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

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

Author information

1
Dipartimento di Scienze Chimiche, Universita degli Studi di Camerino, Via S. Agostino 1, 62032 Camerino, Italy.

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.

PMID:
19886609
DOI:
10.1021/jm901262f
[Indexed for MEDLINE]

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