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[PMID]:26996616
[Au] Autor:Borthwick AD
[Ad] Endereço:DrugMolDesign, 15 Temple Grove, London NW11 7UA, United Kingdom.
[Ti] Título:Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases.
[So] Source:Mini Rev Med Chem;17(7):572-582, 2017.
[Is] ISSN:1875-5607
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed. METHOD: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine and acetylcholine in vivo. CONCLUSION: Furthermore, its potential for the treatment of central neurodegenerative diseases is highlighted, in particular its improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's disease.
[Mh] Termos MeSH primário: Adrenérgicos/farmacologia
Sistema Nervoso Central/efeitos dos fármacos
Disfunção Cognitiva/tratamento farmacológico
Descoberta de Drogas
Doenças Neurodegenerativas/tratamento farmacológico
Piperoxano/análogos & derivados
Pirróis/farmacologia
[Mh] Termos MeSH secundário: Adrenérgicos/síntese química
Adrenérgicos/química
Animais
Sistema Nervoso Central/patologia
Disfunção Cognitiva/patologia
Seres Humanos
Doenças Neurodegenerativas/patologia
Piperoxano/síntese química
Piperoxano/química
Piperoxano/farmacologia
Pirróis/síntese química
Pirróis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Adrenergic Agents); 0 (Pyrroles); 9ZCS27634Y (Piperoxan); WGA8E072GX (fluparoxan)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170822
[Lr] Data última revisão:
170822
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160322
[St] Status:MEDLINE
[do] DOI:10.2174/1389557516666160321115041


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[PMID]:20850464
[Au] Autor:Scullion GA; Kendall DA; Marsden CA; Sunter D; Pardon MC
[Ad] Endereço:University of Nottingham Medical School, Institute of Neuroscience, School of Biomedical Sciences, Queen's Medical Centre, Nottingham NG7 2UH, United Kingdom. gillian.scullion@ed.ac.uk
[Ti] Título:Chronic treatment with the α2-adrenoceptor antagonist fluparoxan prevents age-related deficits in spatial working memory in APP×PS1 transgenic mice without altering ß-amyloid plaque load or astrocytosis.
[So] Source:Neuropharmacology;60(2-3):223-34, 2011 Feb-Mar.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Locus coeruleus degeneration and reduced central noradrenaline content is an early feature of Alzheimer's disease. In transgenic mouse models of Alzheimer's disease-like pathology, lesioning the locus coeruleus exacerbates ß-amyloid (Aß) pathology, neuroinflammation and memory deficits. Here we aimed to determine whether chronic treatment with the α(2)-adrenoceptor antagonist fluparoxan, that enhances noradrenaline release, can prevent the onset of Alzheimer's-like pathology and memory deficits in APP/PS1 transgenic mice (TASTPM). Fluparoxan (1mg/kg/day) was administered to TASTPM and wild type mice from 4 to 8 months of age. Memory was assessed at 4 and 8 months of age using the Morris water maze and contextual fear conditioning and at monthly intervals during the duration of treatment using the object recognition and spontaneous alternation task. Aß plaque load and astrocytosis were measured at 4 and 8 months of age by immunohistochemistry. Fluparoxan treatment prevented age-related spatial working memory deficits in the spontaneous alternation task but not spatial reference memory deficits in the Morris water maze. Aß plaque load and astrocytosis were unaltered by fluparoxan treatment in TASTPM mice. The findings suggest that fluparoxan treatment selectively prevent the decline of forms of memory where noradrenaline plays an integral role and that this beneficial effect is not due to altered Aß plaque pathology or astrocytosis.
