Work

Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists

Year: 2014

Type: article

Abstract: 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.

Source: Journal of Natural Products

DOI: 10.1021/np4009046

Authors: Alyssa M. Hartung, John A. Beutler, Hernán A. Navarro, David F. Wiemer, Jeffrey D. Neighbors

Institutions: University of Iowa, National Cancer Institute, Center for Cancer Research, RTI International

Language: English

Topic: Neuropeptides and Animal Physiology

Subfield: Cellular and Molecular Neuroscience

Field: Neuroscience

Domain: Life Sciences

Open Access status: hybrid

Estimated APC paid: $4,500

Funders: National Cancer Research Institute, National Institutes of Health, National Institute on Drug Abuse, National Cancer Institute