Psychedelic effects of psilocybin correlate with serotonin 2A receptor occupancy and plasma psilocin levels

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• psilocybin

• Psychedelic effects are believed to emerge through stimulation of serotonin 2A receptors (5-HT2ARs) by psilocybin’s active metabolite, psilocin.

• irst time the relationship between intensity of psychedelic effects, cerebral 5-HT2AR occupancy and plasma levels of psilocin in humans.

• first time the relationship between intensity of psychedelic effects, cerebral 5-HT2AR occupancy and plasma levels of psilocin in humans.

• We here show that psilocybin ingestion of between 3 and 30 mg is associated with dose-dependent occupancy of cerebral 5-HT2ARs.

• 5-HT2AR occupancy are positively associated and the relationship conforms with a single-site binding mode

• psychedelic effects of psilocybin

• are closely

• correlated with psilocin stimulation of the 5-HT2AR