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. 2019 Apr 15;151(6):798–819. doi: 10.1085/jgp.201812133

Table 2. Regression results from fitted zolpidem responses at wild-type and concatenated GABAARs.

Zolpidem
Construct Subunit EC50 (µM) pEC50 n GABA316 µM (nA)
 α1 + β2 1:50 No effect 7 2,100 ± 300
 α1 + β2 50:1 No effect 6 750 ± 250
 α1 + β2 + γ2 5:1:5 0.11 6.95 ± 0.02 11 2,900 ± 500
Dimeric constructs
 β2-23-α1 γ2 0.10 7.00 ± 0.03 8 7,600 ± 700
 α1-10-β2 γ2 0.18 6.74 ± 0.03 7 14,000 ± 6,000
 α1-9a-β2 γ2 0.19 6.72 ± 0.03 14 7,000 ± 1,000
 α1-6a-β2 γ2 0.15 6.83 ± 0.03 8 4,000 ± 500
 α1-3a-β2 γ2 0.20 6.71 ± 0.04 7 5,600 ± 1,300
 α1-0a-β2 γ2 0.21 6.68 ± 0.03 12 280 ± 50
Tetrameric constructs
 α1-10-β2-α1-β2 γ2 0.10 7.00 ± 0.03 9 5,000 ± 500
 α1-10-β2-α1-γ2 β2 0.092 7.04 ± 0.02 7 5,800 ± 400
Pentameric constructs
 α1-(-1a)-β2-α1-β2-γ2 0.17 6.76 ± 0.02 6 150 ± 50a
 α1-(-1a)-β2-α1-γ2-β2 0.19 6.72 ± 0.02 12 2,300 ± 300a
 γ2-15a-β2-α1-β2-α1 0.15 6.82 ± 0.02 9 6,100 ± 1,200
 γ2-13a-β2-α1-β2-α1 0.22 6.65 ± 0.02 11 4,400 ± 600a
 γ2-11a-β2-α1-β2-α1 0.27 6.57 ± 0.03 12 2,000 ± 30a
 γ2-10a-β2-α1-β2-α1 0.14 6.86 ± 0.02 11 1,700 ± 200a
 γ2-9a-β2-α1-β2-α1 0.17 6.78 ± 0.03 14 800 ± 150a
Mutant constructs
 α1-9a-β2 γ2(A118R) 3.4 5.46 ± 0.04 11 8,600 ± 1,100
 α1-0a-β2 γ2(A118R) 2.0 5.70 ± 0.03 7 990 ± 90
 α1R94A + β2 + γ2 5:1:5 0.20 6.71 ± 0.02 7 990 ± 110a
 γ2-11a-β2-α1-β2-α1R94A 0.36 6.44 ± 0.03 11 350 ± 50a
 γ2-11a-β2-α1-β2-α1R94A α1 0.20 6.71 ± 0.03 9 510 ± 130a

Data points were fitted to the Hill equation with bottom set to 0 and Hill slope set to 1 by nonlinear regression. Fitted potencies of zolpidem are presented as EC50 in µM and pEC50 ± SEM where p = −Log for the indicated number (n) of individual oocytes. The average peak-current amplitudes obtained with GABA316 µM applications are presented as mean ± SEM in nA for the tested oocytes. No effect, no positive enhancement of GABAcontrol-evoked currents was observed.

a

Due to the GABA EC50 value on this receptor, GABA316 µM applications do not represent a maximal EC100 concentration.