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. 2014 Nov 19;290(2):1039–1048. doi: 10.1074/jbc.M114.605592

FIGURE 3.

FIGURE 3.

Inhibition of nAChR subtypes expressed in Xenopus oocytes by RegIIA and alanine analogs. A, bar graph of inhibition of nAChR subtypes by RegIIA and its analogs. B, two-way analysis of variance scatter plot illustrating the loss of activity of RegIIA analogs (300 nm) relative to wild-type RegIIA at various nAChR subtypes. [H14A]RegIIA completely lost its activity at α3β2, α3β4, and α7 nAChRs. [N9A]RegIIA was more selective for the α3β2 subtype than RegIIA. [N11A]RegIIA and [N12A]RegIIA selectivity for the α3β4 nAChR subtype significantly improved. All analogs, except [P13A]RegIIA, significantly lost activity at the α7 nAChR subtype. ***, p < 0.001; *, p < 0.05; n = 4–6. C, superimposed traces showing inhibition of α3β2 nAChR-mediated ACh-evoked currents by 100 nm RegIIA (i), [N11A]RegIIA (ii), and [N11A]RegIIA (iii). D, concentration-response curves for RegIIA (i), [N11A]RegIIA (ii) and [N12A]RegIIA (iii) inhibition of the α3β4 (black line, open symbols) and α3β2 nAChR subtypes (dash line, closed symbols). [N11A]RegIIA and [N12A]RegIIA shifted the curve to the right for the α3β2 nAChR subtype, giving an IC50 value of 116 and 278 nm, respectively. All data represents mean ± S.E., n = 4–6.