Selective natural kappa opioid and cannabinoid receptor agonists with a potential role in the treatment of gastrointestinal dysfunction.

Salvinorin A is the major active ingredient of Salvia divinorum, a plant used by the Mazatec Indians of Mexico for spiritual and medical purposes. Different preparations from S. divinorum are also used in traditional healing practices to treat gastrointestinal disorders, including diarrhea. The recent extensive research on salvinorin A and other neoclerodane diterpenoids derived from S. divinorum resulted in a large number of reports describing their isolation, synthesis and structure-activity relationship. This review summarizes the present knowledge on salvinorin A and its analogues, with a focus on the effects on gastrointestinal tissues. We furthermore discuss structural changes in salvinorin A that may facilitate future use of its derivatives in human disease.