Analytical and Bioanalytical Chemistry
June 24, 2015
Achim T. Caspar, Andreas G. Helfer, Julian A. Michely et al.
69 citations
25I-NBOMe, a potent hallucinogenic drug that activates 5-HT2A receptors, is extensively metabolized in rats. After administration to male Wistar rats, 68 metabolites were identified in urine using liquid chromatography-high-resolution tandem mass spectrometry. The main metabolic pathways include O-demethylation, O,O-bis-demethylation, hydroxylation, and combinations, followed by glucuronidation and sulfation. Detection of intake is possible through metabolites using LC-MS methods but not by GC-MS standard urine screening. Initial tests indicate that CYP1A2 and CYP3A4 are involved in hydroxylation, while CYP2C9 and CYP2C19 mediate O-demethylation, suggesting potential drug-drug interactions.
Journal of Pharmaceutical and Biomedical Analysis
November 27, 2016
Achim T. Caspar, Simon D. Brandt, Andreas E. Stoever et al.
43 citations
25B-NBOMe and 25C-NBOMe, potent 5-HT2A receptor agonists linked to hallucinogenic effects and severe intoxications, are extensively metabolized in rats and humans. Using LC-HR-MS/MS, 66 metabolites were identified for 25B-NBOMe and 69 for 25C-NBOMe, primarily through O-demethylation, O,O-bis-demethylation, hydroxylation, and subsequent glucuronidation and sulfation. After low-dose administration to rats, both substances were detectable mainly via their metabolites using LC-based screening approaches. In an authentic human urine sample from an acute intoxication, 25B-NBOMe and its metabolites were detected by GC-MS as well. Initial screening showed CYP1A2 and CYP3A4 involvement in hydroxylation, and CYP2C9 and CYP2C19 in O-demethylation.
Current Neuropharmacology
November 3, 2016
Julian A. Michely, Sascha K. Manier, Achim T. Caspar et al.
36 citations
Two new psychoactive substances, 3-MeO-PCP and 3-MeOPCPy, are metabolized in rat and human liver microsomes through multiple pathways including hydroxylation, O-demethylation, and glucuronidation. Specific cytochrome P450 enzymes (CYP 2B6, 2C19, 2C9, 2D6) catalyze initial metabolic steps. Because only polymorphically expressed enzymes are involved, pharmacogenomic variations may affect metabolism, though clinical data are needed to confirm relevance. Standard urine screening approaches using GC-MS, LC-MSn, and LC-HR-MS/MS can detect intake of both drugs via identified metabolites.