Table 2.
Concentration-response data for GABA, P4S, SR-95531, PTX, and pentobarbital for α1β2 and α1β2(E155C) receptors expressed in Xenopus oocytes
| 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.