Base de dados : LILACS
Pesquisa : D02.092.877.787.500 [Categoria DeCS]
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Texto completo SciELO Brasil
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Id: lil-766979
Autor: Vasconcelos, T B; Ribeiro-Filho, H V; Lucetti, L T; Magalhães, P J C.
Título: ß-Citronellol, an alcoholic monoterpene with inhibitory properties on the contractility of rat trachea
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;49(2):e4800, 2016. tab, graf.
Idioma: en.
Resumo: β-Citronellol is an alcoholic monoterpene found in essential oils such Cymbopogon citratus (a plant with antihypertensive properties). β-Citronellol can act against pathogenic microorganisms that affect airways and, in virtue of the popular use of β-citronellol-enriched essential oils in aromatherapy, we assessed its pharmacologic effects on the contractility of rat trachea. Contractions of isolated tracheal rings were recorded isometrically through a force transducer connected to a data-acquisition device. β-Citronellol relaxed sustained contractions induced by acetylcholine or high extracellular potassium, but half-maximal inhibitory concentrations (IC50) for K+-elicited stimuli were smaller than those for cholinergic contractions. It also inhibited contractions induced by electrical field stimulation or sodium orthovanadate with pharmacologic potency equivalent to that seen against acetylcholine-induced contractions. When contractions were evoked by selective recruitment of Ca2+ from the extracellular medium, β-citronellol preferentially inhibited contractions that involved voltage-operated (but not receptor-operated) pathways. β-Citronellol (but not verapamil) inhibited contractions induced by restoration of external Ca2+ levels after depleting internal Ca2+ stores with the concomitant presence of thapsigargin and recurrent challenge with acetylcholine. Treatment of tracheal rings with L-NAME, indomethacin or tetraethylammonium did not change the relaxing effects of β-citronellol. Inhibition of transient receptor potential vanilloid subtype 1 (TRPV1) or transient receptor potential ankyrin 1 (TRPA1) receptors with selective antagonists caused no change in the effects of β-citronellol. In conclusion, β-citronellol exerted inhibitory effects on rat tracheal rings, with predominant effects on contractions that recruit Ca2+ inflow towards the cytosol by voltage-gated pathways, whereas it appears less active against contractions elicited by receptor-operated Ca2+ channels.
Descritores: Bloqueadores dos Canais de Cálcio/farmacologia
Monoterpenos/farmacologia
Contração Muscular/efeitos dos fármacos
Músculo Liso/efeitos dos fármacos
Traqueia/efeitos dos fármacos
-Análise de Variância
Bloqueadores dos Canais de Cálcio/administração & dosagem
Inibidores Enzimáticos/farmacologia
Indometacina/farmacologia
Concentração Inibidora 50
Monoterpenos/administração & dosagem
NG-Nitroarginina Metil Éster/farmacologia
Parassimpatolíticos/administração & dosagem
Ratos Wistar
Tetraetilamônio/farmacologia
Tapsigargina/farmacologia
Verapamil/farmacologia
Limites: Animais
Masculino
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