[Mh] Termos MeSH primário: Antagonistas de Receptores Adrenérgicos alfa 2/administração & dosagem
Envelhecimento
Peptídeos beta-Amiloides/biossíntese
Gliose/tratamento farmacológico
Transtornos da Memória/prevenção & controle
Piperoxano/análogos & derivados
Placa Amiloide/tratamento farmacológico
Pirróis/administração & dosagem
[Mh] Termos MeSH secundário: Envelhecimento/genética
Envelhecimento/metabolismo
Envelhecimento/patologia
Peptídeos beta-Amiloides/genética
Precursor de Proteína beta-Amiloide/biossíntese
Precursor de Proteína beta-Amiloide/genética
Animais
Astrócitos/efeitos dos fármacos
Astrócitos/metabolismo
Astrócitos/patologia
Gliose/genética
Gliose/metabolismo
Seres Humanos
Estudos Longitudinais
Transtornos da Memória/genética
Transtornos da Memória/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Transgênicos
Piperoxano/administração & dosagem
Placa Amiloide/genética
Placa Amiloide/metabolismo
Presenilina-1/biossíntese
Presenilina-1/genética
Receptores Adrenérgicos alfa 2/fisiologia
Resultado do Tratamento
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic alpha-2 Receptor Antagonists); 0 (Amyloid beta-Peptides); 0 (Amyloid beta-Protein Precursor); 0 (Presenilin-1); 0 (Pyrroles); 0 (Receptors, Adrenergic, alpha-2); 9ZCS27634Y (Piperoxan); WGA8E072GX (fluparoxan)
[Em] Mês de entrada:1111
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100921
[St] Status:MEDLINE
[do] DOI:10.1016/j.neuropharm.2010.09.002


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[PMID]:14561692
[Au] Autor:Viemari JC; Bévengut M; Coulon P; Hilaire G
[Ad] Endereço:Centre National de la Recherche Scientifique, Université de la Méditerranée, Groupe d'Etude des Réseaux Moteurs, Biologie des Rythmes et du Développement, 13009 Marseille, France.
[Ti] Título:Nasal trigeminal inputs release the A5 inhibition received by the respiratory rhythm generator of the mouse neonate.
[So] Source:J Neurophysiol;91(2):746-58, 2004 Feb.
[Is] ISSN:0022-3077
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Experiments were performed on neonatal mice to analyze why, in vitro, the respiratory rhythm generator (RRG) was silent and how it could be activated. We demonstrated that in vitro the RRG in intact brain stems is silenced by a powerful inhibition arising from the pontine A5 neurons through medullary alpha(2) adrenoceptors and that in vivo nasal trigeminal inputs facilitate the RRG as nasal continuous positive airway pressure increases the breathing frequency, whereas nasal occlusion and nasal afferent anesthesia depress it. Because nasal trigeminal afferents project to the A5 nuclei, we applied single trains of negative electric shocks to the trigeminal nerve in inactive ponto-medullary preparations. They induced rhythmic phrenic bursts during the stimulation and for 2-3 min afterward, whereas repetitive trains produced on-going rhythmic activity up to the end of the experiments. Electrolytic lesion or pharmacological inactivation of the ipsilateral A5 neurons altered both the phrenic burst frequency and occurrence after the stimulation. Extracellular unitary recordings and trans-neuronal tracing experiments with the rabies virus show that the medullary lateral reticular area contains respiratory-modulated neurons, not necessary for respiratory rhythmogenesis, but that may provide an excitatory pathway from the trigeminal inputs to the RRG as their electrolytic lesion suppresses any phrenic activity induced by the trigeminal nerve stimulation. The results lead to the hypothesis that the trigeminal afferents in the mouse neonate involve at least two pathways to activate the RRG, one that may act through the medullary lateral reticular area and one that releases the A5 inhibition received by the RRG.
[Mh] Termos MeSH primário: Cavidade Nasal/fisiologia
Inibição Neural/fisiologia
Mecânica Respiratória/fisiologia
Nervo Trigêmeo/fisiologia
[Mh] Termos MeSH secundário: Vias Aferentes/efeitos dos fármacos
Vias Aferentes/fisiologia
Animais
Animais Recém-Nascidos
Estimulação Elétrica/métodos
Camundongos
Cavidade Nasal/efeitos dos fármacos
Inibição Neural/efeitos dos fármacos
Piperoxano/farmacologia
Mecânica Respiratória/efeitos dos fármacos
Nervo Trigêmeo/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
9ZCS27634Y (Piperoxan)
[Em] Mês de entrada:0403
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:031017
[St] Status:MEDLINE


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[PMID]:14656145
[Au] Autor:Thome BM; Ivory CF
[Ad] Endereço:Department of Chemical Engineering, Washington State University, 118 Dana Hall, Pullman, Washington 99164-2710, USA.
[Ti] Título:Development of a segmented model for a continuous electrophoretic moving bed enantiomer separation.
[So] Source:Biotechnol Prog;19(6):1703-12, 2003 Nov-Dec.
