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[PMID]:27539344
[Au] Autor:Liu F; Zhu N; Qiu L; Wang JJ; Wang WH
[Ad] Endereço:Shaanxi Provincal Center for Disease Control and Prevention, Xi'an 710054, China.
[Ti] Título:[Application of R-based multiple seasonal ARIMA model, in predicting the incidence of hand, foot and mouth disease in Shaanxi province].
[So] Source:Zhonghua Liu Xing Bing Xue Za Zhi;37(8):1117-20, 2016 Aug 10.
[Is] ISSN:0254-6450
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:OBJECTIVE: To apply the ' auto-regressive integrated moving average product seasonal model' in predicting the number of hand, foot and mouth disease in Shaanxi province. METHODS: In Shaanxi province, the trend of hand, foot and mouth disease was analyzed and tested, under the use of R software, between January 2009 and June 2015. Multiple seasonal ARIMA model was then fitted under time series to predict the number of hand, foot and mouth disease in 2016 and 2017. RESULTS: Seasonal effect was seen in hand, foot and mouth disease in Shaanxi province. A multiple seasonal ARIMA (2,1,0)×(1,1,0)12 was established, with the equation as (1 -B)(1 -B12)Ln (Xt) =((1-1.000B)/(1-0.532B-0.363B(2))*(1-0.644B12-0.454B12(2)))*Epsilont. The mean of absolute error and the relative error were 531.535 and 0.114, respectively when compared to the simulated number of patients from Jun to Dec in 2015. RESULTS under the prediction of multiple seasonal ARIMA model showed that the numbers of patients in both 2016 and 2017 were similar to that of 2015 in Shaanxi province. CONCLUSION: Multiple seasonal ARIMA (2,1,0)×(1,1,0)12 model could be used to successfully predict the incidence of hand, foot and mouth disease in Shaanxi province.
[Mh] Termos MeSH primário: Doença de Mão, Pé e Boca/epidemiologia
Modelos Estatísticos
Estações do Ano
[Mh] Termos MeSH secundário: China/epidemiologia
Previsões
Seres Humanos
Incidência
Moclobemida
Software
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170111
[Lr] Data última revisão:
170111
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160820
[St] Status:MEDLINE
[do] DOI:10.3760/cma.j.issn.0254-6450.2016.08.013


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[PMID]:27111811
[Au] Autor:Doruyter A; Lochner C; Jordaan GP; Stein DJ; Dupont P; Warwick JM
[Ad] Endereço:Division of Nuclear Medicine, Faculty of Health Sciences, Stellenbosch University, Cape Town, South Africa. Electronic address: doruyter@sun.ac.za.
[Ti] Título:Resting functional connectivity in social anxiety disorder and the effect of pharmacotherapy.
[So] Source:Psychiatry Res;251:34-44, 2016 May 30.
[Is] ISSN:1872-7123
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Neuroimaging research has reported differences in resting-state functional connectivity (RFC) between social anxiety disorder (SAD) patients and healthy controls (HCs). Limited research has examined the effect of treatment on RFC in SAD. We performed a study to identify differences in RFC between SAD and HC groups, and to investigate the effect of pharmacotherapy on RFC in SAD. Seed-based RFC analysis was performed on technetium-99m hexamethylpropylene amine oxime (Tc-99m HMPAO) SPECT scans using a cross-subject approach in SPM-12. Seeds were chosen to represent regions in a recently published network model of SAD. A second-level regression analysis was performed to further characterize the underlying relationships identified in the group contrasts. Twenty-three SAD participants were included, of which 18 underwent follow-up measures after an 8-week course of citalopram or moclobemide. Fifteen healthy control (HC) scans were included. SAD participants at baseline demonstrated several significant connectivity disturbances consistent with the existing network model as well as one previously unreported finding (increased connectivity between cerebellum and posterior cingulate cortex). After therapy, the SAD group demonstrated significant increases in connectivity with dorsal anterior cingulate cortex which may explain therapy-induced modifications in how SAD sufferers interpret emotions in others and improvements in self-related and emotional processing.
