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Eur Biophys J ; 40(8): 981-6, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21671152

RESUMO

The activity of dehydroleucodine, a sesquiterpene lactone obtained from Artemisia douglasiana, was studied in mice small intestinal transit. Its mechanism was evaluated in the presence of several adrenergic and cholinergic antagonist drugs and one opioid antagonist. Docking of dehydroleucodine into the homology model of the α2-adrenergic receptor allowed us to analyze the structural basis of their interactions. The experiments showed that dehydroleucodine delayed intestinal transit. The docking of dehydroleucodine showed a unique binding site, equivalent to the binding site of carozolol in the ß-adrenergic receptor. The results suggested that dehydroleucodine produced an inhibitory effect on intestinal transit. Its action could be mediated, at least in part, through the α2-adrenergic receptor.


Assuntos
Motilidade Gastrointestinal/efeitos dos fármacos , Lactonas/química , Lactonas/farmacologia , Receptores Adrenérgicos alfa 1/química , Receptores Adrenérgicos alfa 2/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Animais , Intestino Delgado/efeitos dos fármacos , Camundongos , Fentolamina/antagonistas & inibidores , Receptores Adrenérgicos alfa 1/metabolismo , Receptores Adrenérgicos alfa 2/metabolismo , Receptores Adrenérgicos beta/química , Receptores Adrenérgicos beta/metabolismo , Ioimbina/antagonistas & inibidores
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