Figure 3

Potentiation of hA _2a R-coupled Gα activation. (A) AEA061 dose-dependently increases agonist-mediated GTPγ³⁵S binding to membranes. CHO-hA_2aR membranes were incubated with ADA, CGS 21680 and varying concentrations of AEA061. Each data point is the mean ± SEM of replicates of 5 determinations of a representative experiment. (B) AEA061 potentiates A_2aR-mediated Gα activation. CHO-hA_2aR membranes were incubated with ADA, AEA061 and varying concentrations of CGS 21680. Each data point is the mean ± SEM of replicates of 6 determinations of a representative experiment. EC₅₀ values with 95% confidence intervals in parenthesis were as follows: control = 3.7 nM (2.195 - 6.294); AEA061 (10 μM) = 0.99 nM (0.7810 to 1.260).