Synthesis of ¹³C-Lidocaine as a Probe of Breath Test for the Evaluation of Cytochrome P450 Activity

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  • Mitome Hidemichi
    College of Pharmaceutical Sciences, Matsuyama University
  • Sugiyama Erika
    Division of Pharmacokinetics/Pharmacodynamics, Department of Pharmacotherapeutic Sciences, School of Pharmacy, Showa University
  • Sato Hitoshi
    Division of Pharmacokinetics/Pharmacodynamics, Department of Pharmacotherapeutic Sciences, School of Pharmacy, Showa University
  • Akira Kazuki
    College of Pharmaceutical Sciences, Matsuyama University

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  • Synthesis of <sup>13</sup>C-Lidocaine as a Probe of Breath Test for the Evaluation of Cytochrome P450 Activity

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13C-Labeled lidocaine, 2-di[1-13C]ethylamino-N-(2,6-dimethylphenyl)acetamide (1), was synthesized from [1-13C]acetic acid in six steps, as a probe for a breath test to evaluate in vivo cytochrome P450 activity. The measurement of 13CO2 in breath was successfully performed following oral administration of 13C-lidocaine 1 to mice.

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