Figure 3

G protein mediated effects of chemically diverse mixed MOP/NOP agonists using GIRK assay. Concentration–response curves obtained for prototypical selective agonist DAMGO (A) and N/OFQ (G), novel mixed MOP/NOP agonists cebranopadol (B, H), AT-034 (C, I), AT-324 (D, J), AT-201 (E, K), AT-121 (F, L) at MOP and NOP, respectively. AtT-20 cells stably expressing MOP and NOP were stimulated with the agonists at a concentration range of 10^–6 to 10^–12 M and the signal was measured using GIRK channel-based membrane potential assay. Each data point (mean ± SEM) represents assay read-out obtained from four different experiments in duplicates. (ΔRFU, change in relative fluorescence unit).