BIOTRANSFORMATION OF DERAMCICLANE IN PRIMARY HEPATOCYTES OF RAT, MOUSE, RABBIT, DOG, AND HUMAN

@article{Monostory2005BIOTRANSFORMATIONOD,
  title={BIOTRANSFORMATION OF DERAMCICLANE IN PRIMARY HEPATOCYTES OF RAT, MOUSE, RABBIT, DOG, AND HUMAN},
  author={K. Monostory and Krisztina Kőhalmy and K. Ludányi and G. Czira and S. Holly and L. Vereczkey and I. Ürmös and I. Klebovich and L. K{\'o}bori},
  journal={Drug Metabolism and Disposition},
  year={2005},
  volume={33},
  pages={1708 - 1716}
}
The metabolic fate of deramciclane [(1R,2S,4R)-(–)-2-phenyl-2-(2′-dimethylamino-ethoxy)-1,7,7-trimethyl-bicyclo[2.2.1]heptane], a new anxiolytic drug candidate, has been determined in rat, mouse, rabbit, dog, and human hepatocytes. Rat and rabbit cells were the most active, whereas the rate of metabolism was quite slow in human hepatocytes. During biotransformation, deramciclane underwent side chain modification and oxidation at several positions of the molecule. The side chain modification led… Expand
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