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. 2016 May 20;6:25943. doi: 10.1038/srep25943

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Copyright © 2016, Macmillan Publishers Limited

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(a) Model structure of the GABA_A receptor transmembrane domain. The major isoform of the GABA_A receptor is composed of two α₁, two β₂, and one γ₂ subunits. The model structure depicts the crystalized homomeric β₃ GABA_A receptor (PDB structure 4COF)³⁸. In this figure, some of the β₃ subunits were renamed α₁ (yellow), β₂ (blue) and γ₂ (red); structures are shown in ribbon representation. The mutated residues α₁S269, β₂N265, and γ₂S280 are located at the interfaces between subunits. (b) Potentiation of the GABA response by compound 31 (3 μM), compound 132 (3 μM), and 4-O-methylhonokiol (1 μM, abbreviated Mh) in wild-type α₁β₂γ₂, single mutant (α₁M, β₂M, γ₂M), and triple mutant receptors expressed in Xenopus oocytes. The bars indicate mean ± SD, n = 3.