TABLE 1.
Summary of pharmacological parameters of IGABA enhancement through α1β1γ2S, α1β2γ2S, and α1β3γ2S receptors including maximal IGABA enhancement (Emax), half-maximal effective concentrations (EC50), Hill-coefficients (nH), and number of experiments for each compound at the tested subunit combinations
Data for IGABA enhancement of α1β3γ2S receptors by VA at GABA EC3-7 concentrations taken from Luger et al. (2015).
| Emax (%) | EC50 () | nH | n | |
|---|---|---|---|---|
| % | µM | |||
| α1β1γ2S | ||||
| VA | 111 ± 16 | 74.4 ± 19.3 | 1.6 ± 0.5 | 8 |
| VA-A | 218 ± 78 | 66.6 ± 34.6 | 1.8 ± 0.6 | 6 |
| VA-MA | 387 ± 56 | 58.1 ± 16.5 | 1.6 ± 0.3 | 5 |
| VA-DMA | 305 ± 67 | 52.5 ± 20.1 | 1.7 ± 0.5 | 6 |
| VA-EA | 458 ± 124 | 51.4 ± 19.8 | 1.6 ± 0.3 | 5 |
| VA-DEA | 318 ± 84 | 97.2 ± 33.8 | 1.8 ± 0.3 | 7 |
| VA-CN | 55 ± 14 | 73.0 ± 38.7 | 1.7 ± 0.7 | 7 |
| VA-TET | 176 ± 43 | 23.5 ± 10.9 | 1.8 ± 0.6 | 7 |
| α1β2γ2S | ||||
| VA | 721 ± 68 | 23.1 ± 4.2 | 1.4 ± 0.2 | 5 |
| VA-A | 1119 ± 72 | 14.0 ± 2.2 | 1.4 ± 0.2 | 6 |
| VA-MA | 917 ± 36 | 9.1 ± 1.4 | 1.5 ± 0.1 | 3 |
| VA-DMA | 594 ± 36 | 63.9 ± 23.7 | 1.3 ± 0.2 | 5 |
| VA-EA | 554 ± 49 | 11.0 ± 3.6 | 1.6 ± 0.3 | 3 |
| VA-DEA | 573 ± 33 | 54.4 ± 11.1 | 1.6 ± 0.3 | 5 |
| VA-CN | 765 ± 117 | 56.5 ± 13.3 | 2.5 ± 0.7 | 4 |
| VA-TET | 1091 ± 87 | 34.1 ± 6.3 | 1.0 ± 0.1 | 5 |
| α1β3γ2S | ||||
| VA | 632 ± 88 | 20.2 ± 5.2 | 1.5 ± 0.3 | 9 |
| VA-A | 972 ± 69 | 7.5 ± 1.8 | 1.5 ± 0.2 | 6 |
| VA-MA | 1043 ± 57 | 12.7 ± 0.9 | 1.5 ± 0.1 | 6 |
| VA-DMA | 415 ± 61 | 48.0 ± 16.0 | 1.4 ± 0.2 | 6 |
| VA-EA | 677 ± 64 | 27.2 ± 6.7 | 1.3 ± 0.2 | 12 |
| VA-DEA | 374 ± 102 | 80.8 ± 31.3 | 1.9 ± 0.5 | 5 |
| VA-CN | 522 ± 114 | 42.4 ± 15.8 | 2.1 ± 0.8 | 7 |
| VA-TET | 668 ± 57 | 6.0 ± 1.0 | 1.1 ± 0.1 | 8 |