TABLE 1.
Comparison of inhibition parameters for human cytosolic aldehyde oxidase-catalyzed oxidation of two different substrates
NO indicates a Ki value that was not observed and was excluded from the best fit model. ND indicates the value was not determined, because the mode of inhibition was not mixed.
| Inhibitor | Phthalazinea | DACA | ||||
|---|---|---|---|---|---|---|
| Kis | Kii | Kii/Kis | Kis | Kii | Kii/Kis | |
| µM | µM | |||||
| β-Estradiol | 0.9 ± 0 | 0.13 ± 0 | 0.14 | 0.87 ± 0.5 | 4.4 ± 0.4 | 5.1 |
| Menadione | 0.75 ± 0.2 | 0.12 ± 0 | 0.16 | 0.47 ± 0.0 | 1.5 ± 0.5 | 3.2 |
| Ethinyl estradiol | 1.1 ± 0.3 | 0.23 ± 0.01 | 0.21 | 0.43 ± 0.2 | 3.6 ± 0.4 | 8.5 |
| Domperidone | 5.3 ± 3 | 14 ± 3 | 2.1 | 1.2 ± 0.2 | NO | ND |
| Chlorpromazine | 0.62 ± 0.2 | 3.3 ± 0.5 | 5.3 | 0.62 ± 0.07 | NO | ND |
| Clozapine | 3.9 ± 0.4 | 60 ± 2 | 15 | 5.1 ± 0.9 | NO | ND |
| Raloxifene | NO | 0.00087 ± 0.00005b | ND | 0.0023 ± 0.0006 | NO | ND |
a
All values for phthalazine oxidase inhibition with exception of raloxifene were previously reported in Barr and Jones (2011).
b
Data reported from Obach (2004).