Might Adrenergic α2C-Agonists/α2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?

Cardinaletti, Claudia; Mattioli, Laura; Ghelfi, Francesca; Bello, Fabio Del; Giannella, Mario; Bruzzone, Ariana; Paris, Hervé; Perfumi, Marina; Piergentili, Alessandro; Quaglia, Wilma; Pigini, Maria

doi:10.1021/jm901262f.s001

jm901262f_si_001.pdf (96.47 kB)

Might Adrenergic α_2C-Agonists/α_2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?

journal contribution

posted on 2009-11-26, 00:00 authored by Claudia Cardinaletti, Laura Mattioli, Francesca Ghelfi, Fabio Del Bello, Mario Giannella, Ariana Bruzzone, Hervé Paris, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia, Maria Pigini

The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided α₂-adrenergic (AR) ligands endowed with significant α_2C-agonism/α_2A-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to α_2C-AR stimulation) and sedation overcoming (due to α_2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine.