• Corpus ID: 11742677

A sensitive method for determination of cytochrome P4502D6 activity in vitro using bupranolol as substrate.

  title={A sensitive method for determination of cytochrome P4502D6 activity in vitro using bupranolol as substrate.},
  author={G Appanna and B. K. Tang and Rudi Mller and Werner Kalow},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  volume={24 3},
  • G. Appanna, B. Tang, +1 author W. Kalow
  • Published 1 March 1996
  • Chemistry, Medicine
  • Drug metabolism and disposition: the biological fate of chemicals
Previous studies have shown that bupranolol, a beta-adrenoceptor blocker, is a substrate of cytochrome P4502D6 (CYP2D6). A sensitive in vitro assay was developed to quantify the formation of hydroxybupranolol using HPLC. A TLC method, using radiolabeled bupranolol, was also developed to test the reproducibility of the two methods. Both of them gave virtually identical results; however, the HPLC method was sensitive to 20 pmol and the TLC with radiolabeled substrate to <1 pmol of… 
Involvement of human cytochrome P450 3A4 in reduced haloperidol oxidation
  • S. Kudo, M. Odomi
  • Chemistry, Medicine
    European Journal of Clinical Pharmacology
  • 1998
It was concluded that CYP3A4, not CYP2D6, is the principal isoform of cytochrome P450 involved in the metabolic conversion of reduced haloperidol to haloperidsol and that haloperIDol has both stimulatory and inhibitory effects on CYP 2D6 activity.
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Molecular cloning, expression, and characterization of CYP2D17 from cynomolgus monkey liver.
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Comparative molecular field analysis and QSAR on substrates binding to cytochrome p450 2D6.
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Metabolism Site Prediction Based on Xenobiotic Structural Formulas and PASS Prediction Algorithm
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