Table 1.

Binding affinity of TP003 to recombinant human GABAA receptors expressed in Ltk—cells using [3H]Ro 15-1788 ([3H]flumazenil) as a radioligand for α1-, α2-, α3-, and α5-containing receptors and [3H]Ro 15-4513 for α4- and α6-containing receptors

Receptor combination Binding Ki (nm)
α1β3γ2 0.32 ± 0.21
α2β3γ2 0.54 ± 0.17
α3β3γ2 0.50 ± 0.18
α4β3γ2 2435 ± 1041
α5β3γ2 0.26 ± 0.08
α6β3γ2 1815 ± 767
  • Data represent means ± SEM of five to eight determinations.