Inhibition of MAO-A and MAO-B by the 18 compounds of ISB seriesa.
| Compound | Residual activity at 10 μM (%) | IC50 (μM) | SIb | ||
|---|---|---|---|---|---|
| MAO-A | MAO-B | MAO-A | MAO-B | ||
| ISB1 | 38.78 ± 0.25 | −8.77 ± 0.14 | 6.824 ± 0.049 | 0.124 ± 0.007 | 55.03 |
| ISB2 | 87.76 ± 1.11 | 64.91 ± 1.24 | >40 | 14.182 ± 0.250 | >2.82 |
| ISB3 | 74.49 ± 0.95 | 59.65 ± 1.11 | >40 | 13.943 ± 0.204 | >2.87 |
| ISB4 | 84.69 ± 1.55 | 54.39 ± 2.01 | >40 | 9.764 ± 1.349 | >4.10 |
| ISB5 | 85.71 ± 2.04 | 66.67 ± 1.35 | >40 | 17.622 ± 0.202 | >2.27 |
| ISB6 | 89.80 ± 1.12 | 40.35 ± 0.99 | >40 | 6.563 ± 0.206 | >6.09 |
| ISFB1 | 4.17 ± 0.32 | −3.03 ± 0.24 | 0.678 ± 0.006 | 0.135 ± 0.002 | 5.02 |
| ISFB2 | 88.54 ± 1.38 | 57.58 ± 1.10 | >40 | 16.043 ± 0.308 | >2.49 |
| ISFB3 | 53.13 ± 0.44 | 24.50 ± 1.03 | 10.937 ± 0.220 | 1.189 ± 0.362 | 9.20 |
| ISFB4 | 84.38 ± 1.24 | 63.64 ± 0.15 | >40 | 20.768 ± 0.027 | >1.93 |
| ISFB5 | 87.50 ± 1.88 | 50.00 ± 0.38 | >40 | 8.986 ± 0.079 | >4.45 |
| ISFB6 | 84.38 ± 1.52 | 30.30 ± 0.77 | >40 | 4.100 ± 0.311 | >9.76 |
| ISBB1 | 4.84 ± 1.61 | 1.99 ± 0.86 | 1.570 ± 0.048 | 0.540 ± 0.029 | 2.91 |
| ISBB2 | 81.52 ± 1.64 | 46.88 ± 0.88 | >40 | 8.127 ± 0.383 | >4.92 |
| ISBB3 | 35.87 ± 1.02 | 29.69 ± 0.54 | 0.731 ± 0.028 | 0.607 ± 0.011 | 1.20 |
| ISBB4 | 73.91 ± 0.04 | 40.63 ± 0.63 | >40 | 6.058 ± 0.318 | >6.60 |
| ISBB5 | 58.70 ± 0.29 | 48.44 ± 0.44 | 11.054 ± 0.060 | 12.061 ± 3.567 | 0.92 |
| ISBB6 | 65.22 ± 0.87 | 39.06 ± 0.21 | 14.422 ± 0.670 | 15.157 ± 0.419 | 0.95 |
| Toloxatone | 1.080 ± 0.025 | — | |||
| Lazabemide | — | 0.110 ± 0.016 | |||
| Clorgyline | 0.007 ± 0.0007 | — | |||
| Pargyline | — | 0.140 ± 0.006 | |||
a
Results are the means ± standard errors of duplicate or triplicate experiments.
b
Selectivity index (SI) values are expressed for MAO-B compared to MAO-A.