Table 2. Kinetic Parameters for the Reversible and Irreversible Inhibition of the hMAOs by the Selected 4-Styrylpiperidine Inhibitors.
| reversible inhibition | irreversible inhibition |
||||
|---|---|---|---|---|---|
| MAO | inhibitor | Ki (μM) | KI (μM) | kinact (min–1) | kinact/KI (min–1 μM–1) |
| hMAO-A | 69 | 0.23 ± 0.02 | 1.01 ± 0.76 | 1.25 ± 0.25 | 1.24 |
| clorgylinea | 0.040 ± 0.004b | 0.22 ± 0.08b | 0.12 ± 0.05b | 0.55b | |
| hMAO-B | 1 | 1.92 ± 0.32 | 1.38 ± 0.29 | 0.66 ± 0.04 | 0.48 |
| 84 | 1.25 ± 0.23 | 17.25 ± 4.38 | 2.03 ± 0.38 | 0.12 | |
| 97 | 1.36 ± 0.31 | 6.55 ± 1.62 | 1.04 ± 0.12 | 0.16 | |
| l-deprenyla | 0.97 ± 0.11 | 5.68 ± 0.78 | 2.56 ± 0.24 | 0.45 | |
Kinetic parameters were compared to clorgyline and l-deprenyl in the cases of hMAO-A and hMAO-B selective inhibitors, respectively.
Data from Esteban et al. (2014).25