TABLE 1

Affinity of NS11394 and diazepam at GABAA receptors in rat cortical membranes and human α1–α6 containing GABAA receptors expressed in HEK-293 cells Data are expressed as mean Ki (nM) ± S.E.M. of three to four independent experiments in triplicate.


Compound

[3H]Flunitrazepam

[3H]Ro 15-1788

[3H]Ro 15-4513
Rat Cortex
α1β3*γ2S
α2β3*γ2S
α3β3*γ2S
α5β3*γ2S
α4β3*γ2S
α6β3*γ2S
NS11394 0.423 ± 0.083 0.41 ± 0.12 0.84 ± 0.10 0.497 ± 0.046 0.119 ± 0.029 324 ± 24 1009 ± 160
Diazepam
11.3 ± 3.1
10.1 ± 1.8
7.5 ± 1.4
19.3 ± 3.6
5.33 ± 0.53
>15,000
>15,000