Table 1

Assays of individual P450-catalyzed metabolism of substrates used for inhibition kinetics

SubstrateConc. rangeP450Product FormedInternal StandardAssayReference
μM
Estrone6.25–400CYP1A22-OH-EstroneBA t-5,6-diolHPLC Shou et al., 1997
Phenacetin3.9–250CYP1A2AcetaminophenTemazepamLC-MSSee text
Ethoxyresorufin0.05–50CYP1A2ResorufinExternal standardFluorescenceSee text
Diazepam1–500CYP2B6NordiazepamBA t-5,6-DHPLC Yang et al., 1998
Paclitaxel1.6–200CYP2C86α-OH-PaclitaxelBacctinHPLC Rahman et al., 1994
Flurbiprofen15.6–1000CYP2C94′-OH-FlurbiprofenBA t-5,6-DHPLC Tracy et al., 1995
Celecoxib0.5–30CYP2C9HydroxycelecoxibDiclofenacHPLC Tang et al., 2000
CYP2C9*2
CYP2C9*3
(S)-Mephenytoin1.56–150CYP2C194′-OH-MNirvanolHPLC Goldstein et al., 1994
Dextromethorphan3.0–2000CYP2D6DextrorphanBA t-5,6-diolHPLCSee text
Chlorzoxazone2–1000CYP2E16-OH-CBA t-5,6-diolHPLC Peter et al., 1990
Testosterone6.26–1250CYP3A46β-OH-T6β-OH-ProgesteroneHPLC Hanioka et al., 1990
Progesterone2.5–500CYP3A46β-OH-PEstradiolHPLCSee text
Benzyloxyresorufin2.5–50CYP3A4ResorufinExternal standardFluorescenceSee text
  • 6-OH-C, 6-OH-chlorzoxazone; 6β-OH-T, 6β-OH-testosterone; 6β-OH-P, 6β-OH-progesterone; BA t-5,6-D, BAt-5,6-diol; LC-MS, liquid chromatography-mass spectrometry.