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Chem Phys Lipids ; 154(1): 19-25, 2008 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-18407836

RESUMO

Fluorescent probe techniques were used to evaluate the effect of propoxycaine.HCl on the physical properties (transbilayer asymmetric lateral and rotational mobilities, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortex. An experimental procedure was used based on selective quenching of both 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer (RET) from the tryptophans of membrane proteins to Py-3-Py. Propoxycaine.HCl increased the bulk lateral and rotational mobilities, and annular lipid fluidity in SPMVs lipid bilayers, and had a greater fluidizing effect on the inner monolayer than that of the outer monolayer. The magnitude of increasing effect on annular lipid fluidity in SPMVs lipid bilayer induced by propoxycaine.HCl was significantly far greater than magnitude of increasing effect of the drug on the lateral and rotational mobilities of SPMVs lipid bilayer. It also caused membrane proteins to cluster. These effects of propoxycaine.HCl on neuronal membranes may be responsible for some, though not all, of the local anesthetic actions of propoxycaine.HCl.


Assuntos
Anestésicos Locais/farmacologia , Córtex Cerebral/metabolismo , Fluidez de Membrana/efeitos dos fármacos , Proteínas de Membrana/metabolismo , Propoxicaína/farmacologia , Membranas Sinápticas/efeitos dos fármacos , Animais , Bovinos , Relação Dose-Resposta a Droga , Transferência de Energia , Corantes Fluorescentes , Fluidez de Membrana/fisiologia , Proteínas de Membrana/química , Espectrometria de Fluorescência , Membranas Sinápticas/metabolismo
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