Might Adrenergic α 2C -Agonists/α 2A -Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?
2009; American Chemical Society; Volume: 52; Issue: 22 Linguagem: Inglês
10.1021/jm901262f
ISSN1520-4804
AutoresClaudia Cardinaletti, Laura Mattioli, Francesca Ghelfi, Fabio Del Bello, Mario Giannella, Ariana Bruzzone, Hervé Paris, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia, Maria Pigini,
Tópico(s)Neuroscience and Neuropharmacology Research
ResumoThe 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 α2C-agonism/α2A-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to α2C-AR stimulation) and sedation overcoming (due to α2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine.
Referência(s)