Author/Authors :
Barbara Czak?، نويسنده , , J?nos Marton، نويسنده , , S?ndor Berényi، نويسنده , , Katarzyna Gach، نويسنده , , Jakub Fichna، نويسنده , , Martin Storr، نويسنده , , Geza Toth، نويسنده , , Attila Sipos، نويسنده , , Anna Janecka، نويسنده ,
Abstract :
A set of novel 6-substituted orvinols was synthesized and pharmacologically characterized in order to explore the effect of the polarity and steric effects of these new moieties on the opioid activity. It was revealed that longer 6-O-alkyl chains led to increased agonistic activities, while the lack of C6-etheral oxygen gave rise to an antagonistic profile at the opioid receptors in the mouse ileum.
Keywords :
Analgesics , Orvinols , Partial agonism , Drug abuse , DFT study
