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. Author manuscript; available in PMC: 2020 Jan 3.
Published in final edited form as: J Med Chem. 2018 Mar 6;61(6):2422–2446. doi: 10.1021/acs.jmedchem.7b01664

Figure 1:

Figure 1:

The GABAAR α6β3γ2 Subtypea

aThe GABAAR α6β3γ2 subtype is a pentameric ligand-gated chloride channel comprised of two α6, two β3 and one γ2 subunits. PQs, like 8b, mediate their effects at the α6+β3- interface (PQ Site) as positive allosteric modulators and act at the DI-Bz site (α6+γ2- interface) as null modulators. The PQ site, the DI-Bz binding site and the endogenous ligand (GABA) binding sites at the β3+α6- interfaces are displayed. Image modified from Jacob et al., Nature Reviews Neuroscience, 2008.