Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions

Gentili, Francesco; Cardinaletti, Claudia; Vesprini, C.; Ghelfi, Francesca; Farande, Aniket Vijaykumar; Giannella, Mario; Piergentili, Alessandro; Quaglia, Wilma; Mattioli, Laura; Perfumi, Marina Cecilia; Hudson, A.; Pigini, Maria

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

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Titolo:	Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions
Autori:	GENTILI, Francesco CARDINALETTI, CLAUDIA VESPRINI C. GHELFI, Francesca FARANDE, ANIKET VIJAYKUMAR GIANNELLA, Mario PIERGENTILI, Alessandro QUAGLIA, Wilma MATTIOLI, LAURA PERFUMI, Marina Cecilia HUDSON A. PIGINI, Maria mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2008
Rivista:	JOURNAL OF MEDICINAL CHEMISTRY
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
Handle:	http://hdl.handle.net/11581/200592
Appare nelle tipologie:	Articolo

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