Article ID Journal Published Year Pages File Type
1372855 Bioorganic & Medicinal Chemistry Letters 2009 5 Pages PDF
Abstract

We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus the mu and kappa opioid receptors. This study uncovered compounds with improved agonist potency and selectivity compared to the standard, non-peptidic delta agonist SNC-80. In vivo anti-nociceptive activity of analog 8e in two rodent models is discussed, demonstrating the potential of delta agonists to provide a novel mechanism for pain relief.

Graphical abstractPhenolic diaryl amino piperidines were found to have excellent agonist potency at the delta opioid receptor. Compound 8e displays in vivo anti-nociceptive activity in two rodent models.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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