[Mh] Termos MeSH primário: Encéfalo/diagnóstico por imagem
Citalopram/uso terapêutico
Moclobemida/uso terapêutico
Fobia Social/diagnóstico por imagem
Fobia Social/tratamento farmacológico
Tomografia Computadorizada de Emissão de Fóton Único/métodos
[Mh] Termos MeSH secundário: Adulto
Antidepressivos/farmacologia
Antidepressivos/uso terapêutico
Encéfalo/efeitos dos fármacos
Encéfalo/fisiologia
Citalopram/farmacologia
Emoções/efeitos dos fármacos
Emoções/fisiologia
Feminino
Giro do Cíngulo/fisiopatologia
Seres Humanos
Masculino
Moclobemida/farmacologia
Neuroimagem/métodos
Fobia Social/psicologia
Descanso/fisiologia
Tecnécio Tc 99m Exametazima
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents); 0DHU5B8D6V (Citalopram); 3B744AG22N (Technetium Tc 99m Exametazime); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160426
[St] Status:MEDLINE


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[PMID]:27053354
[Au] Autor:Nazimek K; Kozlowski M; Bryniarski P; Strobel S; Bryk A; Myszka M; Tyszka A; Kuszmiersz P; Nowakowski J; Filipczak-Bryniarska I
[Ad] Endereço:Department of Immunology, Jagiellonian University Medical College, PL 31-121 Krakow, Poland katarzyna.nazimek@uj.edu.pl.
[Ti] Título:Repeatedly administered antidepressant drugs modulate humoral and cellular immune response in mice through action on macrophages.
[So] Source:Exp Biol Med (Maywood);241(14):1540-50, 2016 Aug.
[Is] ISSN:1535-3699
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Depression is associated with an altered immune response, which could be normalized by antidepressant drugs. However, little is known about the influence of antidepressants on the peripheral immune response and function of macrophages in individuals not suffering from depression. Our studies were aimed at determining the influence of antidepressant drugs on the humoral and cellular immune response in mice. Mice were treated intraperitoneally with imipramine, fluoxetine, venlafaxine, or moclobemide and contact immunized with trinitrophenyl hapten followed by elicitation and measurement of contact sensitivity by ear swelling response. Peritoneal macrophages from drug-treated mice were either pulsed with sheep erythrocytes or conjugated with trinitrophenyl and transferred into naive recipients to induce humoral or contact sensitivity response, respectively. Secretion of reactive oxygen intermediates, nitric oxide, and cytokines by macrophages from drug-treated mice was assessed, respectively, in chemiluminometry, Griess-based colorimetry and enzyme-linked immunosorbent assay, and the expression of macrophage surface markers was analyzed cytometrically. Treatment of mice with fluoxetine, venlafaxine, and moclobemide results in suppression of humoral and cell-mediated immunity with a reduction of the release of macrophage proinflammatory mediators and the expression of antigen-presentation markers. In contrast, treatment with imipramine enhanced the humoral immune response and macrophage secretory activity but slightly suppressed active contact sensitivity. Our studies demonstrated that systemically delivered antidepressant drugs modulate the peripheral humoral and cell-mediated immune responses, mostly through their action on macrophages. Imipramine was rather proinflammatory, whereas other tested drugs expressed immunosuppressive potential. Current observations may be applied to new therapeutic strategies dedicated to various disorders associated with excessive inflammation.
[Mh] Termos MeSH primário: Antidepressivos/farmacologia
Imunidade Celular/efeitos dos fármacos
Imunidade Humoral/efeitos dos fármacos
Macrófagos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Antidepressivos/administração & dosagem
Biomarcadores/metabolismo
Citocinas/secreção
Transtorno Depressivo/imunologia
Dermatite de Contato/imunologia
Fluoxetina/farmacologia
Imipramina/farmacologia
Imunossupressão
Injeções Intraperitoneais
Macrófagos/imunologia
Macrófagos/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos
Moclobemida/farmacologia
Cloridrato de Venlafaxina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidepressive Agents); 0 (Biomarkers); 0 (Cytokines); 01K63SUP8D (Fluoxetine); 7D7RX5A8MO (Venlafaxine Hydrochloride); OGG85SX4E4 (Imipramine); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170614
[Lr] Data última revisão:
170614
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160408
[St] Status:MEDLINE
[do] DOI:10.1177/1535370216643769


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[PMID]:26805819
[Au] Autor:Plenis A; Rekowska N; Baczek T
[Ad] Endereço:Department of Pharmaceutical Chemistry, Medical University of Gdansk, Hallera 107, 80-416 Gdansk, Poland. aplenis@gumed.edu.pl.
[Ti] Título:Column Selection for Biomedical Analysis Supported by Column Classification Based on Four Test Parameters.
