TABLE 3

Effect of Org 27569 and PSNCBAM-1 on CP55940 and WIN55212-2 in the PathHunter β-arrestin assay

Increase in luminescence (relative light units, RLU) are presented as a percentage of the maximal CP55940 stimulation.

AgonistVehicle/ModulatorpEC50aEmaxb
(%) (95% CI)% Inhibition
±SEM
CP55940DMSO7.9 ± 0.0699.5 (95–104)
Org 27569 (1 nM)8.1 ± 0.166.7 (60–73)32.9 ± 5.2
Org 27569 (10 nM)8.0 ± 0.115.3 (13.5–17)84.3 ± 1.1
Org 27569 (100 nM)98.9 ± 0.2
WIN55212DMSO6.9 ± 0.183.5 (70–97)
Org 27569 (1 nM)7.1 ± 0.0776.4 (70–83)8.5 ± 2.7
Org 27569 (10 nM)7.0 ± 0.137.9 (33–43)54.2 ± 0.7
Org 27569 (100 nM)7.3 ± 0.73.4 (0.3–7)94.6 ± 1.7
AnandamideDMSO7.4 ± 0.2100.0 (83– 117)
Org 27569 (1 nM)7.0 ± 0.1110.9 (96–126)−10.92 ± 0.6
Org 27569 (10 nM)6.0 ± 0.680.2 ± 3.3
Org 27569 (100 nM)8.8 ± 1.6135 ± 1.8
CP55940DMSO7.9 ± 0.06102.3 (98–107)
PSNCBAM (1 nM)7.9 ± 0.176.8 (70–83)24.5 ± 4.3
PSNCBAM (10 nM)8.6 ± 0.318.3 (15–21)82.1 ± 1.2
PSNCBAM (100 nM)96.9 ± 2.1
WIN55212DMSO7.6 ± 0.1101.3 (90–112)
PSNCBAM (1 nM)7.5 ± 0.190.2 (82–98)10.0 ± 6.6
PSNCBAM (10 nM)7.8 ± 0.246.1 (39–53)53.8 ± 3.7
PSNCBAM (100 nM)8.6 ± 1.58.9 (5–13)90.5 ± 2.6
  • 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.