Might Adrenergic α2C-Agonists/α2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?

被引：15

作者：

Cardinaletti, Claudia ^{[1
]}

Mattioli, Laura ^{[2
]}

Ghelfi, Francesca ^{[1
]}

Del Bello, Fabio ^{[1
]}

Giannella, Mario ^{[1
]}

Bruzzone, Ariana ^{[3
]}

Paris, Herve ^{[4
]}

Perfumi, Marina ^{[2
]}

Piergentili, Alessandro ^{[1
]}

Quaglia, Wilma ^{[1
]}

Pigini, Maria ^{[1
]}

机构：

[1] Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy

[2] Univ Camerino, Dipartimento Med Sperimentale & Sanita Publ, I-62032 Camerino, Italy

[3] Consejo Nacl Invest Cient & Tecn, Inst Biol & Med Expt, RA-1033 Buenos Aires, DF, Argentina

[4] CHU Rangueil, INSERM, U858, I2MR, F-31432 Toulouse 4, France

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 22期

关键词：

ALPHA(2)-ADRENORECEPTORS PROFILE MODULATION; ANALOGS; ANALGESIA; AGONIST; ANTAGONIST; CIRAZOLINE; SERIES;

D O I：

10.1021/jm901262f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：7319 / 7322

页数：4

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