[So] Source:Int J Mol Sci;17(1), 2016 Jan 21.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:This article focuses on correlating the column classification obtained from the method created at the Katholieke Universiteit Leuven (KUL), with the chromatographic resolution attained in biomedical separation. In the KUL system, each column is described with four parameters, which enables estimation of the FKUL value characterising similarity of those parameters to the selected reference stationary phase. Thus, a ranking list based on the FKUL value can be calculated for the chosen reference column, then correlated with the results of the column performance test. In this study, the column performance test was based on analysis of moclobemide and its two metabolites in human plasma by liquid chromatography (LC), using 18 columns. The comparative study was performed using traditional correlation of the FKUL values with the retention parameters of the analytes describing the column performance test. In order to deepen the comparative assessment of both data sets, factor analysis (FA) was also used. The obtained results indicated that the stationary phase classes, closely related according to the KUL method, yielded comparable separation for the target substances. Therefore, the column ranking system based on the FKUL-values could be considered supportive in the choice of the appropriate column for biomedical analysis.
[Mh] Termos MeSH primário: Antidepressivos/isolamento & purificação
Cromatografia Líquida de Alta Pressão/instrumentação
Moclobemida/isolamento & purificação
[Mh] Termos MeSH secundário: Antidepressivos/sangue
Cromatografia Líquida de Alta Pressão/métodos
Análise Fatorial
Seres Humanos
Limite de Detecção
Moclobemida/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antidepressive Agents); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160126
[St] Status:MEDLINE


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[PMID]:26537155
[Au] Autor:Smith DM; Fisher D; Blier P; Ilivitsky V; Knott V
[Ad] Endereço:University of Ottawa Institute of Mental Health Research, Ottawa, ON, Canada Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, ON, Canada dylan.m.smith@gmail.com.
[Ti] Título:The separate and combined effects of monoamine oxidase A inhibition and nicotine on resting state EEG.
[So] Source:J Psychopharmacol;30(1):56-62, 2016 Jan.
[Is] ISSN:1461-7285
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:While nicotine is often associated with the neuropsychological effects of tobacco smoke, the robust monoamine oxidase (MAO) inhibition observed in chronic smokers is also likely to play a role. Electroencephalographically-indexed alterations in baseline neural oscillations by nicotine have previously been reported in both smokers and non-smokers, however, little is known about the effects of MAO inhibition in combination with nicotine on resting state EEG. In a sample of 24 healthy non-smoking males, the effects of 6 mg nicotine gum, as well as MAO-A inhibition via 75 mg moclobemide, were investigated in separate and combined conditions over four separate test sessions. Drug effects were observed in the alpha2, beta2, and theta band frequencies. Nicotine increased alpha2 power, and moclobemide decreased beta2 power. Theta power was decreased most robustly by the combination of both drugs. Therefore, this study demonstrated that the nicotinic and MAO inhibiting properties of tobacco may differentially influence fast-wave oscillations (alpha2 and beta2), while acting in synergy to influence theta oscillations.
[Mh] Termos MeSH primário: Moclobemida/farmacologia
Inibidores da Monoaminoxidase/farmacologia
Nicotina/farmacologia
Agonistas Nicotínicos/farmacologia
[Mh] Termos MeSH secundário: Estudos Cross-Over
Método Duplo-Cego
Interações Medicamentosas
Sinergismo Farmacológico
Eletroencefalografia
Seres Humanos
Masculino
Moclobemida/administração & dosagem
Inibidores da Monoaminoxidase/administração & dosagem
Nicotina/administração & dosagem
Agonistas Nicotínicos/administração & dosagem
Produtos para o Abandono do Uso de Tabaco
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Monoamine Oxidase Inhibitors); 0 (Nicotinic Agonists); 6M3C89ZY6R (Nicotine); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151225
[Lr] Data última revisão:
151225
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151106
[St] Status:MEDLINE
[do] DOI:10.1177/0269881115613518


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[PMID]:26404738
[Au] Autor:Stuhec M; Oravecz R
[Ad] Endereço:Department for Clinical Pharmacy, Psychiatric Hospital Ormoz, Ptujska Cesta 33, Ormoz, Slovenia. matejstuhec@gmail.com.
[Ti] Título:Moclobemide as add-on therapy to agomelatine in a patient with treatment-resistant major depressive disorder: a psychopharmacological case.
[So] Source:Wien Klin Wochenschr;128(7-8):295-8, 2016 Apr.
