Novel Ligands Rationally Designed for Characterizing I2−Imidazoline Binding Sites Nature and Functions
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- 作者：Francesco Gentili ; Claudia Cardinaletti ; Cristian Vesprini ; Francesca Ghelfi ; Aniket Farande ; Mario Giannella ; Alessandro Piergentili ; Wilma Quaglia ; Laura Mattioli ; Marina Perfumi ; Alan Hudson ; Maria
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：August 28, 2008
- 年：2008
- 卷：51
- 期：16
- 页码：5130-5134
- 全文大小：174K
- 年卷期：v.51,no.16(August 28, 2008)
- ISSN：1520-4804
文摘
The study of two series of 2-aryl-ethylen-imidazolines 3−7 and 8−12 inspired by I2−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 I2−IBS proteins and α2C-adrenoreceptor emerged.