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[PMID]:18931243
[Au] Autor:Riad W; Ahmed N
[Ad] Endereço:Department of Anaesthesia, King Khaled Eye Specialist Hospital, P.O. Box 7191, Riyadh 11462, Kingdom of Saudi Arabia. waleed_riad@yahoo.com
[Ti] Título:Single injection peribulbar anesthesia with a short needle combined with digital compression.
[So] Source:Anesth Analg;107(5):1751-3, 2008 Nov.
[Is] ISSN:1526-7598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: We compare the efficacy of using a 15 mm to the standard 25 mm needle for performing peribulbar blockade. METHODS: Blocks were performed on 150 patients using 15 or 25 mm needle length. Digital compression was applied by the thumb and index finger around the needle hub during injection with 15 mm needle. Anesthetic was injected until lid fullness was noted. Inadequate block was augmented. RESULTS: No significant differences were noted between groups with respect to local anesthetic volume, supplementation, and akinesia. CONCLUSION: Peribulbar blockade performed with a 15 mm needle with digital pressure is comparable to blockade using a 25 mm needle.
[Mh] Termos MeSH primário: Analgesia/métodos
Anestesia Local/métodos
Extração de Catarata
Injeções/métodos
[Mh] Termos MeSH secundário: Idoso
Desenho de Equipamento
Etidocaína/uso terapêutico
Pálpebras
Feminino
Dedos
Lateralidade Funcional
Seres Humanos
Masculino
Meia-Idade
Agulhas
Bloqueio Nervoso/métodos
Músculos Oculomotores/cirurgia
Medição da Dor
Facoemulsificação/métodos
Pressão
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
I6CQM0F31V (Etidocaine)
[Em] Mês de entrada:0811
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:081022
[St] Status:MEDLINE
[do] DOI:10.1213/ane.0b013e3181864d1c


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[PMID]:18288959
[Au] Autor:Erve JC
[Ad] Endereço:Drug Safety and Metabolism, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. ERVEJ@wyeth.com
[Ti] Título:Cyclic metabolites: chemical and biological considerations.
[So] Source:Curr Drug Metab;9(2):175-88, 2008 Feb.
[Is] ISSN:1389-2002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Metabolism of xenobiotics can sometimes generate cyclic metabolites. Such metabolites are usually the result of intramolecular reactions occurring within a primary or secondary metabolite and this chemistry may lead to unexpected structures. Intramolecular chemistry is often driven by nucleophilic groups reacting with electrophilic atoms, often carbon, although radical processes also occur. Conjugation of xenobiotics or their metabolites with endogenous thiols, such as glutathione or cysteine, introduce a reactive amino group that can lead to the formation of cyclic structures. Less common than chemically driven cyclizations are enzymatically mediated ring-closures, although this may reflect our incomplete recognition of enzymatic involvement in this step of cyclic metabolite formation. While some cyclic metabolites are biologically inactive, others are biologically active. Thus, a cyclic metabolite may display desirable pharmacology, or, contribute to toxicology. When a cyclic metabolite is identified, it is important to consider the possibility that it is an artifact, i.e. metabonate, that was formed during processing of the sample, for example, through degradation or by chemical reactions with other components present in the matrix. From a medicinal chemistry perspective, a cyclic metabolite with a different chemical scaffold from the parent structure may lead to a new series of structurally novel, biologically active molecules with the same, or different, pharmacology from the parent. This review will cover a selection of cyclic metabolites from a mechanistic point of view, and when possible, discuss their biological relevance.
