Performs custom synthesis of labelled compounds, and assessment of tests related to pharmacokinetics. ADME & Tox. Research Business of SEKISUI MEDICAL.

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Enzyme Induction Study

We prepare a microsome from the liver in rats following repeated administration of a non-labeled compound, and determine its drug metabolizing enzyme activities with validated systems.
If liver samples obtained from a toxicity study are provided, we also determine drug metabolizing enzyme activities.

Parameters measured

  1. Microsome total protein
  2. Amount of Cytocrome P450
  3. Amount of Cytocrome b5
  4. Determination of metabolizing enzyme activities
  • Aminopyrine N-demethylase activity (involvement of multiple species)
  • Aniline hydroxylase activity (CYP2E1)
  • 7-Ethoxycoumarin O-demethylase activity (CYP1A1)
  • UDP-glucuronosyl transferase activity (conjugation reaction)
  • p-Nitroanisole O-demethylase activity (CYP1A1)
  • NADPH Cytochrome c reductase activity
  • Amount of protein in liver cytosol
  • Glutathione S-transferase activity (conjugation reaction)
  • Lauric acid ω-hydroxylase activity (CYP4A1)
  • Testosterone hydroxylase activity
    2α-hydroxylase activity (CYP2C11)
    6α-hydroxylase activity (CYP3A2)
    16α-hydroxylase activity (CYP2C11)
    16α-hydroxylase activity (CYP2B1)
  • Benzo[a]pyrene hydroxylase activity (CYP1A1)
  • Chlorzoxazone 6-hydroxylase activity (CYP2E1)
  • 7-Ethoxyresorufin O-demethylase activity (CYP1A1, 1A2)
  • Bufuralol 1'-hydroxylase activity (CYP2D1, 2D2)
 
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