Table 3.
Inhibitory activities towards hMAO-A and hMAO-B of EMAC II (i–m) derivatives.
Compound | Structure | MAO-A (IC50) | MAO-B (IC50) | Ratioe |
---|---|---|---|---|
EMAC II i | ![]() |
b | 104.04 ± 3.69 nM | >961d |
EMAC II j | ![]() |
b | 41.05 ± 1.52 nM | >2436d |
EMAC II k | ![]() |
b | 320.22 ± 13.61 nM | >312d |
EMAC II l | ![]() |
b | 11.97 ± 0.37 nM | >8354d |
EMAC II m | ![]() |
b | 449.57 ± 18.02 nM | >222d |
Clorgiline | 4.46 ± 0.32 nMc | 61.35 ± 1.13 μM | 0.000073 | |
l-Deprenyl | 67.25 ± 1.02 μMc | 19.60 ± 0.86 nM | 3431.12 | |
Iproniazide | 6.56 ± 0.76 μM | 7.54 ± 0.36 μM | 0.87 | |
Moclobemide | 361.38 ± 19.37 μM | a | <0.36e |
Inactive at 1 mM (highest concentration tested).
Inactive at 100 μM (highest concentration tested). At higher concentration, the compounds precipitate.
Results are mean ± SEM from five experiments. Level of statistical significance: cP <0.01 versus the corresponding IC50 values obtained against MAO-B, as determined by ANOVA/Dunnett’s.
Values obtained under the assumption that the corresponding IC50 against MAO-A is the highest concentration tested (100 μM).
Selectivity ratios [IC50(MAO-A)]/[IC50(MAO-B)].