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salvinorin A "is the most potent naturally occurring hallucinogen." It is active at doses as low as 200 µg. Synthetic chemicals, such as LSD (active at 20–30 µg doses), can be more potent.Research has shown that salvinorin A is a potent and selective κ-Opioid (kappa-Opioid) receptor agonist. It has been reported that the effects of salvinorin A in mice are blocked by κ-Opioid receptor antagonist However, it is an even more potent D2 receptor partial agonist, and it is likely this action plays a significant role in its effects as well. Salvinorin A has no actions at the 5-HT2A serotonin receptor, the principal molecular target responsible for the actions of 'classic' hallucinogens, such as mescaline and LSD, nor is it known to have affinity for any other sites to date.

Salvinorin's potency should not be confused with toxicity. Rodents chronically exposed to dosages, many times greater than those to which humans are exposed, did not show signs of organ damage