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[PMID]:28466071
[Au] Autor:Walton JC; McNeill JK; Oliver KA; Albers HE
[Ad] Endereço:Neuroscience Institute and Center for Behavioral Neuroscience, Georgia State University, Atlanta, GA 30303.
[Ti] Título:Temporal Regulation of GABA Receptor Subunit Expression: Role in Synaptic and Extrasynaptic Communication in the Suprachiasmatic Nucleus.
[So] Source:eNeuro;4(2), 2017 Mar-Apr.
[Is] ISSN:2373-2822
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Recent molecular studies suggest that the expression levels of δ and γ2 GABA receptor (GABA R) subunits regulate the balance between synaptic and extrasynaptic GABA neurotransmission in multiple brain regions. We investigated the expression of GABA δ and GABA γ2 and the functional significance of a change in balance between these subunits in a robust local GABA network contained within the suprachiasmatic nucleus of the hypothalamus (SCN). Muscimol, which can activate both synaptic and extrasynaptic GABA Rs, injected into the SCN during the day phase advanced the circadian pacemaker, whereas injection of the extrasynaptic GABA superagonist 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) had no effect on circadian phase. In contrast, injection of either THIP or muscimol during the night was sufficient to block the phase shifting effects of light. Gene expression analysis of the whole SCN revealed different temporal patterns in GABA δ and GABA γ2 mRNA expression. When examined across all subregions of the SCN, quantitative immunohistochemical analysis found no significant variations in GABA δ protein immunoreactivity (IR) but did find significant variations in GABA γ2 protein-IR in hamsters housed in either LD cycles or in constant darkness. Remarkably, significant interactions in the ratio of GABA δ:GABA γ2 subunits between lighting condition and circadian phase occurred only within one highly discrete anatomical area of the SCN; a region that functions as the input for lighting information from the retina. Taken together, these data support the hypothesis that the balance between synaptic and extrasynaptic GABA Rs determines the functional response to GABA, and that this balance is differentially regulated in a region-specific manner.
[Mh] Termos MeSH primário: Receptores de GABA-A/metabolismo
Núcleo Supraquiasmático/metabolismo
[Mh] Termos MeSH secundário: Animais
Ritmo Circadiano/efeitos dos fármacos
Ritmo Circadiano/fisiologia
Agonistas GABAérgicos/farmacologia
Masculino
Receptores de GABA-A/efeitos dos fármacos
Núcleo Supraquiasmático/efeitos dos fármacos
Sinapses/efeitos dos fármacos
Sinapses/metabolismo
Transmissão Sináptica/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (GABA Agonists); 0 (Receptors, GABA-A)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE


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[PMID]:29184207
[Au] Autor:Jaepel J; Hübener M; Bonhoeffer T; Rose T
[Ad] Endereço:Synapses - Circuits - Plasticity, Max Planck Institute of Neurobiology, Martinsried, Germany.
[Ti] Título:Lateral geniculate neurons projecting to primary visual cortex show ocular dominance plasticity in adult mice.
[So] Source:Nat Neurosci;20(12):1708-1714, 2017 Dec.
[Is] ISSN:1546-1726
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Experience-dependent plasticity in the mature visual system is widely considered to be cortical. Using chronic two-photon Ca imaging of thalamic afferents in layer 1 of binocular visual cortex, we provide evidence against this tenet: the respective dorsal lateral geniculate nucleus (dLGN) cells showed pronounced ocular dominance (OD) shifts after monocular deprivation in adult mice. Most (86%), but not all, of dLGN cell boutons were monocular during normal visual experience. Following deprivation, initially deprived-eye-dominated boutons reduced or lost their visual responsiveness to that eye and frequently became responsive to the non-deprived eye. This cannot be explained by eye-specific cortical changes propagating to dLGN via cortico-thalamic feedback because the shift in dLGN responses was largely resistant to cortical inactivation using the GABA receptor agonist muscimol. Our data suggest that OD shifts observed in the binocular visual cortex of adult mice may at least partially reflect plasticity of eye-specific inputs onto dLGN neurons.