[Is] ISSN:8756-7938
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:With the recent demonstration of a continuous electrophoretic "moving bed" enantiomer separation at mg/h throughputs, interest has now turned to scaling up the process for use as a benchtop pharmaceutical production tool. To scale the method, a steady-state mathematical model was developed that predicts the process response to changes in input feed rate and counterflow or "moving bed" velocities. The vortex-stabilized apparatus used for the separation was modeled using four regions based on the different hydrodynamic flows in each section. Concentration profiles were then derived on the basis of the properties of the Piperoxan-sulfated beta-cyclodextrin system being studied. The effects of different regional flow rates on the concentration profiles were evaluated and used to predict the maximum processing rate and the hydrodynamic profiles required for a separation. Although the model was able to qualitatively predict the shapes of the concentration profiles and show where the theoretical limits of operation existed, it was not able to quantitatively match the data from actual enantiomer separations to better than 50% accuracy. This is believed to be due to the simplifying assumptions involved, namely, the neglect of electric field variations and the lack of a competitive binding isotherm in the analysis. Although the model cannot accurately predict concentrations from a separation, it provides a good theoretical framework for analyzing how the process responds to changes in counterflow rate, feed rate, and the properties of the molecules being separated.
[Mh] Termos MeSH primário: Eletroquímica/instrumentação
Eletroquímica/métodos
Eletroforese/instrumentação
Eletroforese/métodos
Microfluídica/métodos
Modelos Químicos
Piperoxano/química
Piperoxano/isolamento & purificação
[Mh] Termos MeSH secundário: Simulação por Computador
Projeto Auxiliado por Computador
Desenho de Equipamento/métodos
Análise de Falha de Equipamento/métodos
Microfluídica/instrumentação
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
[Pt] Tipo de publicação:COMPARATIVE STUDY; EVALUATION STUDIES; JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
9ZCS27634Y (Piperoxan)
[Em] Mês de entrada:0408
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:031206
[St] Status:MEDLINE


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[PMID]:11534728
[Au] Autor:Gratz SR; Schneiderman E; Mertens TR; Stalcup AM
[Ad] Endereço:Forensic Chemistry Center, FDA, Cincinnati, Ohio 45237-3097, USA.
[Ti] Título:Use of dyes to investigate migration of the chiral selector in CFFE and the impact on the chiral separations.
[So] Source:Anal Chem;73(16):3999-4005, 2001 Aug 15.
[Is] ISSN:0003-2700
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Continuous free flow electrophoresis was investigated as a tool for the preparative chiral separation of piperoxan enantiomers using sulfated beta-cyclodextrin (sbeta-CD) as the chiral additive. Bulk migration of sbeta-CD was confirmed using LC-MS analysis of the individual fractions collected and visualized with the addition of crystal violet to the separation buffer. In the absence of sbeta-CD, the crystal violet-containing buffer was reddish/purple and the crystal violet was deflected cathodically in the chamber. In the presence of sbeta-CD, the crystal violet-containing buffer was blue and was deflected anodically. However, formation of accumulation and depletion zones was apparent in both cases. The addition of sbeta-CD to the cathodic wash solution allowed for almost complete resolution of the piperoxan enantiomers with a processing rate of 0.45 mg/ h.
[Mh] Termos MeSH primário: Corantes/química
Eletroforese Capilar/métodos
Piperoxano/química
beta-Ciclodextrinas
[Mh] Termos MeSH secundário: Ciclodextrinas/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Coloring Agents); 0 (Cyclodextrins); 0 (beta-Cyclodextrins); 9ZCS27634Y (Piperoxan); JV039JZZ3A (betadex)
[Em] Mês de entrada:0109
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:010906
[St] Status:MEDLINE


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[PMID]:11070539
[Au] Autor:Stalcup AM; Sutton RM; Painuly P; Rodrigo JV; Gratz SR; Yanes EG
[Ad] Endereço:Department of Chemistry, University of Cincinnati, OH 45221-0172, USA.
[Ti] Título:Continuous free flow electrophoresis for preparative chiral separations of piperoxan using sulfated beta-cyclodextrin.
[So] Source:Analyst;125(10):1719-24, 2000 Oct.
