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
2008-01-01

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 emerged
2008
262
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/200592
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