Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379250 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Donald S. Middleton, Graham N. Maw, Clare Challenger, Alan Jessiman, Patrick S. Johnson, William A. Million, Carly L. Nichols, Jenny A. Price, Michael Trevethick,