Run | Compound | IC50 | Ratio (IC50EAAT3/IC50EAAT2) | |
---|---|---|---|---|
EAAT2 | EAAT3 | |||
nM | ||||
1 | l-TBOA | 1300 ± 120 | 1300 ± 120 | 1.0 |
2 | A-TBOA | 2100 ± 100 | 7900 ± 760 | 3.8 |
3 | PrA-TBOA | 1200 ± 100 | 4100 ± 390 | 3.4 |
4 | PivA-TBOA | 980 ± 130 | 3500 ± 380 | 3.6 |
5 | cHexcA-TBOA | 244 ± 12 | 288 ± 8.0 | 1.2 |
6 | PhAcA-TBOA | 143 ± 7.9 | 529 ± 32 | 3.7 |
7 | BzA-TBOA | 55 ± 5.0 | 729 ± 98 | 13 |
8 | o-MeO-BzA-TBOA | 145 ± 2.2 | 1000 ± 42 | 7.0 |
9 | m-MeO-BzA-TBOA | 37 ± 2.5 | 356 ± 12 | 9.6 |
10 | PMB-TBOA | 12 ± 0.5 | 266 ± 20 | 22 |
11 | 3,4-MeO-BzA-TBOA | 49 ± 3.8 | 917 ± 30 | 19 |
12 | CNB-TBOA | 36 ± 2.9 | 1400 ± 99 | 39 |
13 | t-Bu-BzA-TBOA | 25 ± 0.5 | 182 ± 11 | 7.3 |
14 | F-BzA-TBOA | 22 ± 2.7 | 473 ± 13 | 22 |
15 | Ph-BzA-TBOA | 21 ± 2.2 | 34 ± 19 | 1.6 |
16 | NO2-BzA-TBOA | 14 ± 1.4 | 278 ± 32 | 20 |
17 | CF3O-BzA-TBOA | 7.0 ± 0.5 | 128 ± 12 | 18 |
18 | TFB-TBOA | 1.9 ± 0.1 | 28 ± 1.6 | 15 |
19 | DHKA | 56 ± 9.7 μM | 1000 ± 100 μM | 18 |
PrA-TBOA, (2S,3S)-3-[3-(propionylamino)benzyloxy]aspartate; cHexcA-TBOA, (2S,3S)-3-[3-(cyclohexylcarbonylamino)benzyloxy]aspartate; PhAcA-TBOA, (2S,3S)-3-{3-[(phenylacetyl)amino]benzyloxy}aspartate; BzA-TBOA, (2S,3S)-3-[3-(benzoylamino)benzyloxy]aspartate; o-MeO-BzA-TBOA, (2S,3S)-3-[3-(2-methoxybenzoylamino)-benzyloxy]aspartate; m-MeO-BzA-TBOA, (2S,3S)-3-[3-(3-methoxybenzoylamino)benzyloxy]aspartate; p-MeO-BzA-TBOA(PMB-TBOA), (2S,3S)-3-[3-(4-methoxybenzoylamino)benzyloxy]aspartate; 3,4-MeO-BzA-TBOA, (2S,3S)-3-[3-(3,4-methoxybenzoylamino)benzyloxy]aspartate; CNB-TBOA, (2S,3S)-3-[3-(4-cyanobenzoylamino)benzyloxy]aspartate; t-Bu-BzA-TBOA, (2S,3S)-3-[3-(4-tert-butylbenzoylamino)benzyloxy]aspartate; F-BzA-TBOA, (2S,3S)-3-[3-(4-fluorobenzoylamino)benzyloxy]aspartate; Ph-BzA-TBOA, (2S,3S)-3-[3-(4-phenylbenzoylamino)benzyloxy]aspartate; NO2-BzA-TBOA, (2S,3S)-3-[3-(4-nitrobenzoylamino)benzyloxy]aspartate; CF3O-BzA-TBOA, (2S,3S)-3-{3-[4-(trifluoromethoxy)benzoylamino]benzyloxy}aspartate; TFB-TBOA, (2S,3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate.