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. Author manuscript; available in PMC: 2010 Dec 22.
Published in final edited form as: Biochemistry. 2009 Dec 22;48(50):11872–11882. doi: 10.1021/bi9014488

Figure 2. Inhibition efficiency of amantadine, BL-1743 and spiran amine 8 on wt A/M2 channels and A/M2 L26F, V27A and S31N mutants.

Figure 2

Channel activity was assayed by TEVC for A/M2 channels expressed in Xenopus oocytes. Responses in the presence of various concentrations of an inhibitor (I) were normalized to the current evoked by application of the activating (pH 5.5) solution without inhibitor (I0). The experimental data are the average of three independent experiments. Each point is the mean (±SD) of 5–8 oocytes. IC50 values in μM: A/M2 with amantadine IC50=15.76±1.24; with BL-1743 IC50=46.25±3.56; with spiran amine 8 IC50=12.59±1.11. A/M2-L26F with amantadine IC50=164.46±14.40; with BL-1743 IC50>10 mM; with spiran amine 8 IC50=30.62±8.13. A/M2-V27A with amantadine IC50=1840; with BL-1743 IC50>10 mM; with spiran amine 8 IC50=84.92±13.61. A/M2- S31N with amantadine IC50=237.01±22.14; with BL-1743 IC50>10 mM; with spiran amine 8 IC50>10 mM.