[Mh] Termos MeSH primário: Biotransformação
Xenobióticos/metabolismo
[Mh] Termos MeSH secundário: Etidocaína/metabolismo
Seres Humanos
Lidocaína/metabolismo
Melatonina/metabolismo
Metadona/metabolismo
Mitoxantrona/metabolismo
Oxazóis/metabolismo
Tocainide/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Oxazoles); 0 (Xenobiotics); 24QIB5VSGX (isamoxole); 27DXO59SAN (Tocainide); 98PI200987 (Lidocaine); BZ114NVM5P (Mitoxantrone); I6CQM0F31V (Etidocaine); JL5DK93RCL (Melatonin); UC6VBE7V1Z (Methadone)
[Em] Mês de entrada:0804
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080222
[St] Status:MEDLINE


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[PMID]:17976897
[Au] Autor:de Paula E; Schreier S; Jarrell HC; Fraceto LF
[Ad] Endereço:Departamento de Bioquímica, Instituto de Biologia/Universidade Estadual de Campinas, SP, Brazil.
[Ti] Título:Preferential location of lidocaine and etidocaine in lecithin bilayers as determined by EPR, fluorescence and 2H NMR.
[So] Source:Biophys Chem;132(1):47-54, 2008 Jan.
[Is] ISSN:0301-4622
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We have examined the effect of the uncharged species of lidocaine (LDC) and etidocaine (EDC) on the acyl chain moiety of egg phosphatidylcholine liposomes. Changes in membrane organization caused by both anesthetics were detected through the use of EPR spin labels (5, 7 and 12 doxyl stearic acid methyl ester) or fluorescence probes (4, 6, 10, 16 pyrene-fatty acids). The disturbance caused by the LA was greater when the probes were inserted in more external positions of the acyl chain and decreased towards the hydrophobic core of the membrane. The results indicate a preferential insertion of LDC at the polar interface of the bilayer and in the first half of the acyl chain, for EDC. Additionally, (2)H NMR spectra of multilamellar liposomes composed by acyl chain-perdeutero DMPC and EPC (1:4 mol%) allowed the determination of the segmental order (S(mol)) and dynamics (T(1)) of the acyl chain region. In accordance to the fluorescence and EPR results, changes in molecular orientation and dynamics are more prominent if the LA preferential location is more superficial, as for LDC while EDC seems to organize the acyl chain region between carbons 2-8, which is indicative of its positioning. We propose that the preferential location of LDC and EDC inside the bilayers creates a "transient site", which is related to the anesthetic potency since it could modulate the access of these molecules to their binding site(s) in the voltage-gated sodium channel.
[Mh] Termos MeSH primário: Anestésicos Locais/química
Etidocaína/química
Lecitinas/química
Lidocaína/química
Bicamadas Lipídicas/química
[Mh] Termos MeSH secundário: Animais
Espectroscopia de Ressonância de Spin Eletrônica
Fluorescência
Corantes Fluorescentes/análise
Lipossomos
Espectroscopia de Ressonância Magnética
Marcadores de Spin
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Fluorescent Dyes); 0 (Lecithins); 0 (Lipid Bilayers); 0 (Liposomes); 0 (Spin Labels); 98PI200987 (Lidocaine); I6CQM0F31V (Etidocaine)
[Em] Mês de entrada:0802
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071103
[St] Status:MEDLINE


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[PMID]:17192120
[Au] Autor:Weinberg G
[Ad] Endereço:Department of Anesthesiology, University of Illinois College of Medicine, Chicago, and University of Illinois Hospital 60612, USA. guyw@uic.edu
[Ti] Título:Lipid rescue resuscitation from local anaesthetic cardiac toxicity.
[So] Source:Toxicol Rev;25(3):139-45, 2006.
[Is] ISSN:1176-2551
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:Systemic local anaesthetic toxicity is a rare but potentially fatal complication of regional anaesthesia. This toxicity is due to inhibition of ionotropic and metabotropic cell signal systems and possibly mitochondrial metabolism. It is associated with CNS excitation and, in the extreme, refractory cardiac dysfunction and circulatory collapse. Infusion of lipid emulsion has been shown in animal models to reliably reverse otherwise intractable cardiac toxicity and the mechanism of lipid rescue is probably a combination of reduced tissue binding by re-established equilibrium in a plasma lipid phase and a beneficial energetic-metabolic effect. Recent case reports have suggested the clinical efficacy of lipid infusion by the recovery of patients from intractable cardiac arrest. Future areas of investigation will focus on improved treatment regimes and better understanding of the mechanism of lipid rescue, which might allow superior alternative therapies, or treatment of other toxic events. An educational website has been established to help disseminate information about lipid emulsion therapy and to serve as a medium for physicians to share experiences or thoughts on the method and local anaesthetic toxicity.
