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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).