TABLE 2

Effect of Org 27569 on CP55940 and WIN55212 in [35S]GTPγS binding, cAMP, and pERK assay in hCB1R cells

AgonistVehicle/ModulatorpEC50aEmaxb
(%) (95% CI)% Inhibition
SEM
[35S]GTPγS Binding (% Stimulation above Basal)
CP55940DMSO7.3 ± 0.264.7 (57–72)
Org 27569 (10 nM)6.2 ± 0.476.2 (48–105)13.8 ± 31
Org 27569 (100 nM)6.9 ± 0.635.2 (19–52)46.3 ± 18
Org 27569 (1 μM)94.4 ± 6.0
WIN55212DMSO6.7 ± 0.270.4 (62–79)
Org 27569 (100 nM)6.5 ± 0.367.7 (49–87)1.2 ± 16
Org 27569 (1 μM)6.9 ± 0.433.1 (20–47)43.4 ± 18
cAMP Assay (% Inhibition of Forskolin Stimulation)
CP55940DMSO8.1 ± 0.286.6 (75–98)
Org 27569 (10 nM)7.6 ± 0.455.0 (37–73)30.3 ± 12.0
Org 27569 (100 nM)155 ± 9.6
WIN55212DMSO7.1 ± 0.278.6 (64–93)
Org 27569 (100 nM)7.0 ± 0.264.6 (51–78)22.3 ± 4.9
Org 27569 (1 μM)6.9 ± 0.341.1 (23–59)37.0 ± 5.9
ERK1/2 Phosphorylation (% Increase above Basal)
CP55940DMSO7.6 ± 0.1450.0 (44–56)
Org 27569 (100 nM)8.0 ± 0.1672.0 (64–80)
Org 27569 (1 μM)7.8 ± 0.2365.0 (58 -72)
WIN55212DMSO6.6 ± 0.5340.2 (27–54)
Org 27569 (100 nM)7.0 ± 0.6750.9 (35–66)
Org 27569 (1 μM)6.6 ± 0.4837.0 (24–51)
  • a Negative logarithm of the agonist EC50 value, determined using nonlinear regression analysis. Values represent the mean ± standard error of the mean (S.E.M.) of four to six experiments.

  • b Maximal agonist effect, determined using nonlinear regression analysis. Values represent the mean with 95% CI of four to six experiments.

  • Significantly different (nonoverlapping confidence limits) from the DMSO vehicle.