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Table 1 Binding affinity of diazepam, ocinaplon and DOV 315,090 for GABAA-Rs with different subunit composition.

From: Pharmacological Properties of DOV 315,090, an ocinaplon metabolite

Receptor Type α1β2γ2S α1β2γ3 α2β2γ2S α2β2γ3 α3β2γ2S α5β2γ2S α5β2γ3
diazepam (DZ) IC50 (μM) 0.03 0.22 0.04 0.21 0.05 0.03 0.09
  pIC50 7.54 ± 0.09 6.67 ± 0.08 7.50 ± 0.10 6.80 ± 0.26 7.32 ± 0.08 7.57 ± 0.13 7.09 ± 0.13
ocinaplon (OC) IC50 (μM) 6.3 2.3 24 20 7.7 9.6 10
  pIC50 5.20 ± 0.14 5.65 ± 0.01 4.62 ± 0.14 4.74 ± 0.15 5.12 ± 0.06 5.02 ± 0.03 5.01 ± 0.18
  IC50/DZ IC50 218 10.5 759 115 158 355 120
DOV 315,090 IC50 (μM) 7.0 5.5 24 20 9.3 22 27
  pIC50 5.19 ± 0.12 5.27 ± 0.07 4.63 ± 0.05 4.72 ± 0.09 5.08 ± 0.14 4.67 ± 0.08 4.58 ± 0.09
  IC50/DZ IC50 220 25 760 120 170 790 323
  IC50/OC IC50 1.02 2.40 0.89 0.98 1.09 2.24 2.59
  1. IC50 values were calculated from [3H]Ro15–1788 displacement curves using non-linear regression analysis for each independent experiment. pIC50 values are averages of the negative logarithms of IC50s. Results from each experiment (n = 3) were fitted independently and fitted parameters were averaged to calculate means and SEM. EC50 values were averaged as their negative logarithms (pIC50).