[Mh] Termos MeSH primário: Dominância Ocular/fisiologia
Corpos Geniculados/citologia
Corpos Geniculados/fisiologia
Plasticidade Neuronal/fisiologia
Neurônios/fisiologia
Córtex Visual/citologia
Córtex Visual/fisiologia
[Mh] Termos MeSH secundário: Animais
Cegueira/patologia
Retroalimentação Sensorial/fisiologia
Agonistas GABAérgicos/farmacologia
Corpos Geniculados/efeitos dos fármacos
Masculino
Camundongos
Muscimol/farmacologia
Plasticidade Neuronal/efeitos dos fármacos
Neurônios/efeitos dos fármacos
Neurônios Aferentes/fisiologia
Tálamo/citologia
Tálamo/fisiologia
Visão Binocular/fisiologia
Vias Visuais/citologia
Vias Visuais/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (GABA Agonists); 2763-96-4 (Muscimol)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171212
[Lr] Data última revisão:
171212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171130
[St] Status:MEDLINE
[do] DOI:10.1038/s41593-017-0021-0


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[PMID]:28822350
[Au] Autor:Liu J; Wang LN
[Ad] Endereço:Department of Neurology, Xuanwu Hospital, Capital Medical University, Changchun Street 45, Beijing, China, 100053.
[Ti] Título:Baclofen for alcohol withdrawal.
[So] Source:Cochrane Database Syst Rev;8:CD008502, 2017 08 20.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Baclofen shows potential for rapidly reducing symptoms of severe alcohol withdrawal syndrome (AWS) in people with alcoholism. Treatment with baclofen is easy to manage and rarely produces euphoria or other pleasant effects, or craving for the drug. This is an updated version of the original Cochrane Review published in 2015, Issue 4. OBJECTIVES: To assess the efficacy and safety of baclofen for people with AWS. SEARCH METHODS: We updated our searches of the following databases to March 2017: the Cochrane Drugs and Alcohol Group Specialised Register, CENTRAL, PubMed, Embase, and CINAHL. We also searched registers of ongoing trials. We handsearched the references quoted in the identified trials, and sought information from researchers, pharmaceutical companies, and relevant trial authors about unpublished or uncompleted trials. We placed no restrictions on language. SELECTION CRITERIA: We included all randomised controlled clinical trials (RCTs) evaluating baclofen versus placebo or any other treatment for people with AWS. We excluded uncontrolled, non-randomised, or quasi-randomised trials. We included both parallel group and cross-over studies. DATA COLLECTION AND ANALYSIS: We used standard methodological procedures expected by Cochrane. MAIN RESULTS: We included three RCTs with 141 randomised participants. We did not perform meta-analyses due to the different control interventions. For the comparison of baclofen and placebo (1 study, 31 participants), there was no significant difference in Clinical Institute Withdrawal Assessment of Alcohol Scale, Revised (CIWA-Ar) scores (very low quality evidence). For the comparison of baclofen and diazepam (1 study, 37 participants), there was no significant difference in CIWA-Ar scores (very low quality evidence), adverse events (risk difference (RD) 0.00, 95% confidence interval (CI) -0.10 to 0.10; very low quality evidence), dropouts (RD 0.00, 95% CI -0.10 to 0.10; very low quality evidence), and dropouts due to adverse events (RD 0.00, 95% CI -0.10 to 0.10; very low quality evidence). For the comparison of baclofen and chlordiazepoxide (1 study, 60 participants), there was no significant difference in CIWA-Ar scores (mean difference (MD) 1.00, 95% CI 0.70 to 1.30; very low quality evidence), global improvement (MD 0.10, 95% CI -0.03 to 0.23; very low quality evidence), adverse events (RD 2.50, 95% CI 0.88 to 7.10; very low quality of evidence), dropouts (RD 0.00, 95% CI -0.06 to 0.06; very low quality evidence), and dropouts due to adverse events (RD 0.00, 95% CI -0.06 to 0.06; very low quality evidence). AUTHORS' CONCLUSIONS: No conclusions can be drawn about the efficacy and safety of baclofen for the management of alcohol withdrawal because we found insufficient and very low quality evidence.
