TABLE 1.
Summary of results obtained using GABA as agonist
Electrophysiological data are shown in regular type, and fluorescence data are shown in bold. —, not quantitated.
| Construct | EC50 | nH | Imax or ΔFmax | n |
|---|---|---|---|---|
| μm | ||||
| α1 β2 unlabeled | 0.8 ± 0.1 | 1.5 ± 0.1 | 9.5 ± 0.7 μA | 5 |
| α1 β2 MTS-R | 0.7 ± 0.1 | 1.4 ± 0.1 | 8.9 ± 0.5 μA | 5 |
| α1 β2 γ2 unlabeled | 3.2 ± 0.2 | 1.6 ± 0.1 | 9.6 ± 0.7 μA | 4 |
| α1 β2 γ2 MTS-R | 3.5 ± 0.4 | 1.8 ± 0.1 | 10.3 ± 1.3 μA | 4 |
| α1-R186C β2 unlabeled | 3.3 ± 0.2a | 1.2 ± 0.1 | 7.4 ± 0.2 μA | 3 |
| α1-R186C β2 MTS-R | 9.2 ± 1.1b | 1.1 ± 0.1 | 2.6 ± 0.3 μAb | 4 |
| α1-R186C β2 MTS-R | 8.0 ± 0.7 | 0.8 ± 0.1 | 4.9 ± 0.4% | 4 |
| α1 β2-I180C unlabeled | 1.0 ± 0.1 | 1.3 ± 0.1 | 6.9 ± 1.2 μA | 3 |
| α1 β2-I180C MTS-TAMRA | 1.1 ± 0.2 | 1.5 ± 0.1 | 7.5 ± 1.8 μA | 4 |
| α1 β2-I180C MTS-TAMRA | 1.0 ± 0.1 | 0.8 ± 0.1 | 1.5 ± 0.1% | 4 |
| α1 β2 γ2-S195C unlabeled | 2.9 ± 0.1 | 1.7 ± 0.03 | 10.1 ± 1.1 μA | 4 |
| α1 β2 γ2-S195C TMRM | 6.1 ± 0.6a | 1.6 ± 0.1 | 13.4 ± 1.7 μA | 3 |
| α1 β2 γ2-S195C TMRM | 3.8 ± 0.2 | 1.8 ± 0.4 | 1.7 ± 0.1% | 3 |
| α1-N20′C β2 unlabeled | 1.5 ± 0.2c | 1.1 ± 0.1 | 8.1 ± 1.1 μA | 3 |
| α1-N20′C β2 TMRM | 0.40 ± 0.03a | 1.2 ± 0.2 | 6.1 ± 0.9 μAc | 4 |
| α1-N20′C β2 TMRM | — | — | 2.2 ± 0.4% | 4 |
| α1-N20′C β2 γ2 unlabeled | 14.2 ± 1.6b | 1.1 ± 0.1 | 6.2 ± 1.0 μAc | 3 |
| α1-N20′C β2 γ2 TMRM | 13.5 ± 0.5b | 1.1 ± 0.1 | 8.3 ± 0.7 μA | 4 |
| α1-N20′C β2 γ2 TMRM | — | — | 0.8 ± 0.1% | 4 |
| α1 β2-K24′C unlabeled | 25.6 ± 4.2b | 1.1 ± 0.1 | 1.6 ± 0.2 μAb | 4 |
| α1 β2-K24′C MTS-R | 30.3 ± 3.8b | 0.7 ± 0.1b | 0.7 ± 0.1 μAb | 4 |
| α1 β2-K24′C MTS-R | 38.4 ± 3.8 | 0.90 ± 0.1 | 1.1 ± 0.1% | 4 |
| α1 β2-K24′C γ2 unlabeled | 91 ± 9b | 1.1 ± 0.1 | 7.8 ± 1.4 μA | 3 |
| α1 β2-K24′C γ2 MTS-R | 31.0 ± 2.3b | 0.8 ± 0.1b | 5.4 ± 1.2 μAc | 4 |
| α1 β2-K24′C γ2 MTS-R | 67 ± 1 | 0.8 ± 0.1 | 0.74 ± 0.02% | 4 |
| α1 β2 γ2-P23′C unlabeled | 2.7 ± 0.1 | 1.8 ± 0.1 | 9.2 ± 0.8 μA | 5 |
| α1 β2 γ2-P23′C TMRM | 4.3 ± 0.7 | 1.7 ± 0.3 | 9.3 ± 0.3 μA | 5 |
| α1 β2 γ2-P23′C TMRM | — | — | 0.9 ± 0.1% | 5 |
a p < 0.01 relative to corresponding value at unlabeled α1 β2 GABAAR using unpaired t test.
b p < 0.001 relative to corresponding value at unlabeled α1 β2 GABAAR using unpaired t test.
c p < 0.05 relative to corresponding value at unlabeled α1 β2 GABAAR using unpaired t test.