Fig 1. Saz-A and TC-2559 act selectively at the α4-β2 interface.
A Schematic showing α4-β2 (black arrow) and α-α (grey arrow) binding sites for ACh at the 3α4:2β2, 2α4:3β2 and 3α4:2β2HQT receptors. B. Current traces of Saz-A (1μM) and C. TC-2559 (10μM) for 3α4:2β2, 2α4:3β2 and 3α4:2β2HQT receptor compared to maximum ACh currents on the same oocyte. Peak currents elicited by D Saz-A and E TC-2559 were normalized to the saturating concentration of ACh and fitted to non-linear curve fits. The injection ratios of α4:β2 that correspond to the 3α4:2β2 (blue) and the 2α4:3β2 (red) receptors are 4:1 and 1:4 respectively. Saz-A and TC-2559 do not activate the 3α4:2β2HQT (green) receptor that has three α4-α4-like interfaces. Dots represent the mean ± s.e.m.