Table 4.
Inhibitory activities towards hMAO-A and hMAO-B of EMAC II (i–m) single enantiomers.
Compound | MAO-A (IC50) | MAO-B (IC50) | Ratio |
---|---|---|---|
R-(−) EMAC II i | a | 15.27 ± 0.95 nM | 6549b |
S-(+) EMAC II i | a | a | |
R-(−) EMAC II j | a | 2.55 ± 0.11 nM | 39 216b |
S-(+) EMAC II j | a | 31.37 ± 1.67 μM | 3188b |
R-(−) EMAC II k | a | 299.86 ± 12.04 nM | 333.5b |
S-(+) EMAC II k | a | 33.82 ± 1.12 μM | 2956b |
R-(−) EMAC II l | a | 1.89 ± 0.16 nM | 52 910b |
S-(+) EMAC II l | a | 10.96 ± 0.83 μM | 9124 |
R-(−) EMAC II m | a | 126.16 ± 8.44 nM | 792.6b |
S-(+) EMAC II m | a | 291.82 ± 13.45 nM | 342.6 |
IC50 values are the mean ± SEM from five experiments.
Inactive at 100 μM (highest concentration tested).
bValues obtained under the assumption that the corresponding IC50 against MAO-B is the highest concentration tested (100 μM).