TABLE 1

Affinity of α5IA for human recombinant and native rat brain GABAA receptors

Affinity at α1-, α2-, α3-, and α5-containing recombinant as well as native rat brain GABAA receptor was measured using a [3H]flumazenil binding assay, whereas affinity for receptors containing either an α4 or α6 subunit was measured using [3H]Ro 15-4513. Data are the mean ± S.E.M. (n = 3–6 separate determinations).

Human Recombinant GABAA Receptors Containing β3, γ2 Plus Native Rat Brain Receptor
α1 α2 α3 α4 α5 α6 Cortex Hippocampus
Ki, nM
0.88 ± 0.19 0.58 ± 0.17 0.61 ± 0.17 60 ± 7 0.66 ± 0.14 418 ± 72 0.90 ± 0.07 1.2 ± 0.2