PREJUNCTIONAL EFFECT of QUATERNARY DERIVATIVES of L-HYOSCYAMINE AT the RAT NEUROMUSCULAR-JUNCTION - A STRUCTURE-ACTIVITY RELATIONSHIP STUDY

PREJUNCTIONAL EFFECT of QUATERNARY DERIVATIVES of L-HYOSCYAMINE AT the RAT NEUROMUSCULAR-JUNCTION - A STRUCTURE-ACTIVITY RELATIONSHIP STUDY

Autor Souccar, C. Google Scholar
Soldera, JDC Google Scholar
Cysneiros, Roberta Monterazzo Autor UNIFESP Google Scholar
Goncalo, MDC Google Scholar
Lapa, A. J. Google Scholar
Instituição Universidade Federal de São Paulo (UNIFESP)
Resumo 1. the effects of phenthonium and related compounds on the spontaneous release of acetylcholine (ACh) were investigated with electrophysiological and radiolabelled techniques to correlate the prejunctional effect with their cholinolytic activities and to determine the structure-activity relationship.2. Phenthonium and endophen are N-(4-phenyl)-phenacyl derivatives of l-hyoscyamine in ''exo'' and ''endo'' conformation, respectively. Tropol is N-(4-phenyl) phenacyl tropan-3-ol whereas ipratropium is 8-isopropyl-noratropine.3. Only phenthonium increased the frequency of miniature endplate potentials and the resting efflux of spontaneous [H-3]-ACh in rat diaphragm muscles.4. the rank order of the antimuscarinic potency was: ipratropium > atropine > phenthonium = endaphen > tropol. the rank order of the antinicotinic activity was: phenthonium = endophen > tropol > atropine > ipratropium.5. It is concluded that the prejunctional facilitatory effect of phenthonium is associated with the N-phenyl-phenacyl group at ''exo'' conformation but the effect is unrelated to its cholinolytic properties.
Palavra-chave MOTOR NERVE TERMINAL
TRANSMITTER RELEASE
MUSCARINIC ANTAGONIST
[H-3] ACH EFFLUX
Idioma Inglês
Data de publicação 1994-11-01
Publicado em General Pharmacology. Oxford: Pergamon-Elsevier B.V., v. 25, n. 7, p. 1397-1404, 1994.
ISSN 0306-3623 (Sherpa/Romeo, fator de impacto)
Publicador Elsevier B.V.
Extensão 1397-1404
Fonte http://dx.doi.org/10.1016/0306-3623(94)90164-3
Direito de acesso Acesso restrito
Tipo Artigo
Web of Science WOS:A1994PT75500014
Endereço permanente http://repositorio.unifesp.br/handle/11600/25442

Exibir registro completo




Arquivo

Arquivo Tamanho Formato Visualização

Não existem arquivos associados a este item.

Este item está nas seguintes coleções

Buscar


Navegar

Minha conta