Stilbenes as 魏-Selective, Non-nitrogenous Opioid Receptor Antagonists

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• 作者：Alyssa M. Hartung ; John A. Beutler ; Hern谩n A. Navarro ; David F. Wiemer ; Jeffrey D. Neighbors
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：February 28, 2014
• 年：2014
• 卷：77
• 期：2
• 页码：311-319
• 全文大小：431K
• 年卷期：v.77,no.2(February 28, 2014)
• ISSN：1520-6025

文摘

The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the 魏 receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features. Assays on these compounds determined that one (compound 29) shows potent opioid receptor binding activity and significantly improved selectivity for the 魏 receptor. These studies begin to illuminate the structural features of these non-nitrogenous opioid receptor antagonists that are required for activity.