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  1 / 2015 MEDLINE  
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[PMID]:28470123
[Au] Autor:Dojo K; Yamaguchi Y; Fustin JM; Doi M; Kobayashi M; Okamura H
[Ad] Endereço:Department of Systems Biology, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto, Japan.
[Ti] Título:Carbachol Induces Phase-dependent Phase Shifts of Per1 Transcription Rhythms in Cultured Suprachiasmatic Nucleus Slices.
[So] Source:J Biol Rhythms;32(2):101-108, 2017 Apr.
[Is] ISSN:1552-4531
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Among nonphotic stimulants, a classic cholinergic agonist, carbachol, is known to have a strong and unique phase-resetting effect on the circadian clock: Intracerebroventricular carbachol treatment causes phase delays during the subjective early night and phase advances in the subjective late night, but the effects of this drug on the suprachiasmatic nucleus (SCN) in vivo and in vitro are still controversial. In the present study, we succeeded in reproducing the biphasic phase-shifting effect of carbachol on clock gene expression in organotypic SCN slices prepared from mice carrying a Per1-promoter fused luciferase gene ( Per1-luc). Since this biphasic effect of carbachol in Per1-luc SCN was prevented by atropine but not by mecamylamine, we concluded that these phase shifts were muscarinic receptor-dependent. Next, we analyzed the expression of muscarinic receptors in the SCN by in situ hybridization and found that M3 and M4 subtypes were expressed in SCN cells. These signals appeared neonatally and reached adult levels at postnatal day 10. Together, these findings suggest that carbachol has a phase-dependent phase-shifting effect on the SCN clock through muscarinic receptor subtypes expressed in the SCN.
[Mh] Termos MeSH primário: Carbacol/farmacologia
Agonistas Colinérgicos/farmacologia
Ritmo Circadiano/efeitos dos fármacos
Proteínas Circadianas Period/genética
Núcleo Supraquiasmático/efeitos dos fármacos
Núcleo Supraquiasmático/fisiologia
Transcrição Genética
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Atropina/farmacologia
Relógios Circadianos/efeitos dos fármacos
Expressão Gênica
Luciferases/genética
Mecamilamina/farmacologia
Camundongos
Atividade Motora
Antagonistas Muscarínicos/farmacologia
Antagonistas Nicotínicos/farmacologia
Técnicas de Cultura de Órgãos
Regiões Promotoras Genéticas
Receptores Muscarínicos/genética
Receptores Muscarínicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Muscarinic Antagonists); 0 (Nicotinic Antagonists); 0 (Per1 protein, mouse); 0 (Period Circadian Proteins); 0 (Receptors, Muscarinic); 6EE945D3OK (Mecamylamine); 7C0697DR9I (Atropine); 8Y164V895Y (Carbachol); EC 1.13.12.- (Luciferases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180126
[Lr] Data última revisão:
180126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE
[do] DOI:10.1177/0748730417691205


  2 / 2015 MEDLINE  
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[PMID]:29283235
[Au] Autor:Silkis IG; Makechiv VA
[Ti] Título:Possible Mechanisms of Influence of Various Concentrations of Acetylcholine on Hippocampal Functioning.
[So] Source:Usp Fiziol Nauk;47(4):57-75, 2016 Oct-Dec.
[Is] ISSN:0301-1798
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Analysis of features of influence of acetylcholine on the hippocampal functioning was performed basing on the modulation rules for the efficacy of excitatory and inhibitory synaptic transmission we earlier proposed, and also on the known data about location of pre- and postsynaptic muscarine and nicotinic receptors. According to these rules, activation of postsynaptic muscarine М1/М3 and nicotinic receptors should promote long-term potentiation of excitatory and depressions (LTD) of inhibitory input to a neuron, whereas action on М2/М4 receptors should promote LTD of excitatory input and a decrease in neuromodulator release. If inhibitory input is stronger than excitatory, LTP (LTD) of excitatory input to the interneuron should promote LTD (LTP) of excitatory input to a target cell. It follows from the proposed mechanism that a lowing concentration of acetylcholine in the hippocampus, a decrease in density of М1/ М3 and a4p2 receptors, and augmenting binding of М2 receptors must lead to a depression of responses of pyramidal neurons in СА3 and СА1 fields to signals from the entorhinal cortex. Thereof, interaction of the semantic information, stored in the cortex, with the information of an episode-, stored in the hippocampus must be hindered and this effect can underlie disturbances of recall of stored information at Alzheimer's disease.
