α1β2 | α1β2(E155C) | ||||
---|---|---|---|---|---|
Ligand | EC50/IC50(μm) | nH | EC50/IC50 (μm) | nH | mut/wt |
GABAa | 1.6 ± 0.2 | 1.35 ± 0.15 | 5400 ± 1500* | 1.21 ± 0.07 | 3375 |
P4S | 4.7 ± 0.4 | 1.59 ± 0.22 | 730.7 ± 52.1* | 1.30 ± 0.11 | 152 |
SR-95531a | 0.2 ± 0.08 | 1.13 ± 0.10 | 1.8 ± 0.4* | 0.66 ± 0.1 | 11.1 |
PTX | 4.7 ± 1.2 | 0.84 ± 0.02 | 3.1 ± 0.1 | 0.81 ± 0.10 | 0.6 |
Pentobarbital | 1100 ± 300 | 1.56 ± 0.07 | 530 ± 100* | 1.08 ± 0.02 | 0.5 |
Data represent the mean ± SE for more than three experiments. EC50 values, IC50 values, KI values, and Hill slopes (nH) were determined from concentration-response data using nonlinear regression analysis with GraphPad Prism software. Hill slopes, log(EC50), log(IC50), and log (KI) values were analyzed using a two-tailed unpaired t test to determine the levels of significance (*p < 0.01; from α1β2). mut, Mutant, wt, wild type.
↵ a Values are from Table 1.