[Is] ISSN:1613-7671
[Cp] País de publicação:Austria
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Treatment-resistant depression is a major depressive disorder that does not respond to adequate treatment of at least two antidepressants and is one of the major clinical challenges for clinicians and clinical pharmacists. One treatment option is to switch the patient to a different medication. Another option is to add a medication to the patient's current pharmacotherapy. This article presents an improvement of symptoms induced by a combination of moclobemide (MOC) and agomelatine (AG) treatment in a 48-year-old Caucasian woman with treatment-resistant major depressive disorder (MDD). The patient had been treated with numerous antidepressants in the last 2 years that had not been effective or had caused serious adverse effects. When MOC 300 mg daily was added to AG 25 mg daily, the patient recovered progressively without any adverse effects. Her functional status also appeared stable. No other drugs known to interact with AG were administered. The MOC dose was subsequently increased to 600 mg daily and was taken with AG 25 mg daily and zolpidem 5 mg daily. DISCUSSION: The positive effects of AG or MOC on MDD have been widely reported, but there have not been reports of a combined treatment with MOG and AG improving symptoms of treatment-resistant MDD. The exact mechanism of this effect on the central nervous system is unknown. The additive activity could have been caused by a broader spectrum activity of AG and MOC. CONCLUSION: In this report, we identified a case with positive evidence of this antidepressant combination relieving the symptoms of treatment-resistant MDD, which is otherwise difficult to manage. This case report may serve to help clinicians and clinical pharmacists as a new treatment option for treatment-resistant MDD, although further research is needed to confirm this practice.
[Mh] Termos MeSH primário: Acetamidas/administração & dosagem
Antidepressivos/administração & dosagem
Transtorno Depressivo Maior/diagnóstico
Transtorno Depressivo Maior/tratamento farmacológico
Moclobemida/administração & dosagem
[Mh] Termos MeSH secundário: Transtorno Depressivo Maior/psicologia
Relação Dose-Resposta a Droga
Resistência a Medicamentos
Quimioterapia Combinada
Feminino
Seres Humanos
Hipnóticos e Sedativos/administração & dosagem
Meia-Idade
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetamides); 0 (Antidepressive Agents); 0 (Hypnotics and Sedatives); 138112-76-2 (S 20098); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171011
[Lr] Data última revisão:
171011
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150926
[St] Status:MEDLINE
[do] DOI:10.1007/s00508-015-0861-0


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[PMID]:26428872
[Au] Autor:Suthar SK; Bansal S; Alam MM; Jaiswal V; Tiwari A; Chaudhary A; Alex AT; Joseph A
[Ad] Endereço:Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal 576104, India.
[Ti] Título:Design, synthesis, and biological evaluation of oxindole derivatives as antidepressive agents.
[So] Source:Bioorg Med Chem Lett;25(22):5281-5, 2015 Nov 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The 3-substituted oxindole derivatives were designed, synthesized, and evaluated for antidepressant activity by employing forced swimming test, tail suspension test, and MAO-A inhibition assay. Results of biological studies revealed that the majority of compounds exhibited potent to moderately potent activity and among them, 12 displayed potency comparable to that of the imipramine with %DID of 37.95 and 44.84 in the FST and TST, respectively. At the same time, imipramine showed %DID of 43.62 and 50.64 in the FST and TST, correspondingly. In the MAO-A inhibition assay, 12 showed an IC50 of 18.27 µmol, whereas the reference drug moclobemide displayed an IC50 of 13.1 µmol. The SAR study disclosed that the presence of bromo atom at the phenyl/furanyl or thienyl moiety in the oxindole derivatives was critical for the antidepressant activity.
[Mh] Termos MeSH primário: Antidepressivos/química
Compostos de Benzilideno/química
Indóis/química
Lactamas/química
Inibidores da Monoaminoxidase/química
[Mh] Termos MeSH secundário: Animais
Antidepressivos/síntese química
Antidepressivos/farmacologia
Compostos de Benzilideno/síntese química
Compostos de Benzilideno/farmacologia
Clorgilina/farmacologia
Imipramina/farmacologia
Indóis/síntese química
Indóis/farmacologia
Lactamas/síntese química
Lactamas/farmacologia
Camundongos
Moclobemida/farmacologia
Simulação de Acoplamento Molecular
Monoaminoxidase/metabolismo
Inibidores da Monoaminoxidase/síntese química
Inibidores da Monoaminoxidase/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-(4-bromobenzylidene)indolin-2-one); 0 (Antidepressive Agents); 0 (Benzylidene Compounds); 0 (Indoles); 0 (Lactams); 0 (Monoamine Oxidase Inhibitors); EC 1.4.3.4 (Monoamine Oxidase); EC 1.4.3.4. (monoamine oxidase A, human); LYJ16FZU9Q (Clorgyline); OGG85SX4E4 (Imipramine); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:151031
[Lr] Data última revisão:
151031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151003
[St] Status:MEDLINE


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[PMID]:26316187
[Au] Autor:Chiuccariello L; Cooke RG; Miler L; Levitan RD; Baker GB; Kish SJ; Kolla NJ; Rusjan PM; Houle S; Wilson AA; Meyer JH
[Ad] Endereço:CAMH Research Imaging Centre and Campbell Family Mental Health Research Institute, Centre for Addiction and Mental Health and Departments of Psychiatry, Pharmacology and Toxicology, and Institute of Medical Sciences, University of Toronto, Canada (Drs Chiuccariello, Cooke, Levitan, Kish, Kolla, Rusj
[Ti] Título:Monoamine Oxidase-A Occupancy by Moclobemide and Phenelzine: Implications for the Development of Monoamine Oxidase Inhibitors.