[Mh] Termos MeSH primário: Acetilcolina/farmacologia
Doença de Alzheimer/metabolismo
Agonistas Colinérgicos/farmacologia
Hipocampo/efeitos dos fármacos
Potenciação de Longa Duração/efeitos dos fármacos
Depressão Sináptica de Longo Prazo/efeitos dos fármacos
[Mh] Termos MeSH secundário: Acetilcolina/metabolismo
Doença de Alzheimer/genética
Doença de Alzheimer/fisiopatologia
Animais
Agonistas Colinérgicos/metabolismo
Córtex Entorrinal/efeitos dos fármacos
Córtex Entorrinal/fisiologia
Regulação da Expressão Gênica
Hipocampo/fisiologia
Seres Humanos
Potenciação de Longa Duração/fisiologia
Depressão Sináptica de Longo Prazo/fisiologia
Neurônios/citologia
Neurônios/efeitos dos fármacos
Neurônios/metabolismo
Receptores Muscarínicos/genética
Receptores Muscarínicos/metabolismo
Receptores Nicotínicos/genética
Receptores Nicotínicos/metabolismo
Sinapses/efeitos dos fármacos
Sinapses/fisiologia
Transmissão Sináptica/efeitos dos fármacos
Transmissão Sináptica/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Receptors, Muscarinic); 0 (Receptors, Nicotinic); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171229
[St] Status:MEDLINE


  3 / 2015 MEDLINE  
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[PMID]:29283233
[Au] Autor:Tsirkin VI; Nozdrachev AD; Sizova EN; Polezhaeva TV; Khlybova SV
[Ti] Título:Endogenous Sensitizer of Beta-Adrenergic Receptors (ESBAR) as a Component of Humoral Links Element of Autonomic Nervous System and Its Analogs (Review).
[So] Source:Usp Fiziol Nauk;47(4):18-42, 2016 Oct-Dec.
[Is] ISSN:0301-1798
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Kirov State Medical Academy, Kirov The results of the 20-years studies of the presence in blood serum and other body fluids of endogenous modulators of adrenergic and M-cholinergic impact a A COMPONENT of humoral element of autonomic nervous system. The article is devoted to the endogenous sensitizer of beta-adrenergic receptor (ESBAR) - water-soluble low molecular weight substances, analogues of which are histidine, tryptophan, tyrosine, mildronat and preduktal. It is shown, that separate dilutions of human serum and animal (as a source of ESBAR) and ESBAR - analogues ways to enhance the effectiveness of activation of beta-adrenoceptors (AR) of smooth muscle (uterus, coronary and renal arteries, trachea, stomach), myocardium and erythrocytes and platelets (respectively influenced of histidine and tryptophan). It is reported? that content of ESBAR in human serum (according to the titers of its dilution) depends on the sex and the presence of somatic diseases, and at women are also on the stage of reproduction and obstetric complications It is discussed hossible mechanisms of ESBAR action, its physiological role, including as a component of beta-adrenoreceptor myometrium inhibitory mechanism, as well as the prospect of the use of analogues ESBAR, including for the prevention of preterm labor, and for the treatment of bronchial asthma, coronary heart disease, hypertension and heart failure.