[Mh] Termos MeSH primário: Transtornos Induzidos por Álcool/tratamento farmacológico
Baclofeno/uso terapêutico
Clordiazepóxido/uso terapêutico
Diazepam/uso terapêutico
Agonistas GABAérgicos/uso terapêutico
Síndrome de Abstinência a Substâncias/tratamento farmacológico
[Mh] Termos MeSH secundário: Baclofeno/efeitos adversos
Clordiazepóxido/efeitos adversos
Diazepam/efeitos adversos
Etanol/efeitos adversos
Agonistas GABAérgicos/efeitos adversos
Seres Humanos
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (GABA Agonists); 3K9958V90M (Ethanol); 6RZ6XEZ3CR (Chlordiazepoxide); H789N3FKE8 (Baclofen); Q3JTX2Q7TU (Diazepam)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170820
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD008502.pub5


  4 / 3897 MEDLINE  
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[PMID]:28790148
[Au] Autor:Shin DJ; Germann AL; Steinbach JH; Akk G
[Ad] Endereço:Department of Anesthesiology (D.J.S., A.L.G., J.H.S., G.A.), and the Taylor Family Institute for Innovative Psychiatric Research (J.H.S., G.A.), Washington University School of Medicine in St. Louis, St. Louis, Missouri.
[Ti] Título:The Actions of Drug Combinations on the GABA Receptor Manifest as Curvilinear Isoboles of Additivity.
[So] Source:Mol Pharmacol;92(5):556-563, 2017 Nov.
[Is] ISSN:1521-0111
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Drug interactions are often analyzed in terms of isobolograms. In the isobologram, the line connecting the axial points corresponding to the concentrations of two different drugs that produce an effect of the same magnitude is termed an isobole of additivity. Although the isobole of additivity can be a straight line in some special cases, previous work has proposed that it is curvilinear when the two drugs differ in their maximal effects or Hill slopes. Modulators of transmitter-gated ion channels have a wide range of maximal effects as well as Hill slopes, suggesting that the isoboles for drug actions on ion channel function are not linear. In this study, we have conducted an analysis of direct activation and potentiation of the human 1 2 2L GABA receptor to demonstrate that: 1) curvilinear isoboles of additivity are predicted by a concerted transition model where the binding of each GABAergic drug additively and independently reduces the free energy of the open receptor compared with the closed receptor; and 2) experimental data for receptor activation using the agonist pair of GABA and propofol or potentiation of responses to a low concentration of GABA by the drug pair of alfaxalone and propofol agree very well with predictions. The approach assuming independent energetic contributions from GABAergic drugs enables, at least for the drug combinations tested, a straightforward method to accurately predict functional responses to any combination of concentrations.
[Mh] Termos MeSH primário: Agonistas GABAérgicos/metabolismo
Propofol/metabolismo
Receptores de GABA-A/metabolismo
Ácido gama-Aminobutírico/metabolismo
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação/fisiologia
Relação Dose-Resposta a Droga
Combinação de Medicamentos
Feminino
Agonistas GABAérgicos/administração & dosagem
Seres Humanos
Propofol/administração & dosagem
Xenopus laevis
Ácido gama-Aminobutírico/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Combinations); 0 (GABA Agonists); 0 (Receptors, GABA-A); 56-12-2 (gamma-Aminobutyric Acid); YI7VU623SF (Propofol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171102
[Lr] Data última revisão:
171102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170810
[St] Status:MEDLINE
[do] DOI:10.1124/mol.117.109595


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[PMID]:28642232
[Au] Autor:Kumar M; Kumar M; Freund JM; Dillon GH
[Ad] Endereço:Department of Physiology and Pharmacology, Center for Neuroscience, Robert C. Byrd Health Sciences Center, West Virginia University, Morgantown, West Virginia (Mo.K., Mi.K., J.M.F., G.H.D.); and Center for Neuroscience Discovery, Institute for Healthy Aging, University of North Texas Health Science
[Ti] Título:A Single Amino Acid Residue at Transmembrane Domain 4 of the Subunit Influences Carisoprodol Direct Gating Efficacy at GABA Receptors.
