Salvinorin A is a hallucinogenic derived from the S. divinorum plant used in traditional spiritual practices of the Mazatec Indians and now gaining popularity as a recreational drug. Unlike other hallucinogens, which mediate their effects through serotonin 5-HT2A receptors, salvinorin A is a potent, selective κ opioid receptor agonist (Ki = 2.4 nM; EC50 = 1.8 nM). Salvinorin B is the major deacetylated metabolite of salvinorin A and reportedly lacks pharmacological activity. Alkoxymethyl ether derivatives of salvinorin B have been designed in an effort to develop selective antagonists or partial agonists of κ-opioid receptors with potential utility in the treatment of depression or mania and the general study of κ opioid receptor signaling.