[Mh] Termos MeSH primário: Agonistas Adrenérgicos/uso terapêutico
Sistema Nervoso Autônomo/efeitos dos fármacos
Agonistas Colinérgicos/uso terapêutico
Insuficiência Cardíaca/prevenção & controle
Músculo Liso/efeitos dos fármacos
Trabalho de Parto Prematuro/prevenção & controle
[Mh] Termos MeSH secundário: Agonistas Adrenérgicos/sangue
Asma/tratamento farmacológico
Asma/metabolismo
Asma/fisiopatologia
Sistema Nervoso Autônomo/metabolismo
Sistema Nervoso Autônomo/fisiopatologia
Agonistas Colinérgicos/sangue
Doença das Coronárias/tratamento farmacológico
Doença das Coronárias/metabolismo
Doença das Coronárias/fisiopatologia
Feminino
Insuficiência Cardíaca/metabolismo
Insuficiência Cardíaca/fisiopatologia
Histidina/sangue
Histidina/uso terapêutico
Seres Humanos
Hipertensão/tratamento farmacológico
Hipertensão/metabolismo
Hipertensão/fisiopatologia
Metilidrazinas/uso terapêutico
Músculo Liso/metabolismo
Músculo Liso/fisiopatologia
Trabalho de Parto Prematuro/metabolismo
Trabalho de Parto Prematuro/fisiopatologia
Gravidez
Triptofano/sangue
Triptofano/uso terapêutico
Tirosina/sangue
Tirosina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Adrenergic Agonists); 0 (Cholinergic Agonists); 0 (Methylhydrazines); 42HK56048U (Tyrosine); 4QD397987E (Histidine); 73H7UDN6EC (3-(2,2,2-trimethylhydrazine)propionate); 8DUH1N11BX (Tryptophan)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180116
[Lr] Data última revisão:
180116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171229
[St] Status:MEDLINE


  4 / 2015 MEDLINE  
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[PMID]:29215244
[Au] Autor:Khnychenko LK; Okunevich IV; Losev NA; Sapronov NS
[Ti] Título:[Hypolipidemic activity of N-cholinergic antagonist Benzohexonium in the experiments ].
[So] Source:Patol Fiziol Eksp Ter;60(1):36-43, 2016 Jan-Mar.
[Is] ISSN:0031-2991
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:Methods: Experiments were carried out on outbred albino male rats (n = 150, 230-250 g). For modeling dislipoproteinemia (DLP) we used 3 models: single intraperitoneal injection of the detergent triton WR-1339; administration of ethanol; maintenance on a special hypercholesterolaemic diet (HD) during 21 days. Animals were divided into four groups: normal control, model group, gemfibrozil (Gfb) group, benzohexonium (Benz) group. Rats received per os benzohexonium (20mg/kg), reference drug gemfibrozil (50 mg/kg). We determined content of total cholesterol (TCh), triglycerides (TG) in samples of blood serum and liver, TCh in aorta. TCh, TG and Ch-HDL were analyzed spectrophotometrically using of standardized methods. Results: Compared with model group the contents of TCh, TG in serum and liver were significantly decreased in model + Benz group, whereas Ch-HDL was raised in rats fed special HD (P<0.05). Calculated index of atherogenity (TCh - Ch-HDL) / (Ch-HDL) showed the positive effect. Conclusion: The results obtained were shown the hypolipidemic activity of N-cholinergic antagonist Benzohexonium (20 mg/kg) lowered the content of lipids in blood, liver, and aorta.
