TABLE 3.
Inhibition of GLT-1 variants by a range of uptake blockers
Values are means ± S.E.M. derived from at least three independent experiments. The rank order and actual IC50 values for this series of inhibitors do not differ among the cell lines tested (P < 0.01).
| irGLT-1 | MAST-KREK | MPK-DIETCI | V5-MPK-DIETCI | |
|---|---|---|---|---|
| WAY-213394 | 106.3 ± 28.4 nM | 87.8 ± 4.2 nM | 119.2 ± 26.4 nM | 152.7 ± 8.8 nM |
| WAY-213613 | 182.7 ± 32.9 nM | 152.0 ± 36.6 nM | 225.6 ± 34.5 nM | 220.6 ± 41.2 nM |
| WAY-212922 | 200.3 ± 42.0 nM | 177.3 ± 34.0 nM | 252.0 ± 19.0 nM | 355.6 ± 70.4 nM |
| TBOA | 1.9 ± 0.5 μM | 1.7 ± 0.2 μM | 2.2 ± 0.5 μM | 1.3 ± 0.1 μM |
| WAY-144855 | 2.4 ± 0.5 μM | 1.5 ± 0.2 μM | 3.1 ± 0.3 μM | 3.3 ± 0.6 μM |
| CCGIII | 6.3 ± 1.1 μM | 5.6 ± 2.6 μM | 9.7 ± 2.3 μM | 11.4 ± 1.4 μM |
| PDC | 11.1 ± 2.2 μM | 11.0 ± 1.6 μM | 10.4 ± 2.0 μM | 17.2 ± 5.4 μM |
| TβHA | 19.0 ± 5.3 μM | 12.8 ± 4.7 μM | 24.9 ± 4.9 μM | 22.8 ± 4.7 μM |
| DHK | 42.6 ± 20.7 μM | 39.1 ± 21.5 μM | 41.3 ± 9.1 μM | 28.2 ± 5.3 μM |
| KA | 92.4 ± 65.8 μM | 76.2 ± 37.5 μM | 51.2 ± 13.8 μM | 38.0 ± 5.1 μM |
| 3MG | 115.2 ± 17.5 μM | 92.1 ± 32.0 μM | 93.7 ± 16.1 μM | 108.5 ± 23.4 μM |
| L-SOS | 207.8 ± 21.7 μM | 232.7 ± 33.4 μM | 400.6 ± 58.1 μM | 452.1 ± 159.9 μM |
TBOA, dl-threo-β-benzyloxyaspartate; CCGIII, 2S,1′S,2′R-2-(carboxycyclopropyl)glycine; PDC, l-transpyrrolidine-2,4-dicarboxylic acid; TβHA, threo-β-hydroxyaspartate; DHK, dihydrokainate; KA, kainite; 3MG, (±)-threo-3-methylglutamate; L-SOS, l-serine-O-sulfate.