Metabolic Fate of Hallucinogenic NBOMes

Sebastian Leth-Petersen, Charlotte Gabel-Jensen, Nic Gillings, Szabolcs Lehel, Hanne D Hansen, Gitte M Knudsen, Jesper L Kristensen

40 Citationer (Scopus)

Abstract

2,5-Dimethoxy-N-benzylphenethylamines (NBOMes) are very potent 5-HT2AR agonists. Illicit use of these psychedelic compounds has emerged in recent years, and several fatalities have been linked to their recreational use. In its [(11)C]-labeled form, one NBOMe (25B-NBOMe) was recently developed as a PET-ligand for clinical investigations of 5HT2AR ([(11)C]Cimbi-36). Herein, we have identified the phase I and phase II metabolites of 25B-NBOMe in pigs as well as in humans. We find that the primary route of metabolism is 5'-demethylation, followed by conjugation to glucuronic acid. Carbon-11 labeling of 25B-NBOMe in three different positions followed by in vivo evaluation in pigs and humans corroborated these findings.

OriginalsprogEngelsk
TidsskriftChemical Research in Toxicology
Vol/bind29
Udgave nummer1
Sider (fra-til)96-100
Antal sider5
ISSN0893-228X
DOI
StatusUdgivet - 19 jan. 2016

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