Highly potent and selective zwitterionic agonists of the δ-opioid receptor. Part 1

…, WA Million, CL Nichols, JA Price, M Trevethick

Index: Middleton, Donald S.; Maw, Graham N.; Challenger, Clare; Jessiman, Alan; Johnson, Patrick S.; Million, William A.; Nichols, Carly L.; Price, Jenny A.; Trevethick, Michael Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 4 p. 905 - 910

Full Text: HTML

Citation Number: 8

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 ...