[Is] ISSN:0003-2654
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Continuous free flow electrophoresis was investigated as a tool for the preparative chiral separation of piperoxan using a sulfated cyclodextrin chiral additive. In the absence of chiral additive, the sample stream was deflected cathodically. However, the presence of sulfated cyclodextrin in the run buffer caused anodic deflection and splitting of the sample stream into two streams, each enriched in one enantiomer. Although the sulfated cyclodextrin used was comprised of a mixture of homologues and isomers, this polydispersity did not seem to significantly impact band dispersion. Sample introduction rates ranged from approximately 0.9-7.2 mg h-1. Maximum resolution was 0.53, using an applied voltage of 220 V, buffer composition of 0.075% sulfated cyclodextrin, 7.6 mM citrate (pH 3), 4.5 degrees C.
[Mh] Termos MeSH primário: Antagonistas Adrenérgicos alfa/isolamento & purificação
Piperoxano/isolamento & purificação
beta-Ciclodextrinas
[Mh] Termos MeSH secundário: Ciclodextrinas
Eletroforese/métodos
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Adrenergic alpha-Antagonists); 0 (Cyclodextrins); 0 (beta-Cyclodextrins); 9ZCS27634Y (Piperoxan); JV039JZZ3A (betadex)
[Em] Mês de entrada:0011
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:001109
[St] Status:MEDLINE


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[PMID]:10611634
[Au] Autor:Millan MJ; Newman-Tancredi A; Audinot V; Cussac D; Lejeune F; Nicolas JP; Cogé F; Galizzi JP; Boutin JA; Rivet JM; Dekeyne A; Gobert A
[Ad] Endereço:Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125, Chemin de Ronde, 78290-Croissy-sur-Seine, Paris, France.
[Ti] Título:Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.
[So] Source:Synapse;35(2):79-95, 2000 Feb.
[Is] ISSN:0887-4476
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Herein, we evaluate the interaction of the alpha(2)-AR antagonist, yohimbine, as compared to fluparoxan, at multiple monoaminergic receptors and examine their roles in the modulation of adrenergic, dopaminergic and serotonergic transmission in freely-moving rats. Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors. In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites. In vivo, agonist actions of yohimbine at 5-HT(1A) sites are revealed by WAY100,635-reversible induction of hypothermia in the rat. In guinea pigs, antagonist actions of yohimbine at 5-HT(1B) receptors are revealed by blockade of hypothermia evoked by the 5-HT(1B) agonist, GR46,611. In distinction to yohimbine, fluparoxan shows only modest partial agonist actions at h5-HT(1A) sites versus marked antagonist actions at halpha(2)-ARs. While fluparoxan selectively enhances hippocampal noradrenaline (NAD) turnover, yohimbine also enhances striatal dopamine (DA) turnover and suppresses striatal turnover of 5-HT. Further, yohimbine decreases firing of serotonergic neurones in raphe nuclei, an action reversed by WAY100,635. Fluparoxan increases extracellular levels of DA and NAD, but not 5-HT, in frontal cortex. In analogy, yohimbine enhances FCX levels of DA and NAD, yet suppresses those of 5-HT, the latter effect being antagonized by WAY100,635. The induction by fluoxetine of FCX levels of 5-HT, DA, and NAD is potentiated by fluparoxan. Yohimbine likewise facilitates the influence of fluoxetine upon DA and NAD levels, but not those of 5-HT. In conclusion, the alpha(2)-AR antagonist properties of yohimbine increase DA and NAD levels both alone and in association with fluoxetine. However, in contrast to the selective alpha(2)-AR antagonist, fluparoxan, the 5-HT(1A) agonist actions of yohimbine suppress 5-HT levels alone and underlie its inability to augment the influence of fluoxetine upon 5-HT levels.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos alfa 2
Lobo Frontal/fisiologia
Piperoxano/análogos & derivados
Pirróis/farmacologia
Receptores de Dopamina D2/fisiologia
Receptores de Serotonina/fisiologia
Transmissão Sináptica/fisiologia
Ioimbina/farmacologia
[Mh] Termos MeSH secundário: Antagonistas de Receptores Adrenérgicos alfa 2
Antagonistas Adrenérgicos alfa/farmacologia
Animais
Antidepressivos/farmacologia
Temperatura Corporal/efeitos dos fármacos
Lobo Frontal/efeitos dos fármacos
Cobaias
Hipocampo/efeitos dos fármacos
Hipocampo/fisiologia
Seres Humanos
Camundongos
Neurônios/efeitos dos fármacos
Neurônios/fisiologia
Piperoxano/farmacologia
Ratos
Receptor 5-HT1B de Serotonina
Receptor 5-HT1D de Serotonina
Receptores de Dopamina D2/efeitos dos fármacos
Receptores de Dopamina D3
Receptores de Serotonina/efeitos dos fármacos
Receptores 5-HT1 de Serotonina
Suínos
Transmissão Sináptica/efeitos dos fármacos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-2 Receptor Agonists); 0 (Adrenergic alpha-2 Receptor Antagonists); 0 (Adrenergic alpha-Antagonists); 0 (Antidepressive Agents); 0 (DRD3 protein, human); 0 (Drd3 protein, mouse); 0 (Drd3 protein, rat); 0 (HTR1B protein, human); 0 (Pyrroles); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptor, Serotonin, 5-HT1D); 0 (Receptors, Dopamine D2); 0 (Receptors, Dopamine D3); 0 (Receptors, Serotonin); 0 (Receptors, Serotonin, 5-HT1); 2Y49VWD90Q (Yohimbine); 9ZCS27634Y (Piperoxan); WGA8E072GX (fluparoxan)
[Em] Mês de entrada:0002
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:991228
[St] Status:MEDLINE


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[PMID]:10340630
[Au] Autor:Béïque JC; de Montigny C; Blier P; Debonnel G
[Ad] Endereço:Department of Psychiatry, McGill University, Montréal, Québec, Canada.