[So] Source:J Pharmacol Exp Ther;362(3):395-404, 2017 Sep.
[Is] ISSN:1521-0103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The muscle relaxant carisoprodol has recently been controlled at the federal level as a Schedule IV drug due to its high abuse potential and consequences of misuse, such as withdrawal syndrome, delusions, seizures, and even death. Recent work has shown that carisoprodol can directly gate and allosterically modulate the type A GABA (GABA ) receptor. These actions are subunit-dependent; compared with other GABA receptors, carisoprodol has nominal direct gating effects in 3 2 2 receptors. Here, using site-directed mutagenesis and whole-cell patch-clamp electrophysiology in transiently transfected human embryonic kidney 293 cells, we examined the role of GABA receptor subunit transmembrane domain 4 (TM4) amino acids in direct gating and allosteric modulatory actions of carisoprodol. Mutation of 3 valine at position 440 to leucine (present in the equivalent position in the 1 subunit) significantly increased the direct gating effects of carisoprodol without affecting its allosteric modulatory effects. The corresponding reverse mutation, 1(L415V), decreased carisoprodol direct gating potency and efficacy. Analysis of a series of amino acid mutations at the 415 position demonstrated that amino acid volume correlated positively with carisoprodol efficacy, whereas polarity inversely correlated with carisoprodol efficacy. We conclude that 1(415) of TM4 is involved in the direct gating, but not allosteric modulatory, actions of carisoprodol. In addition, the orientation of alkyl or hydroxyl groups at this position influences direct gating effects. These findings support the likelihood that the direct gating and allosteric modulatory effects of carisoprodol are mediated via distinct binding sites.
[Mh] Termos MeSH primário: Aminoácidos/metabolismo
Carisoprodol/farmacologia
Relaxantes Musculares Centrais/farmacologia
Transporte Proteico/efeitos dos fármacos
Receptores de GABA-A/efeitos dos fármacos
[Mh] Termos MeSH secundário: Substituição de Aminoácidos
Sítios de Ligação/efeitos dos fármacos
Agonistas GABAérgicos/farmacologia
Células HEK293
Seres Humanos
Ativação do Canal Iônico/efeitos dos fármacos
Mutagênese Sítio-Dirigida
Técnicas de Patch-Clamp
Pentobarbital/farmacologia
Receptores de GABA-A/genética
Esteroides/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acids); 0 (GABA Agonists); 0 (Muscle Relaxants, Central); 0 (Receptors, GABA-A); 0 (Steroids); 21925K482H (Carisoprodol); I4744080IR (Pentobarbital)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170902
[Lr] Data última revisão:
170902
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE
[do] DOI:10.1124/jpet.117.242156


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[PMID]:28339742
[Au] Autor:Wang Z; Huang S; Sheng Y; Peng X; Liu H; Jin N; Cai J; Shu Y; Li T; Li P; Fan C; Hu X; Zhang W; Long R; You Y; Huang C; Song Y; Xiang C; Wang J; Yang Y; Liu K
[Ad] Endereço:Department of Geriatrics, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1277 Jiefang Ave, Wuhan 430022, China.
[Ti] Título:Topiramate modulates post-infarction inflammation primarily by targeting monocytes or macrophages.
[So] Source:Cardiovasc Res;113(5):475-487, 2017 Apr 01.
