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. Author manuscript; available in PMC: 2022 Aug 11.
Published in final edited form as: J Med Chem. 2018 Oct 11;61(20):9335–9346. doi: 10.1021/acs.jmedchem.8b01249

Figure 2.

Figure 2.

Antagonistic effect of the studied compounds on global cellular response induced by sumanirole. Dynamic mass redistribution (DMR) assays were performed in CHO cells stably expressing D2R and A2AR. A) Quantification of the antagonist effect of all D2R ligands on DMR. Values are mean±SEM from 3 determinations carried out in triplicates. Statistical significance was calculated by one-way ANOVA followed by Dunnett’s post hoc test. **p<0.01 compared to sumanirole alone. B) Representative DMR curves from one of these experiments in which cells were treated with medium (control) (black), with 1μM of spiperone (grey), with 1μM of monovalent compounds 14 (light blue) or 15 (dark blue) or with 500 nM of bivalent compounds 12 (orange) or 13 (red) for 30 minutes. After that, cells were treated with 100 nM of sumanirole. Each curve is the mean of a representative optical trace experiment carried out in triplicates. The resulting shifts of reflected light wavelength (pm) were monitored over time. C) Dose-response of the antagonistic effect of bivalent compound 13 (black) (IC50=15±3 nM) and monovalent 15 (red) (IC50=280±70 nM) on the DMR induced by 100 nM sumanirole. Data are mean±SEM from 3–8 experiments and are presented as percentage of the maximal effect of sumanirole.