Table 1.
Potency and efficiency of piperine/SCT-66 enhancement of GABAA receptors with different subunit compositions.
| Subunit combination | EC50 (μM) | Maximum stimulation of-IGABA at EC3–7 | Hill coefficient (nH) | Number of experiments (n) |
|---|---|---|---|---|
| Piperine | ||||
| α1β1 | 57.6 ± 4.2 | 171 ± 22 | 1.4 ± 0.2 | 10 |
| α1β2 | 50.0 ± 7.9 | 271 ± 36 | 1.5 ± 0.3 | 13 |
| α1β3 | 48.3 ± 7.3 | 332 ± 64 | 1.5 ± 0.3 | 7 |
| α2β2 | 42.8 ± 17.6 | 248 ± 48 | 1.9 ± 0.5 | 6 |
| α3β2 | 59.6 ± 12.3 | 375 ± 51 | 1.4 ± 0.2 | 6 |
| α5β2 | 47.5 ± 17.9 | 136 ± 22 | 1.7 ± 0.4 | 6 |
| SCT-66 | ||||
| α1β1 | 13.3 ± 2.9 | 1112 ± 136 | 1.5 ± 0.2 | 4 |
| α1β2 | 19.8 ± 9.7 | 1256 ± 292 | 1.3 ± 0.4 | 4 |
| α1β3 | 12.3 ± 4.5 | 1128 ± 155 | 1.5 ± 0.3 | 3 |
| α1β2γ2S | 21.5 ± 1.7 | 378 ± 15 | 1.8 ± 0.2 | 6 |
| α2β2 | 13.1 ± 9.0 | 1204 ± 233 | 1.1 ± 0.3 | 4 |
| α2β2γ2S | 24.1 ± 7.5 | 572 ± 51 | 1.3 ± 0.3 | 5 |
| α3β2 | 22.2 ± 12.1 | 1169 ± 195 | 0.9 ± 0.2 | 3 |
| α3β2γ2S | 15.1 ± 1.8 | 584 ± 20 | 1.6 ± 0.2 | 5 |
| α5β2 | 11.5 ± 2.7 | 705 ± 24 | 1.3 ± 0.2 | 3 |
| α5β2γ2S | 14.2 ± 1.4 | 398 ± 26 | 2.0 ± 0.3 | 5 |