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The Analytical Scientist / App Notes / 2014 / Fast Mimicking of Phase 1 and 2 Metabolism of Acetaminophen using the ROXY™ EC System

Fast Mimicking of Phase 1 and 2 Metabolism of Acetaminophen using the ROXY™ EC System

11/06/2014

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Summary
  • Acetaminophen, Paracetamol, Tylenol, Panadol, APAP
  • Simulating CYP450 oxidative metabolism in <10 min.
  • Controlled oxidation (phase 1) and detoxification (phase 2) reactions
  • Fast and easy in use, complements HLM, RLM
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Introduction

The knowledge of the metabolic pathways and the biotransformation of new drugs are crucial for elucidation of degradation routes of the new active compounds, especially in the area of possible toxicity. In vitro studies are based on incubating drug candidates with, e.g., liver cells (in microsomes activity of cytochrome P450 is high) and isolating and detecting the metabolic products. With the introduction of the ROXY™ EC system oxidative metabolism, which usually occurs in the liver cells by Cytochrome P450 oxidation, can be simulated successfully within seconds and detected by electrospray mass spectrometry (ESI-MS) [1-5]. Combining the ROXY EC System with MS creates a powerful platform for oxidative metabolite investigations and helps to overcome many of the laborious tasks by isolating the metabolites form in vivo studies, e.g., urine, plasma, etc., or in vitro studies, e.g., rat liver microsomes (RLM) or human liver micorosomes (HLM).

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