[Mh] Termos MeSH primário: Anestésicos Locais/toxicidade
Emulsões Gordurosas Intravenosas/uso terapêutico
Parada Cardíaca/prevenção & controle
Ressuscitação/métodos
[Mh] Termos MeSH secundário: Anestésicos Locais/administração & dosagem
Animais
Bupivacaína/administração & dosagem
Bupivacaína/toxicidade
Modelos Animais de Doenças
Etidocaína/administração & dosagem
Etidocaína/toxicidade
Emulsões Gordurosas Intravenosas/administração & dosagem
Parada Cardíaca/induzido quimicamente
Seres Humanos
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Fat Emulsions, Intravenous); I6CQM0F31V (Etidocaine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:0704
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:061229
[St] Status:MEDLINE


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[PMID]:16360344
[Au] Autor:Mathieu O; Hillaire-Buys D; Dadure C; Barnay F; Mathieu-Daudé JC; Bressolle F
[Ad] Endereço:Department of Medical Pharmacology and Toxicology, Lapeyronie Hospital, Montpellier, France.
[Ti] Título:Liquid chromatography-electrospray mass spectrometry determination of free and total concentrations of ropivacaine in human plasma.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;831(1-2):91-8, 2006 Feb 02.
[Is] ISSN:1570-0232
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A specific and sensitive liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method was developed for the determination of free and total ropivacaine in human plasma. The work-up procedure involved a simple precipitation of plasma proteins with methanol. Etidocaine served as the internal standard. After microscale equilibrium-dialysis, measurement of free ropivacaine levels was performed after direct injection of the dialysate into the chromatograph. The system used a Zorbax eclipse XD8 C8 analytical column packed with 5 microm diameter particles as the stationary phase. The mobile phase consisted of a 15-min gradient (mobile phase A: 0.05% (v/v) trimethylamine in acetonitrile, mobile phase B: 2mM ammonium formate buffer (pH 3)). Mass spectrometric data were acquired in single ion monitoring mode at m/z 275 for ropivacaine and m/z 277 for etidocaine. The drug/internal standard peak area ratios (plasma) or peak areas (dialysate) were linked via a quadratic relationship to concentrations. Precision ranged from 1 to 7.6% accuracy was between 92.6 and 109%. The lower limits of quantitation were 1 microg/l in plasma and 2 microg/l in the dialysate. This method was found suitable for the analysis of plasma samples collected during a clinical trial performed in 30 infants undergoing epidural anaesthesia or continuous psoas compartment block.
[Mh] Termos MeSH primário: Amidas/sangue
Cromatografia Líquida/métodos
[Mh] Termos MeSH secundário: Anestesia Local/métodos
Diálise
Estabilidade de Medicamentos
Etidocaína
Seres Humanos
Bloqueio Nervoso
Músculos Psoas/inervação
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Amides); 7IO5LYA57N (ropivacaine); I6CQM0F31V (Etidocaine)
[Em] Mês de entrada:0604
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:051220
[St] Status:MEDLINE


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[PMID]:12751552
[Au] Autor:Cox B; Durieux ME; Marcus MA
[Ad] Endereço:Department of Anesthesiology, University Hospital Maastricht, PO Box 5800, 6202 AZ Maastricht, The Netherlands.
[Ti] Título:Toxicity of local anaesthetics.
[So] Source:Best Pract Res Clin Anaesthesiol;17(1):111-36, 2003 Mar.