  2 / 5 LILACS  
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Id: lil-748218
Autor: López-Canales, J.S.; Lozano-Cuenca, J.; Muãoz-Islas, E.; Aguilar-Carrasco, J.C.; López-Canales, O.A.; López-Mayorga, R.M.; Castillo-Henkel, E.F.; Valencia-Hernández, I.; Castillo-Henkel, C..
Título: Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;48(6):537-544, 06/2015. graf.
Idioma: en.
Resumo: Amfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, it is not known whether amfepramone produces immediate vascular effects when applied in vitro to rat aortic rings and, if so, what mechanisms may be involved. We analyzed the effect of amfepramone on phenylephrine-precontracted rat aortic rings with or without endothelium and the influence of inhibitors or blockers on this effect. Amfepramone produced a concentration-dependent vasorelaxation in phenylephrine-precontracted rat aortic rings that was not affected by the vehicle, atropine, 4-AP, glibenclamide, indomethacin, clotrimazole, or cycloheximide. The vasorelaxant effect of amfepramone was significantly attenuated by NG-nitro-L-arginine methyl ester (L-NAME) and tetraethylammonium (TEA), and was blocked by removal of the vascular endothelium. These results suggest that amfepramone had a direct vasorelaxant effect on phenylephrine-precontracted rat aortic rings, and that inhibition of endothelial nitric oxide synthase and the opening of Ca2+-activated K+ channels were involved in this effect.
Descritores: Acetilcolina/farmacologia
Aorta Torácica/efeitos dos fármacos
Depressores do Apetite/farmacologia
Dietilpropiona/farmacologia
Vasodilatadores/farmacologia
-Aorta Torácica/metabolismo
Canais de Cálcio/efeitos dos fármacos
Canais de Cálcio/metabolismo
Endotélio Vascular/efeitos dos fármacos
NG-Nitroarginina Metil Éster/metabolismo
Óxido Nítrico Sintase Tipo III/efeitos dos fármacos
Fenilefrina/farmacologia
Canais de Potássio/efeitos dos fármacos
Canais de Potássio/metabolismo
Ratos Wistar
Tetraetilamônio/metabolismo
Vasoconstritores/farmacologia
Vasodilatação/efeitos dos fármacos
Limites: Animais
Masculino
Tipo de Publ: Estudo de Avaliação
Responsável: BR1.1 - BIREME


  3 / 5 LILACS  
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Id: lil-712208
Autor: Rosa, Ronaldo Fernandes.
Título: Suplementação mineral e vitamínica em doenças crônicas e de convalescença / Mineral and vitamin supplementation in chronic diseases and convalescence
Fonte: J. bras. med;102(1), jan.-fev. 2014.
Idioma: pt.
Resumo: A síndrome de fadiga crônica (SFC) é uma condição clínica que, apesar de muito prevalente, tem tratamento controverso. A suplementação com substratos como glutamina e vitaminas pode atuar como adjuvante terapêutico. Os autores descrevem um medicamento que pode atender essa finalidade, composto por glutamina 200mg, glutamato de cálcio 250mg, cloridrato de piridoxina 20mg e fosfato de ditetraetilamônio 6mg. São descritas também as ações de cada um dos componentes, e como podem auxiliar na terapêutica da SFC e em períodos de convalescença em diversas condições.

The chronic fatigue syndrome (CFS) is a clinical condition which, although highly prevalent, treatment is controversial and supplementation of substrates such as glutamine and vitamins can act as therapeutic adjuvant. A drug composition that can serve this purpose, the composition is glutamine 200mg, 250mg calcium glutamate, 20mg pyridoxine hydrochloride and phosphate ditetraetilammonium 6mg is described. Also described the actions of each component and how they can assist in the treatment of CFS and in periods of convalescence from various other conditions described.
Descritores: Síndrome de Fadiga Crônica/dietoterapia
Síndrome de Fadiga Crônica/terapia
-Convalescença
Vitaminas na Dieta
Glutamatos/uso terapêutico
Glutamina/uso terapêutico
Minerais/uso terapêutico
Piridoxina/uso terapêutico
Suplementos Nutricionais
Tetraetilamônio/uso terapêutico
Limites: Humanos
Masculino
Feminino
Responsável: BR1365.1 - Biblioteca Biomédica A - CB/A


  4 / 5 LILACS  
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Texto completo SciELO Brasil
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Id: lil-586505
Autor: López-Canales, J. S; López-Sanchez, P; Perez-Alvarez, V. M; Wens-Flores, I; Polanco, A. C; Castillo-Henkel, E; Castillo-Henkel, C.
Título: The methyl ester of rosuvastatin elicited an endothelium-independent and 3-hydroxy-3-methylglutaryl coenzyme A reductase-independent relaxant effect in rat aorta
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;44(5):438-444, May 2011. ilus.
Idioma: en.
Resumo: The relaxant effect of the methyl ester of rosuvastatin was evaluated on aortic rings from male Wistar rats (250-300 g, 6 rats for each experimental group) with and without endothelium precontracted with 1.0 µM phenylephrine. The methyl ester presented a slightly greater potency than rosuvastatin in relaxing aortic rings, with log IC50 values of -6.88 and -6.07 M, respectively. Unlike rosuvastatin, the effect of its methyl ester was endothelium-independent. Pretreatment with 10 µM indomethacin did not inhibit, and pretreatment with 1 mM mevalonate only modestly inhibited the relaxant effect of the methyl ester. Nω-nitro-L-arginine methyl ester (L-NAME, 10 µM), the selective nitric oxide-2 (NO-2) inhibitor 1400 W (10 µM), tetraethylammonium (TEA, 10 mM), and cycloheximide (10 µM) partially inhibited the relaxant effect of the methyl ester on endothelium-denuded aortic rings. However, the combination of TEA plus either L-NAME or cycloheximide completely inhibited the relaxant effect. Inducible NO synthase (NOS-2) was only present in endothelium-denuded aortic rings, as demonstrated by immunoblot with methyl ester-treated rings. In conclusion, whereas rosuvastatin was associated with a relaxant effect dependent on endothelium and hydroxymethylglutaryl coenzyme A reductase in rat aorta, the methyl ester of rosuvastatin exhibited an endothelium-independent and only slightly hydroxymethylglutaryl coenzyme A reductase-dependent relaxant effect. Both NO produced by NOS-2 and K+ channels are involved in the relaxant effect of the methyl ester of rosuvastatin.
Descritores: Aorta/efeitos dos fármacos
Endotélio Vascular/efeitos dos fármacos
Fluorbenzenos/farmacologia
Hidroximetilglutaril-CoA Redutases/efeitos dos fármacos
NG-Nitroarginina Metil Éster/farmacologia
Pirimidinas/farmacologia
Sulfonamidas/farmacologia
Vasodilatação/efeitos dos fármacos
Vasodilatadores/farmacologia
-Aorta/enzimologia
Cicloeximida/farmacologia
Fluorbenzenos/química
Óxido Nítrico Sintase Tipo II/farmacologia
Pirimidinas/química
Ratos Wistar
Sulfonamidas/química
Tetraetilamônio/farmacologia
Vasodilatação/fisiologia
Limites: Animais
Masculino
Ratos
Responsável: BR1.1 - BIREME


  5 / 5 LILACS  
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Texto completo SciELO Chile
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Id: lil-437383
Autor: Mears, David; Rojas, Eduardo.
Título: Properties of voltage-gated Ca2+ currents measured from mouse pancreatic â-cells in situ
Fonte: Biol. Res;39(3):505-520, 2006. ilus.
Idioma: en.
Projeto: El Fondo Nacional de Desarrollo Científico y Tecnológico.
Resumo: We used the single-microelectrode voltage-clamp technique to record ionic currents from pancreatic â-cells within intact mouse islets of Langerhans at 37C, the typical preparation for studies of glucose-induced "bursting" electrical activity. Cells were impaled with intracellular microelectrodes, and voltage pulses were applied in the presence of tetraethylammonium. Under these conditions, a voltage-dependent Ca2+ current (I Cav), containing L-type and non-L-type components, was observed. The current measured in situ was larger than that measured in single cells with whole-cell patch clamping, particularly at membrane potentials corresponding to the action potentials of â-cell electrical activity. The temperature dependence of I Cav was not sufficient to account for the difference in size of the currents recorded with the two methods. During prolonged pulses, the voltage-dependent Ca2+ current measured in situ displayed both rapid and slow components of inactivation. The rapid component was Ca2+-dependent and was inhibited by the membrane-permeable Ca2+ chelator, BAPTA-AM. The effect of BAPTA-AM on â-cell electrical activity then demonstrated that Ca2+-dependent inactivation of I Cav contributes to action potential repolarization and to control of burst frequency. Our results demonstrate the utility of voltage clamping â-cells in situ for determining the roles of ion channels in electrical activity and insulin secretion.
Descritores: Canais de Cálcio/fisiologia
Células Secretoras de Insulina/fisiologia
Potenciais da Membrana/fisiologia
-Eletrofisiologia
Células Secretoras de Insulina/efeitos dos fármacos
Microeletrodos
Técnicas de Patch-Clamp
Tetraetilamônio/farmacologia
Limites: Animais
Camundongos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME



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