Pharmaceutical Sciences Faculty Presentations
Novel κ-opioid Receptor Antagonists Derived from Salvinorin A
Document Type
Poster Session
Event Date
2007
Conference/Event
International Narcotics Research Conference
Location
Berlin, Germany
Abstract
Salvinicins A and B are neoclerodane diterpenes from the Mexican mint Salvia divinorum. These compounds are congeners of salvinorin A, one of the major metabolites of S. divinorum and a selective κ-opioid receptor ligand. Naturally occurring compounds possessing a furan ring, for example salvinorin A, are of limited medicinal value due to their potential to produce hepatotoxic eff ects. Preparation of salvinicin-like analogues was undertaken in order to further delineate structure-activity relationships and to identify compounds with reduced hepatotoxic potential. Two of these analogues were found to possess κ antagonist activity and are the fi rst neoclerodane diterpenes reported to display such activity. The synthetic routes to these compounds along with their activity at opioid receptors will be presented. This research is funded by a grant from the National Institute on Drug Abuse (DA 18151).
Keywords
Kappa opioids, salvinorin A, pharmacy, narcotics
Recommended Citation
Simpson, Denise S.; Katavic, Peter L.; Lozama, Anthony; Harding, Wayne W.; Parrish, Damon; Deschamps, Jeffrey R.; Dersch, Christina M.; Rothman, Richard B.; Navarro, Hernan; and Prisinzano, Thomas E., "Novel κ-opioid Receptor Antagonists Derived from Salvinorin A" (2007). Pharmaceutical Sciences Faculty Presentations. 46.
https://digitalcommons.cedarville.edu/pharmaceutical_sciences_presentations/46
