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

Article Details

Citation

Cardinaletti C, Mattioli L, Ghelfi F, Del Bello F, Giannella M, Bruzzone A, Paris H, Perfumi M, Piergentili A, Quaglia W, Pigini M

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

J Med Chem. 2009 Nov 26;52(22):7319-22. doi: 10.1021/jm901262f.

PubMed ID
19886609 [View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
Drug Target Property Measurement pH Temperature (°C)
Norepinephrine Alpha-2A adrenergic receptor EC 50 (nM) 371.54 N/A N/A Details
Norepinephrine Alpha-2C adrenergic receptor EC 50 (nM) 794.33 N/A N/A Details