DIM is a CB2 partial agonist. Response of the human
CB2 receptor to the test molecules in the β-arrestin assay
(A), radioligand competition binding assay (B), GTPγS
binding assay (C), and cAMP assay (D). ○, CP55940;
□, DIM; ▴, 2-AG; ▾, anandamide; and ♦, arachidonic acid.
A, HEK293-BAEA parental cells were transiently transfected with
CB2 and then assayed the next day. B and C,
membrane preparations from a CB2-CHO stable cell line were used.
D, CB2-CHO stable cell line was seeded and 16 h later
stimulated with test compounds along with 60 μm of for skolin.
After 30 min of stimulation, cells were lysed, and cAMP level was measured
using cAMP-HTRF HighRange kit. The y axis plots the FRET ratio which
is inversely proportional to the cellular cAMP concentration.