Extraction and Exploration of a Novel Selective Kappa Opioid Ligand.

Gordon, James

Salvinorin A is a neoclerodane diterpene and is the active component in plant, Salvia divinorum. This compound has been shown to be a potent kappa opioid agonist in vitro and in vivo. At this moment, salvinorin A is the only known naturally occurring nonnitrogenous kappa opioid selective ligand. Its selectivity and activity at the kappa opioid receptor makes it a possible novel treatment for substance abuse. This is because kappa opioid agonists have been shown to antagonize the effects of central nervous stimulants by regulating the effect of dopamine in the brain; thereby, diminishing the stimulating effects of cocaine. In addition, kappa opioid agonists also have analgesic properties, so salvinorin A could also be a potential analgesia. As part of our ongoing research, we have successfully optimized a procedure to extract salvinorin A from the leaves of Salvia divinorum; we are also exploring analogues of Salvinorin A using structure-activity relationship studies.

Prisinzano, T.E., W. Harding, K. Tidgewell and * N. Echebiri. College of Pharmacy, Medicinal Natural Product Chemistry Department, University of Iowa and Department of Agriculture and Natural Sciences, Lincoln University.