Dataset Information


In Vitro Metabolism of 25B-NBF, 2-(4-Bromo-2,5-Dimethoxyphenyl)-N-(2-Fluorobenzyl)ethanamine, in Human Hepatocytes Using Liquid Chromatography?Mass Spectrometry.

ABSTRACT: 25B-NBF, 2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-fluorobenzyl)ethanamine, is a new psychoactive substance classified as a phenethylamine. It is a potent agonist of the 5-hydroxytryptamine receptor, but little is known about its metabolism and elimination properties since it was discovered. To aid 25B-NBF abuse screening, the metabolic characteristics of 25B-NBF were investigated in human hepatocytes and human cDNA-expressed cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes using liquid chromatography?high resolution mass spectrometry. At a hepatic extraction ratio of 0.80, 25B-NBF was extensively metabolized into 33 metabolites via hydroxylation, O-demethylation, bis-O-demethylation, N-debenzylation, glucuronidation, sulfation, and acetylation after incubation with pooled human hepatocytes. The metabolism of 25B-NBF was catalyzed by CYP1A1, CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2J2, CYP3A4, and UGT2B7 enzymes. Based on these results, it is necessary to develop a bioanalytical method for the determination of not only 25B-NBF but also its metabolites in biological samples for the screening of 25B-NBF abuse.


PROVIDER: S-EPMC6412758 | BioStudies | 2019-01-01

REPOSITORIES: biostudies

Similar Datasets

2015-01-01 | S-EPMC4534236 | BioStudies
2017-01-01 | S-EPMC5552776 | BioStudies
| S-EPMC2726048 | BioStudies
| PRJNA555610 | ENA
2019-01-01 | S-EPMC6838616 | BioStudies
| S-EPMC3871180 | BioStudies
1999-01-01 | S-EPMC1220242 | BioStudies
2019-01-01 | S-EPMC6484009 | BioStudies
2011-01-01 | S-EPMC3202326 | BioStudies
2018-01-01 | S-EPMC6073759 | BioStudies