Fig. 4. Characterization of G protein activation of wild type (WT) and mutant CB₂R by synthetic agonists and endocannabinoids.

Dose-response curves for G protein activation of WT and mutants that are located in the CB₂R binding pocket by a LEI-102, b APD371, c HU308, and d CP55,940. e–j Dose response curves for G protein activation of WT and mutants that are proposed to be involved in ligand entry of CB₂R via either the ECL2 or membrane access by e LEI-102, f APD371, g HU308, h CP55,940, i AEA and j 2-AG. a–j The maximum activation level of WT CB₂R was set to 100% while the basal levels were set to 0%. Data are presented as mean ± SEM of at least three individual experiments performed in duplicate (specific n values are given in Supplementary Table 6). Source data are provided as a Source Data file.