Metabolism of 3-chloro-4-fluoroaniline in rat using [14C]-radiolabelling, 19F-NMR spectroscopy, HPLC-MS/MS, HPLC-ICPMS and HPLC-NMR

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
C J DuckettJ K Nicholson

Abstract

The metabolic fate of 3-chloro-4-fluoroaniline was investigated in rat following intraperitoneal (i.p.) administration at 5 and 50 mg kg(-1) using a combination of HPLC-MS, HPLC-MS/MS, (19)F-NMR spectroscopy, HPLC-NMR spectroscopy and high-pressure liquid chromatography-inductively coupled plasma mass spectrometry (HPLC-ICPMS) with (35)Cl and (34)S detection. The metabolism of 3-chloro-4-fluoroaniline at both doses was rapid and extensive, to a large number of metabolites, with little unchanged compound excreted via the urine. Dosing at 5 mg kg(-1) with [(14)C]-labelled compound enabled the comparison of standard radioassay analysis methods with (19)F-NMR spectroscopy. (19)F-NMR resonances were only readily detectable in the 0-12 h post-dose samples. Dosing at 50 mg kg(-1) allowed the facile and specific detection and quantification of metabolites by (19)F-NMR spectroscopy. Metabolite profiling was also possible at this dose level using HPLC-ICPMS with (35)Cl-specific detection. The principal metabolites of 3-chloro-4-fluoroaniline were identified as 2-amino-4-chloro-5-fluorophenyl sulfate and 2-acetamido-4-chloro-5-fluorophenyl glucuronide. N-acetylation and hydroxylation followed by O-sulfation were the major metabolic transf...Continue Reading

References

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Citations

Jun 1, 2009·Bioanalysis·Götz Schlotterbeck, Simona M Ceccarelli
Jul 1, 2009·Bioanalysis·Pat WrightBarclay Shilliday
Aug 30, 2008·Expert Opinion on Drug Metabolism & Toxicology·Bente GammelgaardCharlotte Møller
Oct 27, 2011·Progress in Nuclear Magnetic Resonance Spectroscopy·James S McKenzieAdrian J Charlton
Dec 1, 2006·Journal of Mass Spectrometry : JMS
Mar 26, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Pat Wright
Feb 7, 2013·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Toby J AthersuchJohn C Lindon
Apr 4, 2015·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Catherine DuckettIan D Wilson
Dec 21, 2006·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·T J AthersuchI D Wilson
Oct 19, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Abdul MutlibJoann Scatina
Jul 13, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·B KammererS Laufer
May 7, 2010·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·T J AthersuchIan D Wilson
Sep 27, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·E MonteagudoV Summa
Sep 22, 2017·Chemical Research in Toxicology·Gabriele Sabbioni

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