Psilocin, also known as 4-hydroxy-N,N-dimethyltryptamine (4-HO-DMT), is a psychedelic drug and fungal alkaloid of the tryptamine and 4-hydroxytryptamine families. Along with its phosphate ester psilocybin, it is found in most species of psilocybin-containing mushrooms, such as Psilocybe cubensis and Psilocybe mexicana, and is the compound responsible for their hallucinogenic effects, although concentrations of psilocin are variably lower than those of psilocybin. The drug is taken orally and its effects include perceptual changes and visual effects, emotional changes, ego dissolution, time dilation, and mystical experiences, among others. Synthetic acyl esters such as 4-AcO-DMT (psilacetin; O-acetylpsilocin) and 4-PrO-DMT (O-propionylpsilocin), are prodrugs of psilocin and have similar properties and effects. More recently, MSP-1014 has emerged as a novel prodrug of psilocin under development for the treatment of major depressive disorder. Psilocin acts as a non-selective serotonin receptor agonist, including of the serotonin 5-HT2A receptor among others. The drug produces its hallucinogenic effects specifically via activation of the serotonin 5-HT2A receptor. However, other serotonin receptors, such as the serotonin 5-HT1A and 5-HT2C receptors, may also contribute to its effects. Notable analogues of psilocin include dimethyltryptamine (DMT), its positional isomer bufotenin (5-HO-DMT), its higher homologue 4-HO-MET (metocin), and others. Psilocin and psilocybin were discovered via isolation from psilocybin-containing mushrooms by Albert Hofmann in 1958. This followed the Western re-discovery of psilocybin-containing mushrooms by Robert Gordon Wasson and Valentina Pavlovna Wasson in Mexico in 1955. Psilocin, in the form of psilocybin, psilocybin-containing mushrooms, and other prodrugs such as 4-AcO-DMT, is a widely used entheogen as well as recreational psychedelic drug. Psilocybin and psilocin became controlled substances in the United States and internationally under the United Nations in 1971. Since then, psilocin, as the active form of psilocybin, has become of interest for potential use in medicine to treat psychiatric disorders such as depression. Psilocybin was approved for such purposes in Australia in 2023 and is in late-stage clinical trials in the United States and other countries.
Use and effects
Psilocin is used recreationally, spiritually or shamanically, and medically. It is most commonly used in the form of its prodrugs such as psilocybin and 4-AcO-DMT (psilacetin). However, psilocin may also be used itself, either in the form of psilocybin-containing mushrooms (which variably contain psilocin up to similar amounts as psilocybin) or in synthetic form. Psilocin is usually used orally, but may also be taken intravenously. In terms of dose, it is slightly more potent than psilocybin, about 1.4-fold so (i.e., 1.4 mg psilocybin equals about 1.0 mg psilocin). This is related to psilocin's lack of ester prodrug moiety, which results in its molecular weight being about 40% lower than that of psilocybin (204 g/mol and 284 g/mol, respectively). The human dose of psilocin has been given as 10 to 20 mg orally. In his book TiHKAL (Tryptamines I Have Known and Loved), Alexander Shulgin described the properties and effects of psilocin, either as psilocin itself, as a prodrug like psilocybin or 4-AcO-DMT, or as Psilocybe cubensis mushrooms. The dose, regardless of form, was listed as 10 to 20 mg orally and the duration as 3 to 6 hours. The onset, in the case of psilocin specifically, was 15 to 40 minutes. The perceptual and related effects included brightened colors, increased visual contrast, closed-eye visuals such as patterns, textures, and colors, open-eye visuals such as colors, distortions, and movement, pareidolia, increased appreciation of scenery, perceiving beauty, and enhanced imagination. Other effects variably included feeling intoxicated, high, and/or stimulated, feelings of peacefulness and serenity, emotional amplification, mood swings, feelings of neuroticism and introversion, feelings of despair, apathy, and unpleasantness, anxiety, confusion, distractibility, impairment, and feeling heavy and tired. Side effects included chills, nausea, vomiting, and motion sickness, but no hangover. In other reports, the effects observed after ingestion of psilocin can include but are not limited to tachycardia, dilated pupils, restlessness or arousal, euphoria, open and closed eye visuals (common at medium to high doses), synesthesia (e.g. hearing colors and seeing sounds), increased body temperature, headache, sweating and chills, and nausea.
Contraindications
Side effects
There has been no direct lethality associated with psilocin. There has been no reported withdrawal syndrome when chronic use of this drug is ceased. There is cross tolerance among psilocin, mescaline, lysergic acid diethylamide (LSD), and other psychedelics due to downregulation of these receptors.
Overdose
Interactions
Pharmacology
Pharmacodynamics
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