Stilbenes as Îº-Selective, Non-nitrogenous Opioid Receptor Antagonists
Hartung | Alyssa M. | Beutler | John A. | Navarro | HernaÌn A. | Wiemer | David F. | Neighbors | Jeffrey D.
The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the Îº 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 Îº receptor. These studies begin to illuminate the structural features of these non-nitrogenous opioid receptor antagonists that are required for activity.Show more [+] Less [-]