[So] Source:Int J Neuropsychopharmacol;19(1), 2015 Aug 27.
[Is] ISSN:1469-5111
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Monoamine oxidase inhibitors (MAOIs) are being developed for major depressive disorder, Alzheimer's, and Parkinson's Disease. Newer MAOIs have minimal sensitivity to tyramine, but a key limitation for optimizing their development is that standards for in vivo monoamine oxidase-A (MAO-A) occupancy in humans are not well established. The objectives were to determine the dose-occupancy relationship of moclobemide and the occupancy of phenelzine at typical clinical dosing. METHODS: Major depressive episode (MDE) subjects underwent [(11)C]harmine positron emission tomography scanning prior to and following 6 weeks of treatment with moclobemide or phenelzine. RESULTS: Mean brain MAO-A occupancies were 74.23±8.32% for moclobemide at 300-600 mg daily (n = 11), 83.75±5.52% for moclobemide at 900-1200 mg daily (n = 9), and 86.82±6.89% for phenelzine at 45-60 mg daily (n = 4). The regional dose-occupancy relationship of moclobemide fit a hyperbolic function [F(x) = a(x/[b + x]); F(1,18) = 5.57 to 13.32, p = 0.002 to 0.03, mean 'a': 88.62±2.38%, mean 'b': 69.88±4.36 mg]. Multivariate analyses of variance showed significantly greater occupancy of phenelzine (45-60mg) and higher-dose moclobemide (900-1200 mg) compared to lower-dose moclobemide [300-600 mg; F(7,16) = 3.94, p = 0.01]. CONCLUSIONS: These findings suggest that for first-line MDE treatment, daily moclobemide doses of 300-600mg correspond to a MAO-A occupancy of 74%, whereas for treatment-resistant MDE, either phenelzine or higher doses of moclobemide correspond to a MAO-A occupancy of at least 84%. Therefore, novel MAO inhibitor development should aim for similar thresholds. The findings provide a rationale in treatment algorithm design to raise moclobemide doses to inhibit more MAO-A sites, but suggest switching from high-dose moclobemide to phenelzine is best justified by binding to additional targets.
[Mh] Termos MeSH primário: Encéfalo/efeitos dos fármacos
Moclobemida/farmacologia
Inibidores da Monoaminoxidase/farmacocinética
Monoaminoxidase/metabolismo
Fenelzina/farmacologia
[Mh] Termos MeSH secundário: Adulto
Encéfalo/diagnóstico por imagem
Isótopos de Carbono/farmacocinética
Relação Dose-Resposta a Droga
Feminino
Harmina/farmacocinética
Voluntários Saudáveis
Seres Humanos
Masculino
Meia-Idade
Análise Multivariada
Tomografia por Emissão de Pósitrons
Ligação Proteica/efeitos dos fármacos
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Carbon Isotopes); 0 (Monoamine Oxidase Inhibitors); 4FHH5G48T7 (Harmine); EC 1.4.3.4 (Monoamine Oxidase); O408N561GF (Phenelzine); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150829
[St] Status:MEDLINE


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[PMID]:26293971
[Au] Autor:Evranos-Aksöz B; Baysal I; Yabanoglu-Çiftçi S; Djikic T; Yelekçi K; Uçar G; Ertan R
[Ad] Endereço:Analysis and Control Laboratories of General Directorate of Pharmaceuticals and Pharmacy, Ministry of Health of Turkey, Sihhiye, Ankara, Turkey.
[Ti] Título:Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives.