[Mh] Termos MeSH primário: Agonistas Colinérgicos
Dislipidemias
Compostos de Hexametônio
Hipolipemiantes
[Mh] Termos MeSH secundário: Animais
Agonistas Colinérgicos/farmacocinética
Agonistas Colinérgicos/farmacologia
Dislipidemias/sangue
Dislipidemias/tratamento farmacológico
Compostos de Hexametônio/farmacocinética
Compostos de Hexametônio/farmacologia
Hipolipemiantes/farmacocinética
Hipolipemiantes/farmacologia
Masculino
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Hexamethonium Compounds); 0 (Hypolipidemic Agents); V26UVZ0360 (benzohexonium)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171221
[Lr] Data última revisão:
171221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE


  5 / 2015 MEDLINE  
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[PMID]:28985235
[Au] Autor:Tilunaite A; Croft W; Russell N; Bellamy TC; Thul R
[Ad] Endereço:School of Mathematical Sciences, University of Nottingham, Nottingham, England, United Kingdom.
[Ti] Título:A Bayesian approach to modelling heterogeneous calcium responses in cell populations.
[So] Source:PLoS Comput Biol;13(10):e1005794, 2017 Oct.
[Is] ISSN:1553-7358
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Calcium responses have been observed as spikes of the whole-cell calcium concentration in numerous cell types and are essential for translating extracellular stimuli into cellular responses. While there are several suggestions for how this encoding is achieved, we still lack a comprehensive theory. To achieve this goal it is necessary to reliably predict the temporal evolution of calcium spike sequences for a given stimulus. Here, we propose a modelling framework that allows us to quantitatively describe the timing of calcium spikes. Using a Bayesian approach, we show that Gaussian processes model calcium spike rates with high fidelity and perform better than standard tools such as peri-stimulus time histograms and kernel smoothing. We employ our modelling concept to analyse calcium spike sequences from dynamically-stimulated HEK293T cells. Under these conditions, different cells often experience diverse stimulus time courses, which is a situation likely to occur in vivo. This single cell variability and the concomitant small number of calcium spikes per cell pose a significant modelling challenge, but we demonstrate that Gaussian processes can successfully describe calcium spike rates in these circumstances. Our results therefore pave the way towards a statistical description of heterogeneous calcium oscillations in a dynamic environment.
[Mh] Termos MeSH primário: Potenciais de Ação/fisiologia
Teorema de Bayes
Sinalização do Cálcio/fisiologia
Cálcio/metabolismo
Modelos Biológicos
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Sinalização do Cálcio/efeitos dos fármacos
Carbacol/farmacologia
Agonistas Colinérgicos/farmacologia
Células HEK293
Seres Humanos
Análise de Célula Única/métodos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 8Y164V895Y (Carbachol); SY7Q814VUP (Calcium)
[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:171007
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pcbi.1005794


  6 / 2015 MEDLINE  
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[PMID]:28796813
[Au] Autor:Klaka P; Grüdl S; Banowski B; Giesen M; Sättler A; Proksch P; Welss T; Förster T
[Ad] Endereço:Henkel AG & Co. KGaA, Düsseldorf, Germany.
[Ti] Título:A novel organotypic 3D sweat gland model with physiological functionality.
[So] Source:PLoS One;12(8):e0182752, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Dysregulated human eccrine sweat glands can negatively impact the quality-of-life of people suffering from disorders like hyperhidrosis. Inability of sweating can even result in serious health effects in humans affected by anhidrosis. The underlying mechanisms must be elucidated and a reliable in vitro test system for drug screening must be developed. Here we describe a novel organotypic three-dimensional (3D) sweat gland model made of primary human eccrine sweat gland cells. Initial experiments revealed that eccrine sweat gland cells in a two-dimensional (2D) culture lose typical physiological markers. To resemble the in vivo situation as close as possible, we applied the hanging drop cultivation technology regaining most of the markers when cultured in its natural spherical environment. To compare the organotypic 3D sweat gland model versus human sweat glands in vivo, we compared markers relevant for the eccrine sweat gland using transcriptomic and proteomic analysis. Comparing the marker profile, a high in vitro-in vivo correlation was shown. Carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5), muscarinic acetylcholine receptor M3 (CHRM3), Na+-K+-Cl- cotransporter 1 (NKCC1), calcium-activated chloride channel anoctamin-1 (ANO1/TMEM16A), and aquaporin-5 (AQP5) are found at significant expression levels in the 3D model. Moreover, cholinergic stimulation with acetylcholine or pilocarpine leads to calcium influx monitored in a calcium flux assay. Cholinergic stimulation cannot be achieved with the sweat gland cell line NCL-SG3 used as a sweat gland model system. Our results show clear benefits of the organotypic 3D sweat gland model versus 2D cultures in terms of the expression of essential eccrine sweat gland key regulators and in the physiological response to stimulation. Taken together, this novel organotypic 3D sweat gland model shows a good in vitro-in vivo correlation and is an appropriate alternative for screening of potential bioactives regulating the sweat mechanism.