[Is] ISSN:1755-3245
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Aims: Monocytes/macrophages response plays a key role in post-infarction inflammation that contributes greatly to post-infarction ventricular remodelling and cardiac rupture. Therapeutic targeting of the GABAA receptor, which is enriched in monocytes/macrophages but not expressed in the myocardium, may be possible after myocardial infarction (MI). Methods and results: After MI was induced by ligation of the coronary artery, C57BL/6 mice were intraperitoneally administered with one specific agonist or antagonist of the GABAA receptor (topiramate or bicuculline), in the setting of presence or depletion of monocytes/macrophages. Our data showed that within the first 2 weeks after MI, when monocytes/macrophages dominated, in contrast with bicuculline, topiramate treatment significantly reduced Ly-6Chigh monocyte numbers by regulating splenic monocytopoiesis and promoted foetal derived macrophages preservation and conversion of M1 to M2 or Ly-6Chigh to Ly-6Clow macrophage phenotype in the infarcted heart, though GABAAergic drugs failed to affect M1/M2 or Ly-6Chigh/Ly-6Clow macrophage polarization directly. Accordingly, pro-inflammatory activities mediated by M1 or Ly-6Chigh macrophages were decreased and reparative processes mediated by M2 or Ly-6Clow macrophages were augmented. As a result, post-infarction ventricular remodelling was attenuated, as reflected by reduced infarct size and increased collagen density within infarcts. Echocardiographic indices, mortality and rupture rates were reduced. After depletion of monocytes/macrophages by clodronate liposomes, GABAAergic drugs exhibited no effect on cardiac dysfunction and surrogate clinical outcomes. Conclusion: Control of the GABAA receptor activity in monocytes/macrophages can potently modulate post-infarction inflammation. Topiramate emerges as a promising drug, which may be feasible to translate for MI therapy in the future.
[Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia
Frutose/análogos & derivados
Agonistas GABAérgicos/farmacologia
Ventrículos do Coração/efeitos dos fármacos
Macrófagos/efeitos dos fármacos
Monócitos/efeitos dos fármacos
Infarto do Miocárdio/tratamento farmacológico
Miocardite/prevenção & controle
Receptores de GABA/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Antígenos Ly/metabolismo
Colágeno/metabolismo
Modelos Animais de Doenças
Fibrose
Frutose/farmacologia
Ruptura Cardíaca Pós-Infarto/metabolismo
Ruptura Cardíaca Pós-Infarto/fisiopatologia
Ruptura Cardíaca Pós-Infarto/prevenção & controle
Ventrículos do Coração/metabolismo
Ventrículos do Coração/patologia
Ventrículos do Coração/fisiopatologia
Macrófagos/metabolismo
Camundongos Endogâmicos C57BL
Monócitos/metabolismo
Infarto do Miocárdio/metabolismo
Infarto do Miocárdio/patologia
Infarto do Miocárdio/fisiopatologia
Miocardite/metabolismo
Miocardite/patologia
Miocardite/fisiopatologia
Miocárdio/metabolismo
Miocárdio/patologia
Fenótipo
Receptores de GABA/metabolismo
Receptores de GABA-A/efeitos dos fármacos
Receptores de GABA-A/metabolismo
Fatores de Tempo
Disfunção Ventricular Esquerda/metabolismo
Disfunção Ventricular Esquerda/fisiopatologia
Disfunção Ventricular Esquerda/prevenção & controle
Função Ventricular Esquerda/efeitos dos fármacos
Remodelação Ventricular/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antigens, Ly); 0 (GABA Agonists); 0 (Gabra1 protein, mouse); 0 (Gabrb3 protein, mouse); 0 (Ly6 protein, mouse); 0 (Receptors, GABA); 0 (Receptors, GABA-A); 0H73WJJ391 (topiramate); 30237-26-4 (Fructose); 9007-34-5 (Collagen)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170325
[St] Status:MEDLINE
[do] DOI:10.1093/cvr/cvx027


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[PMID]:28275709
[Au] Autor:Hamel L; Thangarasa T; Samadi O; Ito R
[Ad] Endereço:Department of Psychology (Scarborough), University of Toronto , 1265 Military Trail , Toronto, Ontario M1C 1A4, Canada.
[Ti] Título:Caudal Nucleus Accumbens Core Is Critical in the Regulation of Cue-Elicited Approach-Avoidance Decisions.
[So] Source:eNeuro;4(1), 2017 Jan-Feb.
