CYTOCHROME P450 3A-MEDIATED METABOLISM OF BUSPIRONE IN HUMAN LIVER MICROSOMES

@article{Zhu2005CYTOCHROMEP3,
  title={CYTOCHROME P450 3A-MEDIATED METABOLISM OF BUSPIRONE IN HUMAN LIVER MICROSOMES},
  author={Mingshe Zhu and Weiping Zhao and Humberto Jimenez and Donglu Zhang and Suresh N. Yeola and Renke Dai and Nimish N. Vachharajani and James G Mitroka},
  journal={Drug Metabolism and Disposition},
  year={2005},
  volume={33},
  pages={500 - 507}
}
This study was carried out to determine the metabolic pathways of buspirone and cytochrome P450 (P450) isoform(s) responsible for buspirone metabolism in human liver microsomes (HLMs). Buspirone mainly underwent N-dealkylation to 1-pyrimidinylpiperazine (1-PP), N-oxidation on the piperazine ring to buspirone N-oxide (Bu N-oxide), and hydroxylation to 3′-hydroxybuspirone (3′-OH-Bu), 5-hydroxybuspirone (5-OH-Bu), and 6′-hydroxybuspirone (6′-OH-Bu) in HLMs. The apparent Km values for buspirone… Expand
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