[Mh] Termos MeSH primário: Glândulas Sudoríparas/citologia
[Mh] Termos MeSH secundário: Acetilcolina/farmacologia
Aquaporina 5/genética
Aquaporina 5/metabolismo
Aquaporina 5/secreção
Biomarcadores/metabolismo
Sinalização do Cálcio
Técnicas de Cultura de Células
Polaridade Celular
Sobrevivência Celular
Células Cultivadas
Agonistas Colinérgicos/farmacologia
Seres Humanos
Modelos Biológicos
Esferoides Celulares/citologia
Esferoides Celulares/fisiologia
Glândulas Sudoríparas/metabolismo
Glândulas Sudoríparas/secreção
Transcriptoma
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (AQP5 protein, human); 0 (Aquaporin 5); 0 (Biomarkers); 0 (Cholinergic Agonists); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170811
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0182752


  7 / 2015 MEDLINE  
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[PMID]:28446461
[Au] Autor:Im YJ; Lee JK; Lee SH; Oh SJ; Park K
[Ad] Endereço:Department of Urology, College of Medicine, Seoul National University, Seoul, Korea.
[Ti] Título:Developmental changes in contractile responses to cholinergic stimuli: role of calcium sensitization and related pathways.
[So] Source:Am J Physiol Renal Physiol;313(2):F370-F377, 2017 Aug 01.
[Is] ISSN:1522-1466
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This study was performed to analyze the developmental changes in bladder response to cholinergic stimulation in detail, highlighting calcium sensitization (CS) and its related pathways. Rats were divided into three groups in accordance with reported time of developmental milestones (newborns, ; youngsters, ; and grown-ups, ). Following cholinergic stimulation (carbachol, 5 µM), the contractile response to detrusor was analyzed with respect to three phases (initial phasic, tonic, and superimposed phasic contractions). Contractile responses were analyzed by their dynamic and kinetic aspects. The responses were further compared in varying external calcium concentrations and in the presence of inhibitors of protein kinase C (PKC) and Rho kinase (ROCK), which are involved in CS. The responses of newborns contrasted with the others by their short and brisk initial phasic contractions, prominent tonic contractions, and delayed participation of irregular superimposed phasic contractions. With development, phasic contractions became prominent, and tonic contractions diminished. These developmental changes in phasic contractions were reproduced when exposed to increasing calcium concentrations. Application of specific inhibitors and molecular phasic analysis revealed that PKC was functional in tonic contractions of the newborns, whereas ROCK took over its role with development. Within a few days of birth, rats' bladders experienced drastic changes in contractile mechanisms. This included dominance of phasic contractions over tonic contractions due to increased calcium dependence and the maturational shift of the calcium sensitivity mechanism from PKC to ROCK.