[Is] ISSN:2373-2822
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The nucleus accumbens (NAc) is thought to be a site of integration of positively and negatively valenced information and action selection. Functional differentiation in valence processing has previously been found along the rostrocaudal axis of the shell region of the NAc in assessments of unconditioned motivation. Given that the core region of the NAc has been implicated in the elicitation of motivated behavior in response to conditioned cues, we sought to assess the role of caudal, intermediate, and rostral sites within this subregion in cue-elicited approach-avoidance decisions. Rats were trained to associate visuo-tactile cues with appetitive, aversive, and neutral outcomes. Following the successful acquisition of the cue-outcome associations, rats received microinfusions of GABA and GABA receptor agonists (muscimol/baclofen) or saline into the caudal, intermediate, or rostral NAc core and were then exposed to a superimposition of appetitively and aversively valenced cues versus neutral cues in a "conflict test," as well as to the appetitive versus neutral cues, and aversive cues versus neutral cues, in separate conditioned preference/avoidance tests. Disruption of activity in the intermediate to caudal parts of the NAc core resulted in a robust avoidance bias in response to motivationally conflicting cues, as well as a potentiated avoidance of aversive cues as compared with control animals, coupled with an attenuated conditioned preference for the appetitive cue. These results suggest that the caudal NAc core may have the capacity to exert bidirectional control over appetitively and aversively motivated responses to valence signals.
[Mh] Termos MeSH primário: Aprendizagem da Esquiva/fisiologia
Comportamento de Escolha/fisiologia
Sinais (Psicologia)
Núcleo Accumbens/fisiologia
[Mh] Termos MeSH secundário: Animais
Aprendizagem por Associação/efeitos dos fármacos
Aprendizagem por Associação/fisiologia
Aprendizagem da Esquiva/efeitos dos fármacos
Baclofeno/farmacologia
Comportamento de Escolha/efeitos dos fármacos
Condicionamento (Psicologia)/efeitos dos fármacos
Condicionamento (Psicologia)/fisiologia
Conflito (Psicologia)
Agonistas GABAérgicos/farmacologia
Masculino
Motivação/efeitos dos fármacos
Motivação/fisiologia
Muscimol/farmacologia
Núcleo Accumbens/efeitos dos fármacos
Proteínas Proto-Oncogênicas c-fos/metabolismo
Ratos Long-Evans
Receptores de GABA-A/metabolismo
Receptores de GABA-B/metabolismo
Percepção do Tato/efeitos dos fármacos
Percepção do Tato/fisiologia
Percepção Visual/efeitos dos fármacos
Percepção Visual/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (GABA Agonists); 0 (Proto-Oncogene Proteins c-fos); 0 (Receptors, GABA-A); 0 (Receptors, GABA-B); 2763-96-4 (Muscimol); H789N3FKE8 (Baclofen)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170310
[St] Status:MEDLINE


  8 / 3897 MEDLINE  
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[PMID]:28225161
[Au] Autor:Niquet J; Baldwin R; Suchomelova L; Lumley L; Eavey R; Wasterlain CG
[Ad] Endereço:Department of Neurology, David Geffen School of Medicine at UCLA, Los Angeles, California, U.S.A.
[Ti] Título:Treatment of experimental status epilepticus with synergistic drug combinations.
[So] Source:Epilepsia;58(4):e49-e53, 2017 Apr.
