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. Author manuscript; available in PMC: 2017 Sep 22.
Published in final edited form as: J Med Chem. 2016 Sep 2;59(18):8381–8397. doi: 10.1021/acs.jmedchem.6b00748

Figure 3.

Figure 3

β-arrestin-2 recruitment and antagonism of β-arrestin-2 recruitment. (A) β-arrestin-2 recruitment: β-arrestin-2 recruitment was determined using the DiscoveRx PathHunter enzyme complementation assay using modified MOR-1 in CHO cells. Compounds were found to be completely G-protein biased. (B) Antagonism of β-arrestin-2 recruitment: The same cells were incubated with the antagonist (2, 3) for 30 min at 37 °C prior to the addition of agonist (10 μM DAMGO) at MOR-1. Compounds 2 and 3 were able to antagonize β-arrestin-2 recruitment by DAMGO. IC50 values: 2: 725 ± 292 nM; 3: 34 ± 2 nM.