The in vitro hepatic metabolism of ABT-418, a cholinergic channel activator, in rats, dogs, cynomolgus monkeys, and humans.

@article{Rodrigues1994TheIV,
  title={The in vitro hepatic metabolism of ABT-418, a cholinergic channel activator, in rats, dogs, cynomolgus monkeys, and humans.},
  author={A. David Rodrigues and J. L. Ferrero and Michael Amann and Gary Rotert and S P Cepa and Bruce W. Surber and J M Machinist and N R Tich and James P. Sullivan and David S. Garvey},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={1994},
  volume={22 5},
  pages={788-98}
}
The metabolism of the cholinergic channel activator [3H]ABT-418 was studied in 9,000g supernatant (S-9) fractions and precision-cut tissue slices prepared from rat, dog, monkey, and human livers. In rat S-9 fractions and tissue slices, the lactam and trans N'-oxide were detected as major metabolites. The lactam was also the major metabolite in monkey and human S-9 fractions and tissue slices, although the rate of formation was greater in monkey (Vmax' of 428 vs. 103 pmol/min/mg S-9 protein… CONTINUE READING