[Ti] Título:Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.
[So] Source:Synapse;32(3):198-211, 1999 Jun 01.
[Is] ISSN:0887-4476
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Using an in vivo electrophysiological paradigm, venlafaxine and paroxetine displayed similar potency for suppressing the firing activity of dorsal raphe 5-HT neurons (ED50: 233 and 211 microg/kg i.v., respectively), while venlafaxine was three times less potent than desipramine (ED50: 727 and 241 microg/kg i.v., respectively) to suppress the firing activity of locus coeruleus NE neurons. The selective 5-HT1A receptor antagonist WAY 100635 (100 microg/kg, i.v.) reversed the suppressant effect of venlafaxine and paroxetine on the firing activity of 5-HT neurons and the alpha2-adrenoceptor antagonist piperoxane (1 mg/kg, i.v.) reversed those of venlafaxine and desipramine on the firing activity of NE neurons. The ED50 of venlafaxine on the firing activity of 5-HT neurons was not altered (ED50: 264 microg/kg) in noradrenergic-lesioned rats, while the suppressant effect of venlafaxine on the firing activity of NE neurons was greater in serotonergic-lesioned rats (ED50: 285 microg/kg). Taken together, these results suggest that, in vivo, venlafaxine blocks both reuptake processes, its potency to block the 5-HT reuptake process being greater than that for NE. Since the affinities of venlafaxine for the 5-HT and NE reuptake carriers are not in keeping with its potencies for suppressing the firing activity of 5-HT and NE neurons, the suppressant effect of venlafaxine on the firing activity of 5-HT and NE neurons observed in vivo may not be mediated solely by its action on the [3H]cyanoimipramine and [3H]nisoxetine binding sites. In an attempt to unravel the mechanism responsible for this peculiarity, in vitro superfusion experiments were carried out in rat brain slices to assess a putative monoamine releasing property for venlafaxine. (+/-)Fenfluramine and tyramine substantially increased the spontaneous outflow of [3H]5-HT and [3H]NE, respectively, while venlafaxine was devoid of such releasing properties.
