Table 1.
Effects of selective CYP inhibitors on 3HCIM binding in brain homogenates. Compounds thought to be isoform-selective CYP inhibitors were screened for their activities on 3HCIM. For each inhibitor, the CYP targeted and the literature Ki value is given.
| CYP Inhibitor | CYP Isoform Inhibited |
Reported Ki (μM) |
Reference | Ki on 3HCIM Binding (μM) a |
|---|---|---|---|---|
| Thio-TEPA | 2B6 | 2.8 | (Turpeinen, et al., 2004) | >100 |
| Tranylcypromine | 2C19 | 8 | (Inaba, et al., 1985) | 10.8 |
| Ticlopidine | 2C19 | 0.18 | (Ko, et al., 2000) | >100 |
| DL-Aminogluthimide | 19A1 | 0.6 | (Foster, et al., 1985) | >100 |
| Fluvoxamine | 1A2 | 0.18 | (Brosen, et al., 1993) | >100 |
| Sulfaphenazole | 2C9 | 0.12 | (Miners, et al., 1988) | >100 |
| Ketoconazole | 3A4 | 0.02 | (Back and Tjia, 1991) | 6.4 |
| Diethyldithiocarbamate | 2E1 | 7 | (Baranova, et al., 2005) | >100 |
| Quercetin | 2C8 | ∼1-3 | (Dierks, et al., 2001) | >100 |
a
Ki values calculated from IC50 values in Figure 4.