Figure 8

Modulation of CB₂ receptor activity by 27a and 34a. (A) [³⁵S]GTPγS binding assay performed in CHO-K1 membranes containing hCB₂ receptors, in the presence of different concentrations of 27a and 34a. The CB₂ inverse agonist AM630 is reported as positive control (red line). Experiments were performed in the presence (dotted line) and in the absence (solid line) of constitutive activity of the receptors. (B) Inhibition of forskolin-induced cAMP formation by 27a and 34a in CHO-hCB₂ cells transfected with pGloSensorTM 22-F plasmid. The experiments were performed in the presence (dotted line) and in the absence (solid line) of constitutive activity. (C) β-arrestin recruitment induced by increasing concentrations of 27a and 34a, measured in PathHunter® β-arrestin cells (CHO-K1-HOMSA-CNR2). ^* P < 0.05, ^** P < 0.01 27a vs. 2-AG (Figure 8A); ^* P < 0.05, ^** P < 0.01 27a and 34a vs. CP55, 940 (Figure 8C).