Hallucinogen actions on human brain revealed

摘要

With regard to hallucinogens like psilocybin—an ingredient of so-called "magic mushrooms" (e.g., Psilocybe cubensis)—it may be high time to reconsider long-standing hypotheses related to their actions in the human brain. Although psilocin (the active metabolite of psilocybin) (Fig. 1A) and other classical hallucinogens like lysergic acid dieth-ylamide (LSD) have complex pharmacologies with high affinities for multiple neurotransmitter receptors (1), it has long been appreciated that their psychedelic actions correlate best with 5-HT_(2A)-serotonin receptor agonism (2). Indeed, in 5-HT_(2A) knockout mice, classical hallucinogens are devoid of activity (3, 4). Importantly, the psychedelic actions of psilocybin in humans are abolished by pretreatment with relatively selective 5-HT_(2A) antagonists (5, 6).