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.

InhibitorPhthalazineaDACA
KisKiiKii/KisKisKiiKii/Kis
µMµM
β-Estradiol0.9 ± 00.13 ± 00.140.87 ± 0.54.4 ± 0.45.1
Menadione0.75 ± 0.20.12 ± 00.160.47 ± 0.01.5 ± 0.53.2
Ethinyl estradiol1.1 ± 0.30.23 ± 0.010.210.43 ± 0.23.6 ± 0.48.5
Domperidone5.3 ± 314 ± 32.11.2 ± 0.2NOND
Chlorpromazine0.62 ± 0.23.3 ± 0.55.30.62 ± 0.07NOND
Clozapine3.9 ± 0.460 ± 2155.1 ± 0.9NOND
RaloxifeneNO0.00087 ± 0.00005bND0.0023 ± 0.0006NOND
  • 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).