Table 3.
Affinity changes of GABA EC50 values obtained from FLIPR experiments
| GABAAR subunits transfected | Agonist / modulator | pEC50 [M] | EC50 [μM] | Ratio [EC50 / EC50mod] |
|---|---|---|---|---|
| Human α1β2γ2 | GABA | 4.75 ± 0.21 | 20.80 ± 7.00 | |
| Diazepam | 5.37 ± 0.06 | 4.19 ± 0.86 | 8.29 | |
| Linalool | 4.96 ± 0.38 | 10.80 ± 0.41 | 3.22 | |
| Carveol | 5.45 ± 0.22 | 3.59 ± 0.60 | 3.96 | |
| Isopulegol | 5.49 ± 0.16 | 3.26 ± 0.69 | 4.36 | |
| Pinocarveol | 5.52 ± 0.06 | 3.03 ± 0.87 | 4.68 | |
| Verbenol | 5.56 ± 0.12 | 2.73 ± 0.76 | 5.21 | |
| Theaspirane | 5.18 ± 0.08 | 6.56 ± 0.83 | 2.06 | |
| Myrtenol | 5.73 ± 0.33 | 1.83 ± 0.46 | 7.40 |
Mean values derived from Flexstation measurements (±SD). EC50 values from GABAARs expressed in HEK293 cells from three independent experiments.