Thin-layer chromatographic characterization of metabolites formed from an AMPA antagonist drug candidate
Katalin Migléczi, István Hazai, Katalin Jemnitz, Márta Pátfalusi · Journal of Planar Chromatography – Modern TLC · 2001
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-11 H -imidazo[1,2 c ] [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.