Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?
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.
Cardinaletti
Claudia
C
Dipartimento di Scienze Chimiche, Universita degli Studi di Camerino, Via S. Agostino 1, 62032 Camerino, Italy.
Mattioli
Laura
L
Ghelfi
Francesca
F
Del Bello
Fabio
F
Giannella
Mario
M
Bruzzone
Ariana
A
Paris
Hervé
H
Perfumi
Marina
M
Piergentili
Alessandro
A
Quaglia
Wilma
W
Pigini
Maria
M
D000277:Adjuvants, Pharmaceutic / Q000494:pharmacology; D058647:Adrenergic alpha-2 Receptor Agonists; D058669:Adrenergic alpha-2 Receptor Antagonists; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D016466:CHO Cells; D003000:Clonidine / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D055808:Drug Discovery; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology; D009020:Morphine / Q000627:therapeutic use*; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism; D018341:Receptors, Adrenergic, alpha-2
C547768:ADRA2A protein, human; D000277:Adjuvants, Pharmaceutic; D058647:Adrenergic alpha-2 Receptor Agonists; D058669:Adrenergic alpha-2 Receptor Antagonists; D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D000700:Analgesics; D007093:Imidazoles; D018341:Receptors, Adrenergic, alpha-2; D009020:Morphine; D003000:Clonidine; C014282:cirazoline