Thin-layer chromatographic characterization of metabolites formed from an AMPA antagonist drug candidate

K. Migléczi, I. Hazai, K. Jemnitz, M. Pátfalusi

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

A pilot study has been conducted to develop sample preparation procedure and TLC separation of radiolabeled metabolites of an AMPA (2-amino-3-(3-hydroxymethylisoxazol-4-yl)propionic acid) antagonist drug (6-(4-aminophenyl)-8-chloro-2-methyl-11H-imidazo[1,2c] [2,3] benzodiazepine). The N-acetyl metabolite was identified by chromatography and mass spectrometry. Both in vivo experiments with experimental animals and in vitro study with rat hepatocytes indicated that the N-acetylation reaction is very important in the metabolism of the compound investigated. N-Acetylation behavior in the rat, dog, mouse, and rabbit were compared to enable selection of suitable species for further study.

Original languageEnglish
Pages (from-to)266-271
Number of pages6
JournalJournal of Planar Chromatography - Modern TLC
Volume14
Issue number4
DOIs
Publication statusPublished - Jan 1 2001

Keywords

  • 2,3-benzodiazepine
  • AMPA antagonist
  • Metabolic profiles
  • N-acetylation
  • Radio TLC

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Clinical Biochemistry

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