Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions

被引：20

作者：

Gentili, Francesco ^{[1
]}

Cardinaletti, Claudia ^{[1
]}

Vesprini, Cristian ^{[1
]}

Ghelfi, Francesca ^{[1
]}

Farande, Aniket ^{[1
]}

Giannella, Mario ^{[1
]}

Piergentili, Alessandro ^{[1
]}

Quaglia, Wilma ^{[1
]}

Mattioli, Laura ^{[2
]}

Perfumi, Marina ^{[2
]}

Hudson, Alan

Pigini, Maria ^{[1
]}

机构：

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

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 16期

关键词：

D O I：

10.1021/jm800400k

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The study of two series of 2-aryl-ethylen-imidazolines 3-7 and 8-12 inspired by I(2)-IBS ligands phenyzoline (1) and diphenyzoline (2), respectively, confirmed the interesting "positive" or "negative" morphine analgesia modulation displayed by their corresponding leads and demonstrated that these effects might be correlated with morphine tolerance and dependence, respectively. By comparative examination of rationally designed compounds, some analogies between binding site cavity of I(2)-IBS proteins and alpha(2C)-adrenoreceptor emerged.

引用

页码：5130 / 5134

页数：5

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