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Table 2 Properties of diazepam, ocinaplon and DOV315090 determined by two-electrode voltage clamp electrophysiology using Xenopus oocytes injected with cRNA.

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

Receptor Type   α1β2γ2S α2β2γ2S α3β2γ2S α5β2γ2S
diazepam (DZ) EC50 (μM) 0.04 (8) 0.03 (10) 0.092 (5) 0.025 (5)
  pEC50 7.46 ± 0.07 7.60 ± 0.044 7.04 ± 0.05 7.51 ± 0.11
  Emax, % 144 ± 8.0 157 ± 14 232 ± 31 224 ± 24
ocinaplon (OC) EC50 (μM) 2.93 (4) 9.12 (5) 8.01 (4) 3.5 (4)
  pEC50 5.57 ± 0.11 5.04 ± 0.03 5.16 ± 0.14 5.48 ± 0.07
  EC50/DZ EC50 77 350 87 139
  Emax, % 132 ± 8 150 ± 6 181 ± 18 84 ± 4
  Emax/DZ Emax 0.91 0.95 0.78 0.37
DOV315090 (MET) EC50 (μM) 4.87 (4) 12.5 (4) 10.21 (4) 10.14 (4)
  pEC50 6.32 ± 0.05 4.92 ± 0.09 5.00 ± 0.05 5.03 ± 0.10
  EC50/DZ EC50 128 482 111 405
  EC50/OC EC50 1.66 1.37 1.27 2.92
  Emax, % 192 ± 4 139 ± 23 * 340 ± 35 * 68 ± 8
  Emax/DZ Emax 1.33 0.88 1.46 0.30
  Emax/OC Emax 1.45 0.92 1.87 0.81
  1. Drugs were prepared from DMSO stock solution prior to experiment, EC10s of GABA were used, errors are SEM of fitted parameter values from the number of oocytes given in parentheses. Results from each oocyte were fitted independently and fitted parameters were averaged to calculate means and SEM. EC50 values were averaged as their negative logarithms (pEC50) * For these two cases, the extrapolated Emax exceeded the observed maximum observed potentiation by over 25%, but parameter SEM was not substantially increased, indicating that range of concentrations was adequate to project Emax. Higher drug concentrations could not be used due to solubility constraints.