TABLE 1

Initial rate conditions and incubation conditions used to measure kinetic parameters for MNTX reduction to M4 and M5 in liver cytosol of mice, rats, monkeys, and humans, and for naltrexone reduction to 6β-naltrexol in human liver cytosol

SubstrateSpeciesLinear RangeConditions for Kinetic Study
Incubation TimeProtein ConcentrationIncubation TimeProtein ConcentrationMNTX Concentration
M4M5M4M5
minminmg/mlmg/mlminmg/mlμM
MNTXMouseN.A.0–1200–6.00–6.01204.05–2000
RatN.A.0–120N.A.0–6.01204.05–5000
Monkey0–600–600–6.00–6.0604.05–2000
Human0–1200–1200–4.00–4.01201.00.5–5000
NaltrexoneHuman0–1200–0.5300.55–1000
  • N.A., not applicable.