A New Quaternary Ammonium Cysteine Analogue as a Trapping Reagent for Reactive Metabolites Screening

ISSN: 1874-0758 (Online)
ISSN: 1872-3128 (Print)


Volume 8, 2 Issues, 2014


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Drug Metabolism Letters

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Editor-in-Chief:
Chandra Prakash
Department of Drug Metabolism and Pharmacokinetics
Biogen Idec
Cambridge, MA
USA


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A New Quaternary Ammonium Cysteine Analogue as a Trapping Reagent for Reactive Metabolites Screening

Author(s): Natalia Penner, Xiaojing Liu and Chandra Prakash

Affiliation: Drug Metabolism and Pharmacokinetics, Biogen Idec, 14 Cambridge Center, Cambridge, MA 02142, USA

Abstract

The novel cysteine-cholamine (Cys-chol) trapping reagent was synthesized by coupling N-(tert-butoxycarbonyl)- S-trityl-L-cysteine with cholamine in the presence of HBTU (O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate), and then deprotecting by trifluoroacetic acid. Cys-chol reagent enhanced the sensitivity of reactive metabolite screening 4 to 20 times without introducing additional sample preparation or derivatization steps. Retention of Cys-chol conjugates on reversed-phase column is higher than for respective GSH conjugates which helps in reduction of background interference. The use of Cys-chol trapping reagent can potentially improve sensitivity and specificity of routine reactive metabolite screening assay in drug discovery


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Article Details

Volume: 8
First Page: 1
Last Page: 1
Page Count: 1
DOI: 10.2174/1872312808666140606100739
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