Table 2.
The Ki values for the inhibition of purified recombinant human MAO by isatin (1) and (E)-styrylisatin analogues (4–5)
MAO-A wild- typea (μM) | MAO-B wild-typeb (μM) | MAO-B selectivityc | MAO-B I199A mutanta (μM) | ||
---|---|---|---|---|---|
1 | Isatin | 15d | 3d | 5.0 | 12 ± 2 |
4a | (E)-5-Styrylisatin | 0.78 ± 0.10 | 0.31 ± 0.06 | 2.5 | 1.1 ± 0.2 |
4b | (E)-5-(3-Chlorostyryl)isatin | 5.6 ± 0.3 | 1.4 ± 0.4 | 4.0 | 12.5 ± 0.7 |
4c | (E)-5-(3-Fluorostyryl)isatin | 2.2 ± 0.2 | 0.60 ± 0.07 | 3.6 | 4.5 ± 0.2 |
5 | (E)-6-Styrylisatin | 22 ± 2 | 0.56 ± 0.02 | 39 | 2.2 ± 0.4 |
The Ki values were determined spectrophotometrically using p-CF3-benzylamine as substrate.
The Ki values were determined spectrophotometrically using benzylamine as substrate.
Selectivity for the B isoform is given as the ratio of Ki(MAO-A) to Ki(MAO-B) of the wild-type enzymes.
Values obtained from reference.9