作者: Achim T. Caspar , Andreas G. Helfer , Julian A. Michely , Volker Auwärter , Simon D. Brandt
DOI: 10.1007/S00216-015-8828-6
关键词: Urine 、 CYP1A2 、 Designer drug 、 CYP3A4 、 Chemistry 、 Sulfation 、 25I-NBOMe 、 Glucuronidation 、 Pharmacology 、 Hydroxylation
摘要: 25I-NBOMe, a new psychoactive substance, is potent 5-HT2A receptor agonist with strong hallucinogenic potential. Recently, it was involved in several fatal and non-fatal intoxication cases. The aim of the present work to study its phase I II metabolism detectability urine screening approaches. After application 25I-NBOMe male Wistar rats, collected over 24 h. metabolites were identified by LC-HR-MS/MS after suitable workup. For studies, standard approaches (SUSA) GC-MS, LC-MSn, applied rat also authentic human samples submitted for toxicological analysis. Finally, an initial CYP activity performed identify isoenzymes major metabolic steps. mainly metabolized O-demethylation, O,O-bis-demethylation, hydroxylation, combinations these reactions as well glucuronidation sulfation main metabolites. All all, 68 could be identified. Intake detectable via both LC-MS approaches, but not GC-MS SUSA. Initial revealed involvement CYP1A2 CYP3A4 hydroxylation CYP2C9 CYP2C19 O-demethylation. presented demonstrated that extensively detected only Since are steps, drug–drug interactions might occur certain constellations.