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/IC50m) nH EC50/IC50m) 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.