TABLE 2.
PUBLISHED AFFINITIES OF SUBTYPE-SPECIFIC γ–AMINO BUTYRIC ACID TRANSPORTER INHIBITOR DRUGS
| SKF 89976A IC50 (21) |
β-Alanine IC50 (21) |
Flufenamic Acid IC50 (22) |
NNC 05-2090 IC50 (20) |
|
|---|---|---|---|---|
| GABA Transporter Subtype | (μM) | (μM) | (μM) | (μM) |
| Human GAT1 | 0.13 ± 0.01 | 5690 ± 1890 | >500 | 19 ± 2 |
| Human GAT2 | 550 ± 225 (rat) | 19 ± 7 | 41 ± 11 | |
| Human GAT3 | 944 ± 259 | 58 ± 3 | ∼30 | 15 ± 4 |
| Human GAT4/BGT-1 | 7210 ± 3630 | 1320 ± 224 | 1.4 ± 0.3 |
Definition of abbreviations: BGT, betaine–GABA transporter; GABA, γ–amino butyric acid; GAT, GABA transporter; IC50, half maximal (50%) inhibitory concentration; SKF 89976A, 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride.