Historical overview of psychoactive mushrooms

Psychoactive mushrooms have been used by humans for medical, recreational, religious, and ritual purposes since prehistory. They produce agents such as psilocybin, psilocin, ibotenic acid, and muscimol, which act on neurotransmitter receptors: psilocybin and psilocin are agonists at 5-HT1A and 5-HT2A/C receptors, ibotenic acid at glutamic acid receptors, and muscimol at GABAA receptors. A newer agent, aeruginascin, has been isolated. Psilocybin and psilocin show high therapeutic potential for obsessive-compulsive disorder, a difficult-to-treat nervous disease. This review covers the history, classification, distribution, and therapeutic effects of psychoactive mushrooms, with special attention to their use in Japan.

Study at a glance

Abstract

Humans have used psychoactive mushrooms for medical, recreational, religious and ritual purposes since pre-history. Previous studies have clarified that psychoactive mushrooms produce psychoactive agents such as psilocybin, psilocin, ibotenic acid, and muscimol. However, the status of psychoactive mushrooms in most countries as illegal hallucinogens has prevented full investigation of their biochemical properties. Recent studies have shown that many psychoactive agents pass through the blood-brain barrier and act on neurotransmitter receptors. Psilocybin and psilocin are 5-HT1A and 5-HT2A/C receptor agonists, respectively, while ibotenic acid is a glutamic acid receptor agonist and muscimol is a GABAA receptor agonist. A new psychoactive agent, aeruginascin, has also been isolated from psychoactive mushrooms, and it is expected that more useful compounds will be discovered as the technology of component analysis advances. In addition, it has been shown that psilocybin and psilocin have high therapeutic efficiency for obsessive-compulsive disorder, which is a difficult-to-treat nervous disease. The increase of nervous diseases in modern society has thus given new importance to psychoactive mushrooms. In this review, we summarize the history of the use of psychoactive mushrooms, from pre-history to the modern age, describe their classification and distribution, survey previous studies, and discuss their therapeutic effects for difficult-to-treat nervous disease. The utilization and distribution of psychoactive mushrooms in Japan is given special attention, as there are few articles on this subject.