Figure 3.

Antagonism of CP55,940-dependent β-arrestin recruitment (A) and cAMP inhibition (B) and by CB₁R analogues of 2 in vitro. Effects on CP55,940-induced β-arrestin recruitment and cAMP inhibition in the presence of various analogues of 2. (A) CHO-K1 PathHunter hCB₁ cells were pretreated with allosteric modulators (0–10 μM) for 30 min followed by treatment with CP55,940 for 90 min. β-Arrestin recruitment was quantified using the PathHunter assay. (B) CHO-K1 cAMP HitHunter hCB₁ cells were pretreated with allosteric modulators (0–10 μM) for 30 min followed by treatment with CP55,940 for 30 min. cAMP inhibition was quantified using the HitHunter assay. Data are presented as % inhibition compared to maximal CP55,940 effect ± SEM from two independent replicates per assay. Derived data are presented in Table 2.