[Mh] Termos MeSH primário: Compostos de Cálcio/farmacologia
Sinalização do Cálcio/efeitos dos fármacos
Carbacol/farmacologia
Agonistas Colinérgicos/farmacologia
Contração Muscular/efeitos dos fármacos
Músculo Liso/efeitos dos fármacos
Bexiga Urinária/efeitos dos fármacos
[Mh] Termos MeSH secundário: Fatores Etários
Animais
Animais Recém-Nascidos
Relação Dose-Resposta a Droga
Técnicas In Vitro
Cinética
Músculo Liso/crescimento & desenvolvimento
Cadeias Leves de Miosina/metabolismo
Fosfoproteínas Fosfatases/metabolismo
Fosforilação
Proteína Quinase C/metabolismo
Proteína Fosfatase 1/metabolismo
Ratos Sprague-Dawley
Bexiga Urinária/crescimento & desenvolvimento
Quinases Associadas a rho/metabolismo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Compounds); 0 (Cholinergic Agonists); 0 (Myosin Light Chains); 8Y164V895Y (Carbachol); EC 2.7.11.1 (rho-Associated Kinases); EC 2.7.11.13 (Protein Kinase C); EC 3.1.3.16 (Phosphoprotein Phosphatases); EC 3.1.3.16 (Ppp1r12a protein, rat); EC 3.1.3.16 (Protein Phosphatase 1)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170918
[Lr] Data última revisão:
170918
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170428
[St] Status:MEDLINE
[do] DOI:10.1152/ajprenal.00597.2016


  8 / 2015 MEDLINE  
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[PMID]:28400257
[Au] Autor:Johnson NW; Özkan M; Burgess AP; Prokic EJ; Wafford KA; O'Neill MJ; Greenhill SD; Stanford IM; Woodhall GL
[Ad] Endereço:Aston Brain Centre, Aston University, School of Life and Health Sciences, Birmingham, B4 7ET, United Kingdom.
[Ti] Título:Phase-amplitude coupled persistent theta and gamma oscillations in rat primary motor cortex in vitro.
[So] Source:Neuropharmacology;119:141-156, 2017 Jun.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In vivo, theta (4-7 Hz) and gamma (30-80 Hz) neuronal network oscillations are known to coexist and display phase-amplitude coupling (PAC). However, in vitro, these oscillations have for many years been studied in isolation. Using an improved brain slice preparation technique we have, using co-application of carbachol (10 µM) and kainic acid (150 nM), elicited simultaneous theta (6.6 ± 0.1 Hz) and gamma (36.6 ± 0.4 Hz) oscillations in rodent primary motor cortex (M1). Each oscillation showed greatest power in layer V. Using a variety of time series analyses we detected significant cross-frequency coupling in 74% of slice preparations. Differences were observed in the pharmacological profile of each oscillation. Thus, gamma oscillations were reduced by the GABA receptor antagonists, gabazine (250 nM and 2 µM), and picrotoxin (50 µM) and augmented by AMPA receptor antagonism with SYM2206 (20 µM). In contrast, theta oscillatory power was increased by gabazine, picrotoxin and SYM2206. GABA receptor blockade with CGP55845 (5 µM) increased both theta and gamma power, and similar effects were seen with diazepam, zolpidem, MK801 and a series of metabotropic glutamate receptor antagonists. Oscillatory activity at both frequencies was reduced by the gap junction blocker carbenoxolone (200 µM) and by atropine (5 µM). These data show theta and gamma oscillations in layer V of rat M1 in vitro are cross-frequency coupled, and are mechanistically distinct. The development of an in vitro model of phase-amplitude coupled oscillations will facilitate further mechanistic investigation of the generation and modulation of coupled activity in mammalian cortex.
