The natural stilbene pawhuskin A
has been shown to function as
an opioid receptor antagonist, with preferential binding to the κ
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 κ receptor. These studies begin to illuminate the structural
features of these non-nitrogenous opioid receptor antagonists that
are required for activity.