em] Mês de entrada:0305
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030408
[St] Status:MEDLINE



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