[So] Source:Arch Pharm (Weinheim);348(10):743-56, 2015 Oct.
[Is] ISSN:1521-4184
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A group of 3,5-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds have a pyrazoline structure, nine of these original compounds have a hydrazone structure, and one of these original compounds has a chalcone structure. Structural elucidation of the compounds was performed by IR, (1)H NMR, (13)C NMR, mass spectral data, and elemental analyses. These compounds were tested for their inhibitory activities toward the A and B isoforms of human monoamine oxidase (MAO). Except for 3k and 6c, all compounds were found to be competitive, reversible, and selective inhibitors for either one of the isoforms (hMAO-A or MAO-B). Compounds 3k and 6c were found to be competitive, reversible, but non-selective MAO inhibitors. Compound 6h showed hMAO-B inhibitory activity whereas the others potently inhibited hMAO-A. Compound 5c showed higher selectivity than the standard drug moclobemide. According to the experimental K(i) values, compounds 6i, 6d, and 6a exhibited the highest inhibitory activity toward hMAO-A. The AutoDock 4.2 program was employed to perform automated molecular docking. The calculated results obtained computationally were in good agreement with the experimental values.
[Mh] Termos MeSH primário: Hidrazonas/síntese química
Hidrazonas/farmacologia
Inibidores da Monoaminoxidase/síntese química
Inibidores da Monoaminoxidase/farmacologia
Monoaminoxidase/metabolismo
Pirazóis/síntese química
Pirazóis/farmacologia
[Mh] Termos MeSH secundário: Desenho de Drogas
Seres Humanos
Cinética
Moclobemida/farmacologia
Simulação de Acoplamento Molecular
Monoaminoxidase/química
Conformação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Hydrazones); 0 (Monoamine Oxidase Inhibitors); 0 (Pyrazoles); EC 1.4.3.4 (Monoamine Oxidase); EC 1.4.3.4. (monoamine oxidase A, human); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150822
[St] Status:MEDLINE
[do] DOI:10.1002/ardp.201500212


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[PMID]:26226350
[Au] Autor:Smith DM; Fisher D; Blier P; Ilivitsky V; Knott V
[Ad] Endereço:University of Ottawa Institute of Mental Health Research, Ottawa, Ontario, Canada; Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, Ontario, Canada. Electronic address: dylan.m.smith@gmail.com.
[Ti] Título:The separate and combined effects of monoamine oxidase A inhibition and nicotine on the mismatch negativity event related potential.
[So] Source:Pharmacol Biochem Behav;137:44-52, 2015 Oct.
[Is] ISSN:1873-5177
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The mismatch negativity (MMN) auditory event-related potential (ERP) has been extensively studied as a potential biomarker for abnormal auditory processing in schizophrenia (SZ), a population which exhibits abnormally high smoking rates. The relationship between nicotinic activation and cognition in SZ may be related to underlying nicotinic and NMDA receptor dysfunction within the disease. However, transient cognitive improvements via smoking in patients may also result from monoamine oxidase (MAO) inhibition, achieved through tobacco smoke. In 24 healthy non-smoking males, we investigated the separate and combined effects of nicotine and MAO-A inhibition via moclobemide (75mg) on the optimal-5 variation of the MMN paradigm. No significant drug effects were observed in our total sample, however, stratification of individuals into low (N=12) and high (N=12) baseline MMN amplitude groups revealed increases in duration MMN amplitude relative to placebo by nicotine, as well as moclobemide, but not after the combination of the two. Because previous research has shown there was no effect of monoamine modulation on MMN, this study shows an unexpected effect of moclobemide on duration MMN.
[Mh] Termos MeSH primário: Potenciais Evocados/efeitos dos fármacos
Moclobemida/administração & dosagem
Inibidores da Monoaminoxidase/administração & dosagem
Monoaminoxidase
Nicotina/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Estudos Cross-Over
Método Duplo-Cego
Combinação de Medicamentos
Potenciais Evocados/fisiologia
Seres Humanos
Masculino
Monoaminoxidase/metabolismo
Estimulação Luminosa/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Drug Combinations); 0 (Monoamine Oxidase Inhibitors); 6M3C89ZY6R (Nicotine); EC 1.4.3.4 (Monoamine Oxidase); EC 1.4.3.4. (monoamine oxidase A, human); PJ0Y7AZB63 (Moclobemide)
[Em] Mês de entrada:1606
[Cu] Atualização por classe:150911
[Lr] Data última revisão:
150911
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150731
[St] Status:MEDLINE



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