[Mh] Termos MeSH primário: Ritmo Gama/fisiologia
Córtex Motor/fisiologia
Ritmo Teta/fisiologia
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Potenciais de Ação/fisiologia
Animais
Animais Recém-Nascidos
Carbacol/farmacologia
Agonistas Colinérgicos/farmacologia
Relação Dose-Resposta a Droga
Agonistas de Aminoácidos Excitatórios
Ritmo Gama/efeitos dos fármacos
Técnicas In Vitro
Ácido Caínico/farmacologia
Masculino
Córtex Motor/efeitos dos fármacos
Neurotransmissores/farmacologia
Ratos
Ratos Wistar
Receptores de GABA/metabolismo
Ritmo Teta/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Excitatory Amino Acid Agonists); 0 (Neurotransmitter Agents); 0 (Receptors, GABA); 8Y164V895Y (Carbachol); SIV03811UC (Kainic Acid)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170831
[Lr] Data última revisão:
170831
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170413
[St] Status:MEDLINE


  9 / 2015 MEDLINE  
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[PMID]:28323272
[Au] Autor:Peters SA; Edogawa S; Sundt WJ; Dyer RB; Dalenberg DA; Mazzone A; Singh RJ; Moses N; Smyrk TC; Weber C; Linden DR; MacNaughton WK; Turner JR; Camilleri M; Katzka DA; Farrugia G; Grover M
[Ad] Endereço:Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, Minnesota, USA.
[Ti] Título:Constipation-Predominant Irritable Bowel Syndrome Females Have Normal Colonic Barrier and Secretory Function.
[So] Source:Am J Gastroenterol;112(6):913-923, 2017 Jun.
[Is] ISSN:1572-0241
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The objective of this study was to determine whether constipation-predominant irritable bowel syndrome (IBS-C) is associated with changes in intestinal barrier and secretory function. METHODS: A total of 19 IBS-C patients and 18 healthy volunteers (all females) underwent saccharide excretion assay (0.1 g C mannitol and 1 g lactulose), measurements of duodenal and colonic mucosal barrier (transmucosal resistance (TMR), macromolecular and Escherichia coli Bio-Particle translocation), mucosal secretion (basal and acetylcholine (Ach)-evoked short-circuit current (Isc)), in vivo duodenal mucosal impedance, circulating endotoxins, and colonic tight junction gene expression. RESULTS: There were no differences in the in vivo measurements of barrier function between IBS-C patients and healthy controls: cumulative excretion of C mannitol (0-2 h mean (s.e.m.); IBS-C: 12.1 (0.9) mg vs. healthy: 13.2 (0.8) mg) and lactulose (8-24 h; IBS-C: 0.9 (0.5) mg vs. healthy: 0.5 (0.2) mg); duodenal impedance IBS-C: 729 (65) Ω vs. healthy: 706 (43) Ω; plasma mean endotoxin activity level IBS-C: 0.36 (0.03) vs. healthy: 0.35 (0.02); and in colonic mRNA expression of occludin, zonula occludens (ZO) 1-3, and claudins 1-12 and 14-19. The ex vivo findings were consistent, with no group differences: duodenal TMR (IBS-C: 28.2 (1.9) Ω cm vs. healthy: 29.8 (1.9) Ω cm ) and colonic TMR (IBS-C: 19.1 (1.1) Ω cm vs. healthy: 17.6 (1.7) Ω cm ); fluorescein isothiocyanate (FITC)-dextran (4 kDa) and E. coli Bio-Particle flux. Colonic basal Isc was similar, but duodenal basal Isc was lower in IBS-C (43.5 (4.5) µA cm ) vs. healthy (56.9 (4.9) µA cm ), P=0.05. Ach-evoked ΔIsc was similar. CONCLUSIONS: Females with IBS-C have normal colonic barrier and secretory function. Basal duodenal secretion is decreased in IBS-C.
