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Abstract: Salvia divinorum is a hallucinogenic plant used by the Mazatec Indians of Mexico for traditional spiritual ceremonies. The active constituent, salvinorin A, induces profound hallucinations, however the biological mechanism for this action is not known. Affinity-binding studies suggest that the biologic activity of salvinorin A involves the κ-opioid receptor. The purpose of this study was to evaluate the antinociceptive effect of salvinorin A in mice. Salvinorin A and opioid receptor antagonists were administered intrathecally and the tail-flick latencies were used as a measure of antinociception. Salvinorin A increased tail-flick latencies in a dose-dependent manner (13.9–23.1 nmol) compared to control trials. Pretreatment with the κ-opioid receptor antagonist nor-binaltorphimine attenuated the salvinorin A induced increase in tail-flick latency. In contrast, neither the μ-opioid receptor antagonist β-funaltrexamine nor δ-opioid receptor antagonist naltrindole significantly affected the antinociceptive response of salvinorin A administration. These data support previous reports that salvinorin A represents a unique non-alkaloidal agonist for the κ-opioid receptor. [Copyright &y& Elsevier]

Salvia divinorum is a sage endemic to a small region of Mexico and has been traditionally used by the Mazatec Indians for divination and spiritual healing. Recently, it has gained increased popularity as a recreational drug, used by adolescents and young adults as an alternative to marijuana and LSD. Salvinorin A, the major active ingredient of the plant, is considered to be the most potent known hallucinogen of natural origin. This review surveys the current state of knowledge on the neurochemical, pharmacokinetic, and pharmacological properties of salvinorin A, the trends and motivation behind S. divinorum use, and the health problems among users of the plant's products. S. divinorum induces intense, but short-lived, psychedelic-like changes in mood and perception, with concomitant hallucinations and disorientation. Many websites have misinterpreted the limited existing research-based information on the side effects of salvia as evidence for its safety. However, data accumulated over the last few years indicate that potential health risks are associated with the use of S. divinorum, especially by teenagers, users of other substances of abuse, and individuals with underlying psychotic disturbances. Taken together, the data presented in this review point to the need for further basic and clinical studies to create a basis for the development of well-addressed prevention and treatment strategies., (Copyright © 2013 John Wiley & Sons, Ltd.)