[Is] ISSN:1528-1167
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:During status epilepticus (SE), synaptic γ-aminobutyric acid A receptors (GABA Rs) become internalized and inactive, whereas spare N-methyl-d-aspartate receptors (NMDARs) assemble, move to the membrane, and become synaptically active. When treatment of SE is delayed, the number of synaptic GABA Rs is drastically reduced, and a GABA agonist cannot fully restore inhibition. We used a combination of low-dose diazepam (to stimulate the remaining GABA Rs), ketamine (to mitigate the effect of the NMDAR increase), and valproate (to enhance inhibition at a nonbenzodiazepine site) to treat seizures in a model of severe cholinergic SE. High doses of diazepam failed to stop electrographic SE, showing that benzodiazepine pharmacoresistance had developed. The diazepam-ketamine-valproate combination was far more effective in stopping SE than triple-dose monotherapy using the same individual drugs. Isobolograms showed that this drug combination's therapeutic actions were synergistic, with positive cooperativity between drugs, whereas drug toxicity was simply additive, without positive or negative cooperativity. As a result, the therapeutic index was improved by this drug combination compared to monotherapy. These results suggest that synergistic drug combinations that target receptor changes can control benzodiazepine-refractory SE.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Estado Epiléptico/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Quimioterapia Combinada
Eletrodos Implantados
Eletroencefalografia
Antagonistas de Aminoácidos Excitatórios/uso terapêutico
Agonistas GABAérgicos/uso terapêutico
Masculino
Agonistas Muscarínicos/toxicidade
Pilocarpina/toxicidade
Ratos
Ratos Wistar
Estado Epiléptico/induzido quimicamente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Excitatory Amino Acid Antagonists); 0 (GABA Agonists); 0 (Muscarinic Agonists); 01MI4Q9DI3 (Pilocarpine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170223
[St] Status:MEDLINE
[do] DOI:10.1111/epi.13695


  9 / 3897 MEDLINE  
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[PMID]:28146602
[Au] Autor:Nicholl GC; Jawad AK; Weymouth R; Zhang H; Beg AA
[Ad] Endereço:Department of Pharmacology, University of Michigan, Ann Arbor, MI, USA.
[Ti] Título:Pharmacological characterization of the excitatory 'Cys-loop' GABA receptor family in Caenorhabditis elegans.
[So] Source:Br J Pharmacol;174(9):781-795, 2017 May.
[Is] ISSN:1476-5381
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND PURPOSE: Ionotropic GABA receptors are evolutionarily conserved proteins that mediate cellular and network inhibition in both vertebrates and invertebrates. A unique class of excitatory GABA receptors has been identified in several nematode species. Despite well-characterized functions in Caenorhabditis elegans, little is known about the pharmacology of the excitatory GABA receptors EXP-1 and LGC-35. Using a panel of compounds that differentially activate and modulate ionotropic GABA receptors, we investigated the agonist binding site and allosteric modulation of EXP-1 and LGC-35. EXPERIMENTAL APPROACH: We used two-electrode voltage clamp recordings to characterize the pharmacological profile of EXP-1 and LGC-35 receptors expressed in Xenopus laevis oocytes. KEY RESULTS: The pharmacology of EXP-1 and LGC-35 is different from that of GABA and GABA -ρ receptors. Both nematode receptors are resistant to the competitive orthosteric antagonist bicuculline and to classical ionotropic receptor pore blockers. The GABA -ρ specific antagonist, TPMPA, was the only compound tested that potently inhibited EXP-1 and LGC-35. Neurosteroids have minimal effects on GABA-induced currents, but ethanol selectively potentiates LGC-35. CONCLUSIONS AND IMPLICATIONS: The pharmacological properties of EXP-1 and LGC-35 more closely resemble the ionotropic GABA -ρ family. However, EXP-1 and LGC-35 exhibit a unique profile that differs from vertebrate GABA and GABA -ρ receptors, insect GABA receptors and nematode GABA receptors. As a pair, EXP-1 and LGC-35 may be utilized to further understand the differential molecular mechanisms of agonist, antagonist and allosteric modulation at ionotropic GABA receptors and may aid in the design of new and more specific anthelmintics that target GABA neurotransmission.
