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. 2020 Jan 9;63(3):1361–1387. doi: 10.1021/acs.jmedchem.9b01886

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
a

Kinetic parameters were compared to clorgyline and l-deprenyl in the cases of hMAO-A and hMAO-B selective inhibitors, respectively.

b

Data from Esteban et al. (2014).25