Inhibitors of GABA transporters
| Inhibitor | Ki | Application | Binding Site Model | |||
|---|---|---|---|---|---|---|
| GAT-1 | BGT-1a | GAT-2b | GAT-3c | |||
| μM | ||||||
| GAT-1 inhibitors | ||||||
| Tiagabined | 0.11 | >100 | >100 | >100 | Therapeutic drug | Skovstrup et al., 2010 |
| NNC-711d | 1.4 | 1500 | 1200 | >1600 | Pharmacological tool | |
| SKF89976Ae | 0.13 | 7210 | 550 | 1990 | Pharmacological tool | |
| CI-966e | 0.26 | 300 | 1280 | 333 | Pharmacological tool | |
| Nonselective inhibitors | ||||||
| Nipecotic acidd,f | 19 | 3000 | 530 | 94 | Pharmacological tool | |
| Guvacined,f | 15 | 2300 | 1000 | 120 | Pharmacological tool | |
| β-Alanined,f | 5000 | 660 | 42 | 36 | Pharmacological tool | |
| Betained,f | >10,000 | 590 | >3000 | >10,000 | Pharmacological tool | |
| (S)-SNAP-5114d | >500 | 250 | 130 | 50 | Pharmacological tool | |
| (R)-EF1502d | 8.9 | 180 | 170 | >250 | Pharmacological tool | |
| THPOd | 1300 | 2100 | 1500 | 2200 | Pharmacological tool | |
| Exo-THPOg | 1000 | 3000 | >3000 | >3000 | Pharmacological tool | |
| NNC 05-2090h | 19 | 1.4 | 41 | 15 | Pharmacological tool | |
THPO, 4,5,6,7-tetrahydroisoxazolo(4,5-c)pyridin-3-ol; exo-THPO, 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazol; NNC 05-2090, 1-[3-(9H-carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-4-piperidinol hydrochloride.
↵a Equivalent to mouse GAT-2.
↵b Equivalent to mouse GAT-3.
↵c Equivalent to mouse GAT-4.
↵d Kvist et al., 2009.
↵e Dhar et al., 1994; human GAT-1, human BGT-1, rat GAT-2, human GAT-3.
↵f Synthetic substrates.
↵g White et al., 2002; mouse GATs.
↵h Thomsen et al., 1997; mouse GATs.