[Mh] Termos MeSH primário: Proteínas de Caenorhabditis elegans/agonistas
Proteínas de Caenorhabditis elegans/metabolismo
Receptores de Canais Iônicos de Abertura Ativada por Ligante com Alça de Cisteína/agonistas
Receptores de Canais Iônicos de Abertura Ativada por Ligante com Alça de Cisteína/metabolismo
Receptores de GABA/metabolismo
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação/fisiologia
Caenorhabditis elegans
Proteínas de Caenorhabditis elegans/genética
Receptores de Canais Iônicos de Abertura Ativada por Ligante com Alça de Cisteína/genética
Relação Dose-Resposta a Droga
Feminino
Agonistas GABAérgicos/metabolismo
Agonistas GABAérgicos/farmacologia
Receptores de GABA/genética
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caenorhabditis elegans Proteins); 0 (Cysteine Loop Ligand-Gated Ion Channel Receptors); 0 (EXP-1 protein, C elegans); 0 (GABA Agonists); 0 (LGC-35 protein, C elegans); 0 (Receptors, GABA)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170202
[St] Status:MEDLINE
[do] DOI:10.1111/bph.13736


  10 / 3897 MEDLINE  
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[PMID]:27940054
[Au] Autor:Kunisawa K; Kido K; Nakashima N; Matsukura T; Nabeshima T; Hiramatsu M
[Ad] Endereço:Department of Chemical Pharmacology, Faculty of Pharmacy, Meijo University, Nagoya, Japan.
[Ti] Título:Betaine attenuates memory impairment after water-immersion restraint stress and is regulated by the GABAergic neuronal system in the hippocampus.
[So] Source:Eur J Pharmacol;796:122-130, 2017 Feb 05.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:GABA mediated neuronal system regulates hippocampus-dependent memory and stress responses by controlling plasticity and neuronal excitability. Here, we demonstrate that betaine ameliorates water-immersion restraint stress (WIRS)-induced memory impairments. This improvement was inhibited by a betaine/GABA transporter-1 (GABA transporter-2: GAT2) inhibitor, NNC 05-2090. In this study, we investigated whether memory amelioration by betaine was mediated by the GABAergic neuronal system. Adult male mice were co-administered betaine and GABA receptor antagonists after WIRS. We also examined whether memory impairment after WIRS was attenuated by GABA receptor agonists. The memory functions were evaluated using a novel object recognition test 3-6 days after WIRS and/or the step-down type passive avoidance test at 7-8 days. The co-administration of the GABA receptor antagonist bicuculline (1mg/kg) or the GABA receptor antagonist phaclofen (10mg/kg) 1h after WIRS suppressed the memory-improving effects induced by betaine. Additionally, the administration of the GABA receptor agonist muscimol (1mg/kg) or the GABA receptor agonist baclofen (10mg/kg) 1h after WIRS attenuated memory impairments. These results were similar to the data observed with betaine. The treatment with betaine after WIRS significantly decreased the expression of GABA transaminase, and this effect was partially blocked by NNC 05-2090 in the hippocampus. WIRS caused a transient increase in hippocampal GABA levels and the changes after WIRS were not affected by betaine treatment in an in vivo microdialysis study. These results suggest that the beneficial effects of betaine may be mediated in part by changing the GABAergic neuronal system.
[Mh] Termos MeSH primário: Betaína/farmacologia
Hipocampo/efeitos dos fármacos
Memória/efeitos dos fármacos
Neurônios/efeitos dos fármacos
Estresse Psicológico/patologia
Estresse Psicológico/fisiopatologia
Ácido gama-Aminobutírico/metabolismo
[Mh] Termos MeSH secundário: Animais
Espaço Extracelular/efeitos dos fármacos
Espaço Extracelular/metabolismo
Agonistas GABAérgicos/farmacologia
Antagonistas GABAérgicos/farmacologia
Proteínas da Membrana Plasmática de Transporte de GABA/metabolismo
Hipocampo/patologia
Hipocampo/fisiopatologia
Imersão
Masculino
Camundongos
Neurônios/patologia
Receptores de GABA/metabolismo
Estresse Psicológico/metabolismo
Água
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (GABA Agonists); 0 (GABA Antagonists); 0 (GABA Plasma Membrane Transport Proteins); 0 (Receptors, GABA); 0 (Slc6a12 protein, mouse); 059QF0KO0R (Water); 3SCV180C9W (Betaine); 56-12-2 (gamma-Aminobutyric Acid)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161213
[St] Status:MEDLINE



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