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. 2013 Apr 25;169(2):371–383. doi: 10.1111/bph.12151

Figure 1.

Figure 1

Top view onto the extracellular domain of GABAA receptors. Each subunit features a plus (+) and a minus (−) side. Binding sites for GABA are located at the interfaces formed by the ‘+’ side of the β and the ‘−’ side of the α subunits. (A) α1β3γ2 receptors composed of one γ2, two α1 and two β3 subunits. The binding site for benzodiazepine ligands (Bz) is located at the interface formed by the ‘+’ side of the α and the ‘−’ side of the γ subunit. The CGS 9895 (compound 3) binding site is located at the interfaces formed by the ‘+’ side of the α and the ‘−’ side of the β subunit. (B) α1β3 receptors composed of two α1 and three β3 subunits. To avoid interaction with the benzodiazepine binding site, we used GABAA receptors composed of α1 and β3 subunits only. Such receptors are assumed to be composed of three β and two α subunits (Tretter et al., 1997; Farrar et al., 1999; Baumann et al., 2001), and should, thus, have two β3+/α1− interfaces (GABA binding sites), two α1+/β3− interfaces and one β3+/β3− interface, but no benzodiazepine binding site.