The pharmacology of psilocybin

Abstract

Psilocybin (4-phosphoryloxy-N,N-dimethyltryptamine) is the major psychoactive alkaloid of some species of mushrooms distributed worldwide. These mushrooms represent a growing problem regarding hallucinogenic drug abuse. Despite its experimental medical use in the 1960s, only very few pharmacological data about psilocybin were known until recently. Because of its still growing capacity for abuse and the widely dispersed data this review presents all the available pharmacological data about psilocybin.

Occurrence and use of hallucinogenic mushrooms containing psilocybin alkaloids

“…Depending on the individual, an intake of 4-10 mg psilocybin/psilocin, or 1-2 g of the dried Psilocybe mushroom, results in effects searched for. These psychic effects include stimulation, enhanced ability for introspection and altered psychological functioning in the direction of Freudian primary processes, also known as hypnagogic experience and dreams (Passie et al, 2002). Especially noteworthy are generally pleasant sensation of intellectual and bodily relaxation and detachment from the environment (perceptual changes such as illusions, synaestesias, affective activation, and alterations of thought and time sense), without producing a setback.…”

“…Other metabolites found in lower quantities include 4-hydroxyindole-3-yl-acetaldehyde, 4-hydroxyindole-3-yl-acetic acid, and 4-hydroxytryptophol (Holzmann, 1995;Hasler et al, 1997). A possible metabolic scheme for psilocybin in humans has been suggested by Passie et al (2002).…”

The effect of particular active substances of hallucinogenic mushrooms

“…Such mental syndrome, caused by various reasons, is often dangerous and may be trigger the development of severe pathologies of mental nature, including states similar to some forms of schizophrenia (Hyde et al 1978, McDonald 1980. Due to reasons mentioned above, psilocybin and psilocin are being currently used in animal models investigating substrates of schizophrenia (Stebelska 2013 , its' distribution in the body is rather uniform (Hopf & Eckert 1974, Passie et al 2002. In the body psilocybin under the influence of alkaline phosphatase, is the subject to dephosphorylation and is converted to psilocin, which is the main and perhaps the only substance showing psychopharmacological activity.…”

“…In the body psilocybin under the influence of alkaline phosphatase, is the subject to dephosphorylation and is converted to psilocin, which is the main and perhaps the only substance showing psychopharmacological activity. About 8 hours after ingestion, the concentration of this substance in the tissues is very low, albeit in the liver and adrenal glands it remains even to about 48 hours (Hopf & Eckert 1974, Passie et al 2002, Stebelska 2013.…”

At-Line Cellular Screening Methodology for Bioactives in Mixtures Targeting the α7-Nicotinic Acetylcholine Receptor

“…Then, the methodology was applied to the screening of an extract of a Psilocybe mushroom, which is known for its hallucinogenic effects. The effect of known hallucinogenic compounds, like psilocybin, is associated with their affinity for the 5-hydroxitryptamine receptor, 23,24 but the activity of compounds in hallucinogenic mushrooms on the α7-nAChR has not been investigated. The developed screening technique allows the direct correlation of bioactivity to the m/z values of the corresponding compounds.…”