TABLE 1

Affinity of TPA023 for human recombinant GABAA receptors containing different α subunits and native rat brain receptors Data shown are the mean ± S.E.M. (n = 3–5 separate determinations).


Ki
Human Recombinant GABAA Receptors Containing β3, γ2 plus
Native Rat Brain Receptor
α1
α2
α3
α4
α5
α6
Cerebellum
Spinal Cord
nM nM
0.27 ± 0.04
0.31 ± 0.03
0.19 ± 0.01
60 ± 7
0.41 ± 0.09
418 ± 72
0.33 ± 0.05
0.32 ± 0.01