Characterization of the hepatic cytochrome P450 enzymes involved in the metabolism of 25I-NBOMe and 25I-NBOH.
Drug Testing and Analysis May 1, 2017 Line Marie Nielsen, Niels Bjerre Holm, Sebastian Leth-Petersen et al.
The NBOMe compounds, potent serotonin 5-HT2A receptor agonists used recreationally for their hallucinogenic effects, are metabolized primarily by specific cytochrome P450 enzymes. For 25I-NBOMe, CYP3A4 is the major enzyme involved; for 25I-NBOH, CYP2D6 is the major enzyme. 25I-NBOH also undergoes direct glucuronidation, which may reduce the impact of CYP2D6 genetic variation. The intrinsic clearance values were 70.1 mL/min/kg for 25I-NBOMe and 118.7 mL/min/kg for 25I-NBOH. Users of 25I-NBOMe may face drug-drug interactions if taken with a strong CYP3A4 inhibitor. Metabolites included hydroxylation, O-demethylation, N-dealkylation, and dehydrogenation products.