10.1021/jm901262f.s001
Claudia Cardinaletti
Claudia
Cardinaletti
Laura Mattioli
Laura
Mattioli
Francesca Ghelfi
Francesca
Ghelfi
Fabio Del Bello
Fabio Del
Bello
Mario Giannella
Mario
Giannella
Ariana Bruzzone
Ariana
Bruzzone
Hervé Paris
Hervé
Paris
Marina Perfumi
Marina
Perfumi
Alessandro Piergentili
Alessandro
Piergentili
Wilma Quaglia
Wilma
Quaglia
Maria Pigini
Maria
Pigini
Might Adrenergic α<sub>2C</sub>-Agonists/α<sub>2A</sub>-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?
American Chemical Society
2009
oxyethylene bridge
steric bulk
Novel Therapeutic Tools
morphine analgesia modulation
adjuvant agents
Pain Treatment
ortho substituent
phenyl ring
position 2
α2
AR
2009-11-26 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Might_Adrenergic_sub_2C_sub_Agonists_sub_2A_sub_Antagonists_Become_Novel_Therapeutic_Tools_for_Pain_Treatment_with_Morphine_/2810173
The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided α<sub>2</sub>-adrenergic (AR) ligands endowed with significant α<sub>2C</sub>-agonism/α<sub>2A</sub>-antagonism. Similar behavior was displayed by cirazoline (<b>12</b>). For their positive morphine analgesia modulation (due to α<sub>2C</sub>-AR stimulation) and sedation overcoming (due to α<sub>2A</sub>-AR antagonism), <b>8</b> and <b>11</b> might be useful as adjuvant agents in the management of pain with morphine.