[Is] ISSN:1521-6896
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The complications of failure, neural injury and local anaesthetic toxicity are common to all regional anaesthetic techniques, and individual techniques are associated with specific complications. All potential candidates for regional anaesthesia should be thoroughly evaluated and informed of potential complications. Central neural blockades still account for more than 70% of regional anaesthesia procedures. Permanent neurological injury is 0.02-0.07%. Pain on injection and paraesthesias while performing regional anaesthesia are danger signals of potential injury and must not be ignored. The incidence of systemic toxicity to local anaesthetics has significantly decreased in the past 30 years, from 0.2 to 0.01%. Peripheral nerve blocks are associated with the highest incidence of systemic toxicity (7.5 per 10,000) and the lowest incidence of serious neural injury (1.9 per 10,000).
[Mh] Termos MeSH primário: Anestésicos Locais/efeitos adversos
Procaína/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Bupivacaína/efeitos adversos
Sistema Cardiovascular/efeitos dos fármacos
Cocaína/efeitos adversos
Hipersensibilidade a Drogas/etiologia
Etidocaína/efeitos adversos
Seres Humanos
Lidocaína/efeitos adversos
Mepivacaína/efeitos adversos
Sistema Nervoso/efeitos dos fármacos
Procaína/efeitos adversos
Tetracaína/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 0619F35CGV (Tetracaine); 4Z8Y51M438 (Procaine); 5YVB0POT2H (chloroprocaine); 98PI200987 (Lidocaine); B6E06QE59J (Mepivacaine); I5Y540LHVR (Cocaine); I6CQM0F31V (Etidocaine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:0305
[Cu] Atualização por classe:171114
[Lr] Data última revisão:
171114
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030520
[St] Status:MEDLINE


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[PMID]:12436827
[Au] Autor:Hawkins JM; Moore PA
[Ad] Endereço:Continuing Education Program, Faculty of Dentistry, University of Toronto, 4800 Leslie Street, Suite 111, Toronto, Ontario, Canada M2J2K9.
[Ti] Título:Local anesthesia: advances in agents and techniques.
[So] Source:Dent Clin North Am;46(4):719-32, ix, 2002 Oct.
[Is] ISSN:0011-8532
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The improvements in agents and techniques for local anesthesia are possibly the most important advances in dental science to have occurred in the past 100 years. The agents currently available in dentistry have most of the characteristics of an ideal local anesthetic. Today's anesthetics can be administered with minimal irritation and little concern for stimulating allergic reactions. A variety of agents are available that provide rapid onset of surgical anesthesia with adequate duration. This article provides a brief review of the local anesthetic agents, formulations, and techniques used in dentistry with special emphasis on newly introduced agents and procedures.
[Mh] Termos MeSH primário: Anestesia Dentária
Anestesia Local
Anestésicos Locais/administração & dosagem
[Mh] Termos MeSH secundário: Anestesia Dentária/métodos
Anestesia Local/métodos
Anestésicos Locais/efeitos adversos
Anestésicos Locais/química
Anestésicos Locais/classificação
Bupivacaína/administração & dosagem
Carticaína/administração & dosagem
Química Farmacêutica
Hipersensibilidade a Drogas/prevenção & controle
Quimioterapia Assistida por Computador
Etidocaína/administração & dosagem
Seres Humanos
Injeções
Injeções a Jato
Lidocaína/administração & dosagem
Mepivacaína/administração & dosagem
Prilocaína/administração & dosagem
Segurança
Fatores de Tempo
Estimulação Elétrica Nervosa Transcutânea
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 046O35D44R (Prilocaine); 98PI200987 (Lidocaine); B6E06QE59J (Mepivacaine); D3SQ406G9X (Carticaine); I6CQM0F31V (Etidocaine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:0212
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:021120
[St] Status:MEDLINE


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[PMID]:12130650
[Au] Autor:Yarov-Yarovoy V; McPhee JC; Idsvoog D; Pate C; Scheuer T; Catterall WA
[Ad] Endereço:Department of Pharmacology, University of Washington, Seattle, Washington 98195-7280, USA.
[Ti] Título:Role of amino acid residues in transmembrane segments IS6 and IIS6 of the Na+ channel alpha subunit in voltage-dependent gating and drug block.
