Might Adrenergic alpha2C-Agonists/alpha2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?

CARDINALETTI C; MATTIOLI L; GHELFI F; DEL BELLO F; GIANELLA M; BRUZZONE A; PARIS H; PERFUMI M; PIERGENTILI A; QUAGLIA W; PIGINI M

JOURNAL OF MEDICINAL CHEMISTRY

American Chemical Society

Lugar: United States ; Año: 2009 vol. 52 p. 7319 - 7322

0022-2623

The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided R2-adrenergic (AR) ligands endowed with significantR2-adrenergic (AR) ligands endowed with significant R2C-agonism/R2A-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to R2C-AR stimulation) and sedation overcoming (due to R2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. morphine analgesia modulation (due to R2C-AR stimulation) and sedation overcoming (due to R2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. morphine analgesia modulation (due to R2C-AR stimulation) and sedation overcoming (due to R2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. 2C-agonism/R2A-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to R2C-AR stimulation) and sedation overcoming (due to R2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine. R2C-AR stimulation) and sedation overcoming (due to R2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine.8 and 11 might be useful as adjuvant agents in the management of pain with morphine.