Table 3.
Rate constants for transitions between states of α1β3γ2, α4β3γ2 and α4β3δ GABAA receptors activated by GABA, muscimol and THIP
| α1β3γ2 |
α4β3γ2 |
α4β3δ |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Constant | Unit | GABA | Muscimol | THIP | GABA | Muscimol | THIP | GABA | Muscimol | THIP |
| k1 | m−1* s−1 | 51 × 106 | 453 × 106 | 1.6 × 106 | 3.5 × 106 | 7.1 × 106 | 3.9 × 106 | 32 × 106 | 15 × 106 | 5.7 × 106 |
| k−1 | s−1 | 399 | 245 | 3 | 6 | 6 | 6 | 7 | 1.3 | 56 |
| k2 | m−1* s−1 | 28 × 106 | 186 × 106 | 2.6 × 106 | 3.2 × 106 | 5.9 × 106 | 0.8 × 106 | 47 × 106 | 21 × 106 | 0.15 × 106 |
| k−2 | s−1 | 360 | 428 | 842 | 51 | 28 | 285 | 12 | 7 | 53 |
| δ | s−1 | 219 | 217 | 110 | 2 | 5 | 6 | 6 | 6 | 7 |
| δ−1 | s−1 | 17 | 21 | 15 | 3 | 11 | 15 | 3 | 6 | 2 |
| β1 | s−1 | 570 | 427 | 40 | 57 | 45 | 39 | 20 | 22 | 142 |
| α1 | s−1 | 2268 | 2471 | 2695 | 2972 | 2887 | 1625 | 465 | 1324 | 956 |
| β2 | s−1 | 2556 | 2690 | 1543 | 936 | 887 | 676 | 255 | 325 | 1362 |
| α2 | s−1 | 356 | 324 | 394 | 970 | 1023 | 812 | 1500 | 1729 | 348 |
| K1 | μm | 7.9 | 0.5 | 1.7 | 1.8 | 0.8 | 1.5 | 0.2 | 0.1 | 9.8 |
| K2 | μm | 12.8 | 2.3 | 330 | 16.0 | 4.7 | 357 | 0.3 | 0.3 | 359 |
| D | 13 | 10 | 7 | 0.62 | 0.45 | 0.40 | 2.0 | 1.0 | 3.5 | |
| E1 | 0.25 | 0.17 | 0.01 | 0.019 | 0.016 | 0.024 | 0.04 | 0.02 | 0.15 | |
| E2 | 7.2 | 8.3 | 3.9 | 1.0 | 0.9 | 0.8 | 0.17 | 0.19 | 3.9 | |
The rate constants were determined by optimally fitting the single channel data for each receptor (α1β3γ2, α4β3γ2 and α4β3δ) in the presence of each agonist (GABA, muscimol and THIP) at each of the three concentrations with the linear/branched receptor model using QuB. Values are accrued from n= 13–20 patches.