Table 2.
Probe drugs used to characterize the activities of Phase I and Phase II drug-metabolizing enzymes.
| CYP1A1/2 | CYP1A2 | CYP2B6 | CYP2C9 | CYP2C19 | CYP2D6 | CYP2D6 | CYP3A4 | UGT1A4 | UGT2B7 | |
|---|---|---|---|---|---|---|---|---|---|---|
| Parent drug | Caffeine | Luciferin-ME | S-mephenytoin | Diclofenac | S-mephenytoin | Dextromethorphan | Bufuralol | Midazolam | Lamotrigine | Morphine |
| Concentration (μM) | 75 | 100 | 60 | 100 | 60 | 80 | 20 | 9.2 | 40 | 10.5 |
| Metabolites (analyte) | Paraxanthine | Luciferin | S-nirvanol | 4-Hydroxy diclofenac | 4-Hydroxy mephenytoin | Dextrorphan | 1-Hydroxy bufuralol | 1-Hydroxy midazolam | Lamotrigine-N-glucuronide | Morphine-6-glucuronide |
| Internal Standard | 7-(β-Hydroxyethyl) theophylline | n.a. | Phenytoin | Indomethacin | Phenytoin | Levallophan | 1-Hydroxy midazolam | Prazepam | 1-Hydroxy midazolam | [2H3]morphine-3-glucuronide |
| Mobile phase %B (min) | 5(0)→95 (5) | n.a. | 30 (0)→95 (5) | 30 (0)→90 (6) | 25 (0)→85 (7) | 10 (0)→90 (7) | 25 (0)→85 (5) | 30 (0)→90 (6) | 15 (0)→90 (7) | 5 (0)→90 (5) |
| Analyte MRM | 181.1/124.1 | n.a. | 205.1/134.2 | 311.9/230.1 | 235.2/150.1 | 258.4/157.0 | 278.4/186.3 | 341.9/324.0 | 432.2/256.0 | 462.3/286.3 |
| Internal Standard MRM | 225.4/181.2 | n.a. | 253.2/182.2 | 357.9/139.1 | 253.2/182.2 | 284.3/157.2 | 341.9/324.0 | 325.0/271.1 | 341.9/324.0 | 465.3/289.3 |