Drug intelligence / Profile preview

bufotenine

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
Inhalation, Intranasal, Oral, Intravenous, Intramuscular, Topical
01

Overview

Bufotenine is a naturally occurring hallucinogenic indole alkaloid and serotonin analog found in the skins of certain frogs and toads (notably in toad poison), mushrooms such as Amanita muscaria, higher plants like Piptadenia peregrina (yopo), and mammals including humans[1][2][3][4]. It was first isolated in 1934. Bufotenine is structurally related to serotonin and psilocin but differs in its pharmacokinetics and blood-brain barrier permeability[2]. It acts primarily as a serotonergic psychedelic of the tryptamine family. Its mechanism involves binding to serotonin receptors—specifically the 5-HT2A and 5-HT2C subtypes—where it can act as an agonist or modulator[3][5][8]. Bufotenine has been used experimentally for central nervous system studies but is not approved for medical use; it has also been misused recreationally for its psychedelic effects. In animal models, it shows mild behavioral alterations at high doses with possible anxiogenic or sedative effects[5]. There are experimental indications that bufotenine may inhibit rabies virus infection by interfering with viral entry into cells; however, its precise antiviral mechanism remains under investigation[6].

Other names
bufotenine5-hydroxy-N,N-dimethyltryptamine5-HO-DMTdimethylserotonin
02

Targets

5-HT (Serotonin receptors)5-HT2C (5-hydroxytryptamine receptor 2C)SERT (Sodium-dependent serotonin transporter)

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