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. Author manuscript; available in PMC: 2014 Nov 15.
Published in final edited form as: Biochem Biophys Res Commun. 2013 Oct 19;441(2):10.1016/j.bbrc.2013.10.057. doi: 10.1016/j.bbrc.2013.10.057

Figure 2.

Figure 2

Tam and 4OH-Tam act as inverse agonists at human CB1 and CB2 receptors to regulate the intracellular effector AC activity in intact cells. A) Modulation of forskolin-stimulated AC-activity was evaluated by incubating intact CHO-hCB1, CHO-hCB2 or CHO-hMOR cells with a receptor saturating concentration of CP-55,950 (1 μM), morphine (1 μM), Tam (10 μM) or 4OH-Tam (10 μM) as described in the Materials and Methods. AC-inhibition produced by the hMOR agonist morphine was evaluated as a positive control in CHO-hMOR cells. The mean ± SEM of basal cAMP levels in the presence of test compounds is presented. B) Increasing concentrations of 4OH-Tam (100 nM - 10 μ M) modulated AC-activity in a concentration-dependent manner in CHO-hCB2 cells. C) Co-incubation with 4OH-Tam produced a parallel shift-to-the-right in the ability of the CB1/CB2 agonist WIN-55,212-2 to inhibit AC-activity in CHO-hCB1 cells, indicative of CB1 receptor antagonism. *Significantly different from basal cAMP levels (P<0.05; One sample t-test).