6-Hydroxybuspirone Is a Major Active Metabolite of Buspirone: Assessment of Pharmacokinetics and 5-Hydroxytryptamine1A Receptor Occupancy in Rats

@article{Wong20076HydroxybuspironeIA,
  title={6-Hydroxybuspirone Is a Major Active Metabolite of Buspirone: Assessment of Pharmacokinetics and 5-Hydroxytryptamine1A Receptor Occupancy in Rats},
  author={Harvey Wong and Randy C. Dockens and Lori Pajor and Suresh N. Yeola and James E Grace and Arlene D. Stark and Rebecca A. Taub and Frank D. Yocca and Robert C. Zaczek and Yu-wen Li},
  journal={Drug Metabolism and Disposition},
  year={2007},
  volume={35},
  pages={1387 - 1392}
}
The pharmacokinetics and in vivo potency of 6-hydroxybuspirone (6-OH-buspirone), a major metabolite of buspirone, were investigated. The plasma clearance (47.3 ± 3.5 ml/min/kg), volume of distribution (2.6 ± 0.3 l/kg), and half-life (1.2 ± 0.2 h) of 6-OH-buspirone in rats were similar to those for buspirone. Bioavailability was higher for 6-OH-buspirone (19%) compared with that for buspirone (1.4%). After intravenous infusions to steady-state levels in plasma, 6-OH-buspirone and buspirone… Expand
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