FIGURE 5.
[N11A,N12A]RegIIA inhibition of α6/α3β2β3 and α6/α3β4β3 nAChR compared with wild-type RegIIA inhibition of these receptors. A, superimposed traces showing ACh-evoked current inhibition of α6/α3β2β3 and α6/α3β4β3 nAChR subtypes by RegIIA and [N11A,N12A]RegIIA. B, wild-type RegIIA was active at α6-containing receptors with IC50 values of 40 and 147 nm at α6/α3β2β3 (♢) and α6/α3β4β3 (○) receptors, respectively. Concentration-response curve for [N11A,N12A]RegIIA gave an IC50 value of 5.1 μm at α6/α3β4β3 (●), with an approximate 35-fold decrease in potency compared with RegIIA. [N11A,N12A]RegIIA showed no activity at α6/α3β2β3 (♦) when tested at a concentration of 10 μm. Data represents mean ± S.E., n = 3–6.