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Rapid CommunicationShort Communication

Investigation of Figopitant and Its Metabolites in Rat Tissue by Combining Whole-Body Autoradiography with Liquid Extraction Surface Analysis Mass Spectrometry

Simone Schadt, Susanne Kallbach, Reinaldo Almeida and Jan Sandel
Drug Metabolism and Disposition March 2012, 40 (3) 419-425; DOI: https://doi.org/10.1124/dmd.111.043562
Simone Schadt
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Susanne Kallbach
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Reinaldo Almeida
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Jan Sandel
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Abstract

This article describes the combination of whole-body autoradiography with liquid extraction surface analysis (LESA) and mass spectrometry (MS) to study the distribution of the tachykinin neurokinin-1 antagonist figopitant and its metabolites in tissue sections of rats after intravenous administration of 5.0 mg/kg figopitant. An overview of autoradiography results is presented together with mass spectrometry identification and semiquantification of parent drug and its metabolites based on LESA-MS. The quality and accuracy of data generated by LESA-MS were assessed in comparison with classic tissue extraction, sample cleanup, and high-performance liquid chromatography analysis. The parent drug and the N-dealkylated metabolite M474(1) (BIIF 1148) in varying ratios were the predominant compounds in all tissues investigated. In addition, several metabolites formed by oxygenation, dealkylation, and a combination of oxygenation and dealkylation were identified. In summary, the LESA-MS technique was shown to be a powerful tool for identification and semiquantification of figopitant and its metabolites in different tissues and was complementary to quantitative whole-body autoradiography for studying the distribution.

Footnotes

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

    http://dx.doi.org/10.1124/dmd.111.043562.

  • ABBREVIATIONS:

    QWBA
    quantitative whole-body autoradiography
    MS/MS
    tandem mass spectrometry
    MS
    mass spectrometry
    LESA
    liquid extraction surface analysis
    SIM
    single ion monitoring
    NK1
    neurokinin-1
    HPLC
    high-performance liquid chromatography
    ACN
    acetonitrile
    FA
    formic acid
    LSC
    liquid scintillation counting
    CV
    coefficient of variation
    LC
    liquid chromatography
    NSI
    nano-electrospray ionization.

  • Received November 4, 2011.
  • Accepted December 19, 2011.
  • Copyright © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 40 (3)
Drug Metabolism and Disposition
Vol. 40, Issue 3
1 Mar 2012
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Rapid CommunicationShort Communication

DISTRIBUTION OF FIGOPITANT AND ITS METABOLITES IN RAT TISSUE

Simone Schadt, Susanne Kallbach, Reinaldo Almeida and Jan Sandel
Drug Metabolism and Disposition March 1, 2012, 40 (3) 419-425; DOI: https://doi.org/10.1124/dmd.111.043562

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Rapid CommunicationShort Communication

DISTRIBUTION OF FIGOPITANT AND ITS METABOLITES IN RAT TISSUE

Simone Schadt, Susanne Kallbach, Reinaldo Almeida and Jan Sandel
Drug Metabolism and Disposition March 1, 2012, 40 (3) 419-425; DOI: https://doi.org/10.1124/dmd.111.043562
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