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. 2014 Oct 20;57(22):9598–9611. doi: 10.1021/jm501284e

Table 2. CYP450 Inhibition Assay Conditions.

CYP450 isoform substrate [S] (μM) [HLM] (mg/mL) incubation time (min) metabolite (mass transition, amua) internal standard (mass transition, amua)
CYP1A2 tacrine 1 0.2 10 1-hydroxytacrine (215 → 182) bucetin (224 → 136)
CYP2B6 bupropion 80 0.2 20 hydroxybupropion (256 → 139) hydroxybupropion-d6 (262 → 244)
CYP2C8 amodiaquine 1.5 0.02 5 desethylamodiaquine (330 → 285) desethylamodiaquine-d3 (333 → 285)
CYP2C9 diclofenac 5 0.05 5 4′-hydroxydiclofenac (312 → 268) 4′-hydroxydiclofenac-13C6 (316 → 272)
CYP2C19 (S)-mephenytoin 40 0.3 10 4′-hydroxy-(S)-mephenytoin (235 → 150) 4′-hydroxy-(S)-mephenytoin-d3 (238 → 150)
CYP2D6 dextromethorphan 5 0.1 5 dextrorphan (258 → 157) dextrorphan-d3 (261 → 157)
CYP3A4 midazolam 3 0.02 5 1′-hydroxymidazolam (342 → 203) 1′-hydroxymidazolam-13C3 (347 → 208)
CYP3A4 testosterone 50 0.05 10 6β-hydroxytestosterone (305 → 269) 6β-hydroxytestosterone-d7 (312 → 276)
a

Atomic mass units.