Fig. 2. (E)-BCP and (Z)-BCP displace [3H]CP-55,940 from hCB2 receptors expressed in HEK293 cells. (A) Sigmoidal displacement curves (R2 = 0.93 for (E)-BCP and 0.98 for (Z)-BCP) show overall displacement (71% and 84%, respectively) with Ki values of 155 and 485 (more ...) |
Fig. 3. Model of the putative interaction of (E)-BCP with the CB2 receptor determined by Surflex–Dock and MD/MM calculations. (E)-BCP is located in the hydrophobic region of the amphipathic CB2 receptor binding pocket where it closely interacts with hydrophobic (more ...) |
Fig. 4. G protein triggered effects of (E)-BCP upon CB2 receptor binding. (A) The high-affinity CB ligand WIN55,212–2 and (E)-BCP dose-dependently inhibit forskolin-stimulated cAMP production in CB2 receptor-transfected CHO-K1 cells. Data are mean values (more ...) |
Fig. 5. Anti-inflammatory effects of (E)-BCP in vitro and in vivo. (A) (E)-BCP (1 h incubation before stimulation) inhibits LPS-stimulated (313 ng/ml) IL-1β and TNF-α protein expression in human peripheral whole blood (determined after 18 h). (more ...) |