Metabolic Fate of Hallucinogenic NBOMes

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• 作者：Sebastian Leth-Petersen ; Charlotte Gabel-Jensen ; Nic Gillings ; Szabolzs Lehel ; Hanne D. Hansen ; Gitte M. Knudsen ; Jesper L. Kristensen
• 刊名：Chemical Research in Toxicology
• 出版年：2016
• 出版时间：January 19, 2016
• 年：2016
• 卷：29
• 期：1
• 页码：96-100
• 全文大小：326K
• ISSN：1520-5010

文摘

2,5-Dimethoxy-N-benzylphenethylamines (NBOMes) are very potent 5-HT2_AR agonists. Illicit use of these psychedelic compounds has emerged in recent years, and several fatalities have been linked to their recreational use. In its [¹¹C]-labeled form, one NBOMe (25B-NBOMe) was recently developed as a PET-ligand for clinical investigations of 5HT_2AR ([¹¹C]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.