[Mh] Termos MeSH primário: Colo/fisiopatologia
Duodeno/fisiopatologia
Mucosa Intestinal/fisiopatologia
Síndrome do Intestino Irritável/fisiopatologia
Lactulose/metabolismo
Manitol/metabolismo
RNA Mensageiro/metabolismo
[Mh] Termos MeSH secundário: Acetilcolina/farmacologia
Adulto
Estudos de Casos e Controles
Agonistas Colinérgicos/farmacologia
Claudinas/genética
Colo/efeitos dos fármacos
Colo/patologia
Constipação Intestinal/etiologia
Duodeno/efeitos dos fármacos
Duodeno/patologia
Impedância Elétrica
Endotoxinas/sangue
Feminino
Expressão Gênica
Seres Humanos
Mucosa Intestinal/efeitos dos fármacos
Mucosa Intestinal/patologia
Síndrome do Intestino Irritável/complicações
Síndrome do Intestino Irritável/genética
Meia-Idade
Ocludina/genética
Permeabilidade
Junções Íntimas/genética
Proteínas da Zônula de Oclusão/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Claudins); 0 (Endotoxins); 0 (Occludin); 0 (RNA, Messenger); 0 (Zonula Occludens Proteins); 3OWL53L36A (Mannitol); 4618-18-2 (Lactulose); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170814
[Lr] Data última revisão:
170814
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170322
[St] Status:MEDLINE
[do] DOI:10.1038/ajg.2017.48


  10 / 2015 MEDLINE  
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[PMID]:28272324
[Au] Autor:Lian W; Fang J; Xu L; Zhou W; Kang; Xiong W; Jia H; Liu AL; Du GH
[Ad] Endereço:Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Xian Nong Tan Street, Beijing 100050, China. lianwenwen1989@imm.ac.cn.
[Ti] Título:DL0410 Ameliorates Memory and Cognitive Impairments Induced by Scopolamine via Increasing Cholinergic Neurotransmission in Mice.
[So] Source:Molecules;22(3), 2017 Mar 06.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Deficiency of the cholinergic system is thought to play a vital role in cognitive impairment of dementia. DL0410 was discovered as a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinestease (BuChE), with potent efficiency in in-vitro experiments, but its in vivo effect on the cholinergic model has not been evaluated, and its action mechanism has also not been illustrated. In the present study, the capability of DL0410 in ameliorating the amnesia induced by scopolamine was investigated, and its effect on the cholinergic system in the hippocampus and its binding mode in the active site of AChE was also explored. Mice were administrated DL0410 (3 mg/kg, 10 mg/kg, and 30 mg/kg), and mice treated with donepezil were used as a positive control. The Morris water maze, escape learning task, and passive avoidance task were used as behavioral tests. The test results indicated that DL0410 could significantly improve the learning and memory impairments induced by scopolamine, with 10 mg/kg performing best. Further, DL0410 inhibited the AChE activity and increased acetylcholine (ACh) levels in a dose-dependent manner, and interacted with the active site of AChE in a similar manner as donepezil. However, no difference in the activity of BuChE was found in this study. All of the evidence indicated that its AChE inhibition is an important mechanism in the anti-amnesia effect. In conclusion, DL0410 could be an effective therapeutic drug for the treatment of dementia, especially Alzheimer's disease.
[Mh] Termos MeSH primário: Agonistas Colinérgicos/farmacologia
Disfunção Cognitiva/metabolismo
Transtornos da Memória/metabolismo
Transmissão Sináptica/efeitos dos fármacos
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Acetilcolinesterase/metabolismo
Animais
Sítios de Ligação
Domínio Catalítico
Agonistas Colinérgicos/química
Inibidores da Colinesterase/farmacologia
Disfunção Cognitiva/tratamento farmacológico
Disfunção Cognitiva/etiologia
Hipocampo/efeitos dos fármacos
Hipocampo/metabolismo
Locomoção/efeitos dos fármacos
Masculino
Aprendizagem em Labirinto/efeitos dos fármacos
Memória/efeitos dos fármacos
Transtornos da Memória/tratamento farmacológico
Transtornos da Memória/etiologia
Camundongos
Modelos Moleculares
Conformação Molecular
Atividade Motora/efeitos dos fármacos
Ligação Proteica
Hidrobrometo de Escopolamina/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Agonists); 0 (Cholinesterase Inhibitors); 451IFR0GXB (Scopolamine Hydrobromide); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170518
[Lr] Data última revisão:
170518
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE



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