The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I2-IBS ligands phenyzoline (1) and diphenyzoline (2), respectively, confirmed the interesting “positive” or “negative” morphine analgesia modulation displayed by their corresponding leads and demonstrated that these effects might be correlated with morphine tolerance and dependence, respectively. By comparative examination of rationally designed compounds, some analogies between binding site cavity of I2-IBS proteins and alpha2C-adrenoreceptor emerged
Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions
GENTILI, Francesco;CARDINALETTI, CLAUDIA;GHELFI, Francesca;FARANDE, ANIKET VIJAYKUMAR;GIANNELLA, Mario;PIERGENTILI, Alessandro;QUAGLIA, Wilma;MATTIOLI, LAURA;PERFUMI, Marina Cecilia;PIGINI, Maria
2008
Abstract
The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I2-IBS ligands phenyzoline (1) and diphenyzoline (2), respectively, confirmed the interesting “positive” or “negative” morphine analgesia modulation displayed by their corresponding leads and demonstrated that these effects might be correlated with morphine tolerance and dependence, respectively. By comparative examination of rationally designed compounds, some analogies between binding site cavity of I2-IBS proteins and alpha2C-adrenoreceptor emergedFile in questo prodotto:
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