Involvement of CYP3A4 and CYP2D6 in the Metabolism of Haloperidol

  title={Involvement of CYP3A4 and CYP2D6 in the Metabolism of Haloperidol},
  author={Jian Fang and Glen B Baker and Peter H. Silverstone and Ronald Thomson Coutts},
  journal={Cellular and Molecular Neurobiology},
1. Human cytochrome P450 (CYP) isoenzymes expressed in a human cell line were used to elucidate their involvement in the metabolism of haloperidol (HAL). 2. It was found that CYP3A4 catalyzes the metabolism of HAL to HAL 1,2,3,6-tetrahydropyridine (HTP). HTP is further metabolized to HAL pyridinium (HP+) by both CYP3A4 and CYP2D6. 3. CYP3A4 and CYP2D6 are also responsible for the N-dealkylation of HAL. The N-dealkylation of reduced HAL (RH) was observed, which is catalyzed by CYP3A4. In… CONTINUE READING


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An HPLC system for the analysis of haloperidol and seven of its metabolites in microsomal preparations

  • J. Fang, J. W. Gorrod
  • J. Chromatogr
  • 1993
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