A Review of Salvinorin Analogs and their Kappa-Opioid Receptor Activity
Bioorganic & Medicinal Chemistry Letters March 12, 2018 Jeremy J Roach, R. Shenvi
Salvinorin A, a plant metabolite, is a potent and selective agonist of the human kappa-opioid receptor, which is being investigated as a target for new painkillers. This review examines analogs of the salvinorin chemotype and how modifications affect their selectivity, affinity, and potency. Extensive modifications to the periphery of the molecule, using isolated salvinorin A, have provided a wealth of structure-activity relationship (SAR) data. Recent advances in chemical synthesis now enable more fundamental changes to the core structure.