Table 1.
Pharmacological properties of studied GABAAreceptors
| Isoform | THDOC | GABA | THDOC + GABA | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| n | EC50 | nH | Imax(pA) | n | EC50 | nH | n | EC50 | nH | Max (%) | |
| α1β3γ2L | 3 | 1.9 | 1.4 | 2141 ± 200 | 4 | 2.3 | 1.4 | 6 | 2.8 | 1.5 | 128 ± 10 |
| α1β3δ | 4 | 9.51-a | 0.9 | 498 ± 150 | 4 | 5.8 | 1.0 | 4 | 6.6 | 1.1 | 265 ± 47* |
| α1β3 | 3 | 6.7 | 1.1 | 1302 ± 360 | 3 | 3.0 | 2.0 | 3 | 1.7 | 1.6 | 113 ± 4 |
| α6β3γ2L | 4 | 0.7 | 2.2 | 1588 ± 700 | 5 | 0.6 | 1.3 | 4 | 0.6 | 1.3 | 124 ± 6 |
| α6β3δ | 3 | 1.4 | 1.3 | 285 ± 60 | 4 | 0.6 | 1.1 | 5 | 0.4 | 1.3 | 145 ± 15 |
| α6β3 | 3 | 2.6 | 1.6 | 778 ± 130 | 3 | 0.6 | 1.2 | 3 | 1.2 | 1.1 | 152 ± 26 |
n indicates the number of cells tested. All EC50 values are in micromolar. nH is the hill coefficient. Max (%) indicates the maximum current observed with THDOC + GABA compared with maximum current observed with GABA alone.
*
Significant difference from all other isoforms (p < 0.05).
F1-a
Indicates that full concentration–response curve could not be obtained because of high DMSO vehicle concentration.