Salvinorin A, a hallucinogen from Salvia divinorum, may serve as a therapeutic for stimulant abuse, but no methods exist to detect it or its metabolites in biological fluids. This work describes a straightforward synthesis of a deuterium-labeled analog of salvinorin A and its use as an internal standard for detecting salvinorin A and its metabolites in biological fluids using LC-MS, providing a tool for studying its metabolism and potential therapeutic development.
Salvinorin A, a hallucinogen from the plant Salvia divinorum, is unique as the first non-nitrogenous compound known to bind to opioid receptors. To understand why it selectively targets kappa opioid receptors, researchers systematically altered its structure and tested the effects on receptor binding and activity. This work describes chemical transformations of salvinorin A, including a semisynthesis of salvinicins A and B. It also identifies compound 10a as the first neoclerodane diterpene with delta opioid antagonist activity, providing new tools for studying opioid receptor interactions.