TABLE 1.
Dose-response properties of GlyR α3 mutants
The data are given as the means ± S.D.
| Subunit | EC50a | nHilla | Isata | Calculated EC50b | KDb | Φb | Imaxb | Number of cellsc | KD ([3H]Stry)d |
|---|---|---|---|---|---|---|---|---|---|
| μm | pA | μm | μm | pA | nm | ||||
| α3L | 35 ± 4 | 1.8 ± 0.3 | 2410 ± 410 | 40 | 56 ± 14 | 0.23 ± 0.11 | 3251 ± 317 | 8 | 12.2 ± 1.7 |
| α3K | 24 ± 2 | 2.8 ± 0.4 | 2088 ± 240 | 30 | 43 ± 9 | 0.23 ± 0.09 | 2838 ± 237 | 7 | 5.3 ± 0.4 |
| α3LΔ6 | 3.9 ± 0.5 | 1.8 ± 0.4 | 3870 ± 400 | 3.6 | 39 ± 16 | 0.007 ± 0.005 | 3938 ± 452 | 5 | 30.1 ± 2.2 |
| α3L+6 | 26 ± 1 | 4.7 ± 0.7 | 1850 ± 150 | 23 | 19 ± 3 | 0.30 ± 0.06 | 2540 ± 148 | 6 | |
| α3LT358A | 86 ± 10 | 1.3 ± 0.3 | 570 ± 50 | 91 | 33 ± 7 | 3.24 ± 0.34 | 1161 ± 132 | 6 | |
| α3LY367F | 8.9 ± 0.4 | 1.6 ± 0.4 | 1790 ± 220 | 8.1 | 7 ± 2 | 0.67 ± 0.04 | 2896 ± 205 | 5 | |
| α3LS370A | 28 ± 4 | 1.2 ± 0.2 | 1350 ± 220 | 17 | 16 ± 3 | 1.04 ± 0.50 | 2738 ± 142 | 5 | |
| α3LT358A/Y367F | 157 ± 23 | 1.1 ± 0.2 | 680 ± 120 | 148 | 51 ± 12 | 5.38 ± 1.93 | 1589 ± 145 | 6 | |
| α3LT358A/S370A | 89 ± 7 | 1.8 ± 0.3 | 360 ± 30 | 93 | 53 ± 16 | 3.11 ± 0.30 | 1215 ± 72 | 5 | 27.8 ± 5.9 |
| α3LY358F/S370A | 16 ± 2 | 1.6 ± 0.3 | 1370 ± 140 | 23 | 11 ± 2 | 1.40 ± 0.90 | 3340 ± 145 | 8 | |
| α3LT358A/Y358F/S370A | 51 ± 5 | 1.6 ± 0.3 | 2020 ± 110 | 54 | 52 ± 12 | 0.55 ± 0.10 | 2451 ± 275 | 5 |
a Data from dose-response curves.
b Data from two-ligand model.
c Data for whole cell recording.
d Data from the radioligand binding assay.