Table 1.
Spectral changes in CYP11A1 elicited by inhibitors and activatorsa
Drug | λmax in the absolute spectrum, nm | λmin and λmax in the difference spectrum, nm | ΔAmax in the difference spectrumb | Spectral Kdc |
---|---|---|---|---|
None | 417 | NAd | NA | NA |
Inhibitors | ||||
Ketoconazole | 422 | 412, 432 | 0.1 ± 0.01 | 1.5 ± 0.2 |
Posaconazole | 422 | 411, 429 | 0.02 ± 0.001 | 1.0 ± 0.2 |
Carbenoxolone | 417e | WSRf | <0.004 | NDg |
Selegeline | 417e | NOh | NA | ND |
Activators | ||||
Pemirolast | 417e | NO | NA | ND |
Clobenpropit | 420 | 412, 433 | 0.03 ± 0.008 | 18.0 ± 2.0 |
Dexmedetomidine | 421 | 413, 434 | 0.08 ± 0.01 | 7.0 ± 1.0 |
Desogestrel | 417e | WSR | <0.002 | ND |
Tizanidine | 417e | NO | NA | ND |
The assay buffer was 40 mM KPi, pH, 7.2, containing 1 mM EDTA.
Normalized per nmol of CYP11A1, except cases with weak or no spectral response.
The results are the mean ± S.D of three independent titrations.
NA, non applicable.
The absorbance at λmax was decreased by 2–8%.
WSR, weak spectral response.
ND, not determined.
NO, not observed.