Article ID Journal Published Year Pages File Type
1379250 Bioorganic & Medicinal Chemistry Letters 2006 6 Pages PDF
Abstract

A series of zwitterionic δ-opioid agonists, with targeted physicochemistry, as a strategy to limit potential for CNS exposure, were prepared. These agents were found to possess exquisite potency and selectivity over mu and κ-opiate activity. Furthermore, analogue 3a was found to display restricted CNS exposure, as evidenced by its inactivity in a rodent hyperlocomotion assay of central opiate activity. Dog pharmacokinetic studies on 3a indicated encouraging oral bioavailability.

Graphical abstractA series of potent and selective zwitterionic δ-opioid agonists (2) and (3) are described.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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