Journal of medicinal and pharmaceutical chemistry 2009-11-26

Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?

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

Index: J. Med. Chem. 52 , 7319-22, (2009)

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Abstract

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