[So] Source:J Biol Chem;277(38):35393-401, 2002 Sep 20.
[Is] ISSN:0021-9258
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Alanine-scanning mutagenesis of transmembrane segments IS6 and IIS6 of the rat brain Na(v)1.2 channel alpha subunit identified mutations N418A in IS6 and L975A in IIS6 as causing strong positive shifts in the voltage dependence of activation. In contrast, mutations V424A in IS6 and L983A in IIS6 caused strong negative shifts. Most IS6 mutations opposed inactivation from closed states, but most IIS6 mutations favored such inactivation. Mutations L421C and L983A near the intracellular ends of IS6 and IIS6, respectively, exhibited significant sustained Na(+) currents at the end of 30-ms depolarizations, indicating a role for these residues in Na(+) channel fast inactivation. These residues, in combination with residues at the intracellular end of IVS6, are well situated to form an inactivation gate receptor. Mutation I409A in IS6 reduced the affinity of the local anesthetic etidocaine for the inactivated state by 6-fold, and mutations I409A and N418A reduced use-dependent block by etidocaine. No IS6 or IIS6 mutations studied affected inactivated-state affinity or use-dependent block by the neuroprotective drug sipatrigine (compound 619C89). These results suggest that the local anesthetic receptor site is formed primarily by residues in segments IIIS6 and IVS6 with the contribution of a single amino acid in segment IS6.
[Mh] Termos MeSH primário: Aminoácidos/fisiologia
Ativação do Canal Iônico
Proteínas do Tecido Nervoso/fisiologia
Canais de Sódio/fisiologia
[Mh] Termos MeSH secundário: Anestésicos Locais/farmacologia
Animais
Anticonvulsivantes/farmacologia
Encéfalo/metabolismo
Etidocaína/farmacologia
Mutagênese Sítio-Dirigida
Canal de Sódio Disparado por Voltagem NAV1.2
Proteínas do Tecido Nervoso/química
Proteínas do Tecido Nervoso/genética
Proteínas do Tecido Nervoso/metabolismo
Mutação Puntual
Ratos
Canais de Sódio/química
Canais de Sódio/genética
Canais de Sódio/metabolismo
Xenopus
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Amino Acids); 0 (Anesthetics, Local); 0 (Anticonvulsants); 0 (NAV1.2 Voltage-Gated Sodium Channel); 0 (Nerve Tissue Proteins); 0 (Scn2a1 protein, rat); 0 (Sodium Channels); I6CQM0F31V (Etidocaine)
[Em] Mês de entrada:0210
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020720
[St] Status:MEDLINE


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[PMID]:12093505
[Au] Autor:Silva N; Schapoval EE
[Ad] Endereço:Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Av. Ipiranga, 2752, Porto Alegre, R/S, CEP 90160-000, Porto Alegre, Brazil. nieelson@hotmail.com
[Ti] Título:Spectrophotometric determination of etidocaine in pharmaceutical (dental) formulation.
[So] Source:J Pharm Biomed Anal;29(4):749-54, 2002 Jul 20.
[Is] ISSN:0731-7085
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A spectrophotometric method was developed for the determination of etidocaine hydrochloride (EH) in injectable pharmaceutical preparation. The proposal of this work was to develop a rapid, simple, inexpensive, precise and accurate visible spectrophotometric method. The method is based on the formation of the ion-pair complex by the EH reaction with bromocresol green in the pH 4.6 which after chloroform extraction gives a yellow color that in basic medium change to blue color and exhibits a maximum absorbance at 625 nm. The calibration graph was linear over the range 2.0-6.0 microg ml(-1) EH calculated on the final yellow solution. The R.S.D. of the slope of the four lines was 0.73%. This method can be applied to injectable pharmaceutical preparation dosage studied.
[Mh] Termos MeSH primário: Anestesia Dentária
Anestésicos Locais/análise
Etidocaína/análise
Preparações Farmacêuticas/análise
[Mh] Termos MeSH secundário: Anestésicos Locais/química
Verde de Bromocresol/química
Tampões (Química)
Etidocaína/química
Reprodutibilidade dos Testes
Acetato de Sódio
Espectrofotometria
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Buffers); 0 (Pharmaceutical Preparations); 4550K0SC9B (Sodium Acetate); 8YGN0Y942M (Bromcresol Green); I6CQM0F31V (Etidocaine)
[Em] Mês de entrada:0210
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020703
[St] Status:MEDLINE


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[PMID]:11024055
[Au] Autor:Yarov-Yarovoy V; Brown J; Sharp EM; Clare JJ; Scheuer T; Catterall WA
[Ad] Endereço:Department of Pharmacology, University of Washington, Seattle, Washington 98195-7280, USA.
[Ti] Título:Molecular determinants of voltage-dependent gating and binding of pore-blocking drugs in transmembrane segment IIIS6 of the Na(+) channel alpha subunit.
[So] Source:J Biol Chem;276(1):20-7, 2001 Jan 05.
[Is] ISSN:0021-9258
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Mutations of amino acid residues in the inner two-thirds of the S6 segment in domain III of the rat brain type IIA Na(+) channel (G1460A to I1473A) caused periodic positive and negative shifts in the voltage dependence of activation, consistent with an alpha-helix having one face on which mutations to alanine oppose activation. Mutations in the outer one-third of the IIIS6 segment all favored activation. Mutations in the inner half of IIIS6 had strong effects on the voltage dependence of inactivation from closed states without effect on open-state inactivation. Only three mutations had strong effects on block by local anesthetics and anticonvulsants. Mutations L1465A and I1469A decreased affinity of inactivated Na(+) channels up to 8-fold for the anticonvulsant lamotrigine and its congeners 227c89, 4030w92, and 619c89 as well as for the local anesthetic etidocaine. N1466A decreased affinity of inactivated Na(+) channels for the anticonvulsant 4030w92 and etidocaine by 3- and 8-fold, respectively, but had no effect on affinity of the other tested compounds. Leu-1465, Asn-1466, and Ile-1469 are located on one side of the IIIS6 helix, and mutation of each caused a positive shift in the voltage dependence of activation. Evidently, these amino acid residues face the lumen of the pore, contribute to formation of the high-affinity receptor site for pore-blocking drugs, and are involved in voltage-dependent activation and coupling to closed-state inactivation.
[Mh] Termos MeSH primário: Anestésicos Locais/farmacologia
Anticonvulsivantes/farmacologia
Ativação do Canal Iônico/efeitos dos fármacos
Canais de Sódio/química
Canais de Sódio/metabolismo
[Mh] Termos MeSH secundário: Substituição de Aminoácidos/genética
Anestésicos Locais/metabolismo
Animais
Anticonvulsivantes/metabolismo
Sítios de Ligação
Encéfalo
Eletrofisiologia
Etidocaína/metabolismo
Etidocaína/farmacologia
Proteínas de Membrana/genética
Proteínas de Membrana/metabolismo
Oócitos/efeitos dos fármacos
Oócitos/metabolismo
Técnicas de Patch-Clamp
Piperazinas/metabolismo
Piperazinas/farmacologia
Mutação Puntual
Ligação Proteica
Estrutura Terciária de Proteína
Pirimidinas/metabolismo
Pirimidinas/farmacologia
Ratos
Bloqueadores dos Canais de Sódio
Canais de Sódio/genética
Termodinâmica
Triazinas/metabolismo
Triazinas/farmacologia
Xenopus laevis
[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 (Anesthetics, Local); 0 (Anticonvulsants); 0 (Membrane Proteins); 0 (Piperazines); 0 (Pyrimidines); 0 (Sodium Channel Blockers); 0 (Sodium Channels); 0 (Triazines); I6CQM0F31V (Etidocaine); OON9AVW1T3 (sipatrigine); U3H27498KS (lamotrigine)
[Em] Mês de entrada:0102
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:001012
[St] Status:MEDLINE



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