Year: 2015
Type: article
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.
Source: Chemical Research in Toxicology
Institutions: University of Copenhagen, Copenhagen University Hospital
Language: English
Subfield: Toxicology
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $4,500
Funder: Lundbeckfonden
Awards: G277898384, G39191063, G6718954776
OpenAlex ID: W2210848389