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

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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

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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