[Mh] Termos MeSH primário: Inibidores da Captação Adrenérgica/farmacologia
Cicloexanóis/farmacologia
Neurônios/efeitos dos fármacos
Norepinefrina/metabolismo
Inibidores da Captação de Serotonina/farmacologia
Serotonina/metabolismo
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Inibidores da Captação Adrenérgica/antagonistas & inibidores
Inibidores da Captação Adrenérgica/metabolismo
Animais
Sítios de Ligação
Cicloexanóis/antagonistas & inibidores
Cicloexanóis/metabolismo
Desipramina/antagonistas & inibidores
Desipramina/metabolismo
Desipramina/farmacologia
Fenfluramina/metabolismo
Fenfluramina/farmacologia
Hipocampo/efeitos dos fármacos
Hipocampo/metabolismo
Técnicas In Vitro
Locus Cerúleo/citologia
Locus Cerúleo/efeitos dos fármacos
Locus Cerúleo/metabolismo
Masculino
Neurônios/metabolismo
Neurônios/fisiologia
Paroxetina/antagonistas & inibidores
Paroxetina/metabolismo
Paroxetina/farmacologia
Piperazinas/farmacologia
Piperoxano/farmacologia
Piridinas/farmacologia
Núcleos da Rafe/citologia
Núcleos da Rafe/efeitos dos fármacos
Núcleos da Rafe/metabolismo
Ratos
Ratos Sprague-Dawley
Inibidores da Captação de Serotonina/antagonistas & inibidores
Inibidores da Captação de Serotonina/metabolismo
Tiramina/metabolismo
Tiramina/farmacologia
Cloridrato de Venlafaxina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Adrenergic Uptake Inhibitors); 0 (Cyclohexanols); 0 (Piperazines); 0 (Pyridines); 0 (Serotonin Uptake Inhibitors); 2DS058H2CF (Fenfluramine); 333DO1RDJY (Serotonin); 41VRH5220H (Paroxetine); 71IH826FEG (N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide); 7D7RX5A8MO (Venlafaxine Hydrochloride); 9ZCS27634Y (Piperoxan); TG537D343B (Desipramine); X4W3ENH1CV (Norepinephrine); X8ZC7V0OX3 (Tyramine)
[Em] Mês de entrada:9907
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:990526
[St] Status:MEDLINE


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Fotocópia
[PMID]:9830161
[Au] Autor:Sutton RM; Gratz SR; Stalcup AM
[Ad] Endereço:Department of Chemistry, University of Cincinnati, OH 45221-0172, USA.
[Ti] Título:Use of capillary electrophoresis as a method development tool for classical gel electrophoresis.
[So] Source:Analyst;123(7):1477-80, 1998 Jul.
[Is] ISSN:0003-2654
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Capillary electrophoresis (CE) was used to optimize the buffer pH, ionic strength and sulfated cyclodextrin concentrations for enantiomeric separation of piperoxan. These enantioseparation conditions were then applied to a classical gel electrophoresis system. Binding constants of the sulfated beta-cyclodextrin-piperoxan couple were approximated using CE and the effects of organic solvents on the system were also investigated.
[Mh] Termos MeSH primário: Eletroforese Capilar
[Mh] Termos MeSH secundário: Tampões (Química)
Eletroforese
Isomerismo
Piperoxano/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Buffers); 9ZCS27634Y (Piperoxan)
[Em] Mês de entrada:9812
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:981127
[St] Status:MEDLINE


  10 / 153 MEDLINE  
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Fotocópia
[PMID]:9186739
[Au] Autor:Bricola A; Jurkiewicz NH; Jurkiewicz A
[Ad] Endereço:Department of Pharmacology, Escola Paulista de Medicina, Federal University of São Paulo, Brazil.
[Ti] Título:Functional study of the excitatory alpha-adrenoceptor in guinea pig ileum, in relation to the hypothesis of an atypical receptor.
[So] Source:Ann N Y Acad Sci;812:189-92, 1997 May 30.
[Is] ISSN:0077-8923
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Agonistas alfa-Adrenérgicos/farmacologia
Antagonistas Adrenérgicos alfa/farmacologia
Íleo/metabolismo
Modelos Biológicos
Receptores Adrenérgicos alfa/metabolismo
[Mh] Termos MeSH secundário: Agonistas alfa-Adrenérgicos/administração & dosagem
Antagonistas Adrenérgicos alfa/administração & dosagem
Animais
Dioxanos
Epinefrina/administração & dosagem
Epinefrina/farmacologia
Cobaias
Íleo/efeitos dos fármacos
Indoramina/administração & dosagem
Indoramina/farmacologia
Contração Muscular/efeitos dos fármacos
Norepinefrina/administração & dosagem
Norepinefrina/farmacologia
Fenilefrina/administração & dosagem
Fenilefrina/farmacologia
Piperoxano/administração & dosagem
Piperoxano/farmacologia
Prazosina/administração & dosagem
Prazosina/farmacologia
Receptores Adrenérgicos alfa/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic alpha-Agonists); 0 (Adrenergic alpha-Antagonists); 0 (Dioxanes); 0 (Receptors, Adrenergic, alpha); 0Z802HMY7H (Indoramin); 1WS297W6MV (Phenylephrine); 9ZCS27634Y (Piperoxan); E9H51OIT2B ((2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane); X4W3ENH1CV (Norepinephrine); XM03YJ541D (Prazosin); YKH834O4BH (Epinephrine)
[Em] Mês de entrada:9707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970530
[St] Status:MEDLINE



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