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. 2014 Nov;144(5):469–486. doi: 10.1085/jgp.201411222

Figure 4.

Figure 4.

Effect of sulfonylureas on (Mg)ADP modulation of SUR1- and SUR2A-containing channels. (A and B) Concentration-response relationships for ADP modulation of Kir6.2/SUR1 channels in the absence (A) or presence (B) of 2 mM Mg2+ and the absence (open symbols) or presence (closed symbols) of 30 µM gliclazide. (A) The lines are the best fit of Eq. 1 to the mean data: IC50 = 64 µM, h = 0.81 (open squares; n = 6); IC50 = 57 µM, h = 0.95 (closed squares; n = 6). (B) The lines are the best fit to the mean data of Eq. 4 with IC50 = 224 µM, h1 = 1.3 and EC50 = 11 µM, h2 = 1.3 and a = 2.7 (open circles; n = 12) or of Eq. 1 with IC50 = 64 µM, h = 0.91 (closed circles; n = 6). (C and D) Concentration-response relationships for ADP modulation of Kir6.2/SUR2A-YS channels in the absence (C) and presence of 2 mM Mg2+ (D) and in the presence (closed symbols; n = 6) or absence (open symbols; n = 6) of 30 µM gliclazide. (C) The lines are the best fit of Eq. 1 to the mean data: IC50 = 94 µM, h = 1.1 (open squares; n = 6); IC50 = 76 µM, h = 1.2 (closed squares; n = 6). (D) The solid line is the best fit to the mean data of Eq. 4 with IC50 = 240 µM, h1 = 1.2 and EC50 = 19 µM, h2 = 1.5 and a = 1.3. The dotted line is the concentration-inhibition curve for Kir6.2/SUR2A-YS channels in the absence of Mg2+ and gliclazide (C, open squares). (E and F) Concentration-response relationships for ADP modulation of Kir6.2/SUR2A channels in the absence (E) and presence of 2 mM Mg2+ (F) and in the absence (open symbols) or presence (closed symbols) of 1 µM glibenclamide. (E) The lines are the best fit of Eq. 1 to the mean data: IC50 = 90 µM, h = 0.86 (open squares; n = 6); IC50 = 70 µM, h = 0.95 (closed squares; n = 6). (F) Both open and closed circles are the mean of seven experiments. The solid line is the best fit to the mean data of Eq. 4 with IC50 = 270 µM, h1 = 1.4 and EC50 = 18 µM, h2 = 1.3 and a = 1.0. The dotted line is the concentration-inhibition curve for Kir6.2/SUR2A channels in the absence of Mg2+ and glibenclamide (E, open squares). Mean ± SEM.