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. 2020 Jun 22;10:10078. doi: 10.1038/s41598-020-66821-0

Figure 3.

Figure 3

Whole-cell patch-clamp electrophysiology studies of α4β1δ receptors support the antagonism determined in the FMP assay. (A) 018 concentration-dependently inhibits the current induced by 2.5 μM GABA (corresponding to GABA EC30-40) at α4β1δ receptors with an IC50 of 10.8 nM and a Hill slope of −0.74. Gabazine was included as reference with an IC50 of 0.18 μM and a Hill slope of −1.53. (B) Representative current traces for 018 and gabazine. The dotted line represents 30 sec pre-application of the antagonist. Data are shown as pooled data from 5–7 cells given as means ± SEM and normalized to the GABA 2.5 μM control.