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. Author manuscript; available in PMC: 2016 Apr 8.
Published in final edited form as: Nature. 2015 Sep 7;526(7572):224–229. doi: 10.1038/nature14853

Figure 3. Strychnine and ivermectin bind at subunit interfaces.

Figure 3

Strychnine binding site (+; light blue) (−; gray); view is parallel to the membrane (a) or from the extracellular side (b). Density for strychnine (blue mesh) is contoured at 7 σ. c, Saturation binding of 3H strychnine to the GlyREM construct. Results are the mean of three biological replicates and the error bars represent s.e.m. d–e, Ivermectin binds at TMD intersubunit interface. Views are parallel to the membrane (d) or the extracellular side (e). f, Activation of GlyR currents by 10 mM glycine determined by TEVC. g, Strychnine (1 μM) inhibits glycine-induced (0.3 mM) currents. h, Effect of picrotoxinin (ptx, 1 mM) on glycine (0.3 mM) induced current. Ptx inhibits ~80% of glycine-induced current. Ivermectin (5 μM) potentiates the GlyR current and causes a slow desensitization. The shown recordings are representative of three independent experiments.