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. 2018 Jun 21;9:645. doi: 10.3389/fphar.2018.00645

FIGURE 1.

FIGURE 1

RO5263397 activates TAAR1 and increases cAMP-BRET signal. (A,B) HEK293 cells transfected with mTAAR1 (left panel) or hTAAR1 (right panel) were treated with increasing concentrations of RO5263397. cAMP is detected using a BRET biosensor where a decrease of a BRET ratio indicates an increase of cAMP levels. RO5263397 is added at the time 0 and then the plate was read for 20 min. We used as TAAR1 standard agonist β-phenyethylamine (PEA) at 10 μM. (C,D) Concentration response experiment. The data were represented using the log of the concentration and the curves were fitted using a non-linear regression in order to calculate the EC50. BRET signal was measured 15 min after the addition of RO5263397. (E) HEK293 cells transfected with mTAAR1 were pretreated with the TAAR1 antagonist EPPTB at 1 μM (or vehicle) and after 5 min with the agonist RO5263397 at 0.1 μM. To evaluate the specificity of EPPTB it was evaluated in combination with forskolin at 20 μM (F). These panels are representative of three independent experiments.