TABLE 1.
Effect of Org 27569 and PSNCBAM-1 on CP55940- and WIN55212-2-stimulated [35S]GTPγS binding in mouse brain membranes
Data are mean ±S.E.M. or with 95% CI.
| Agonist | Vehicle/Modulator | pEC50 a | Emax b (95% CI) | % Inhibition ±SEM |
|---|---|---|---|---|
| % | ||||
| CP55940 | DMSO | 8.2 ± 0.1 | 62.6 (57–69) | |
| Org 27569 (10 nM) | 7.9 ± 0.3 | 43.5 (31–56)† | 33.9 ± 6.7 | |
| Org 27569 (100 nM) | 8.6 ± 0.4 | 17.98 (12–24)† | 71.8 ± 7.0 | |
| Org 27569 (1 μM) | — | — | 95.3 ± 6.6 | |
| WIN55212 | DMSO | 7.8 ± 0.09 | 98.9 (90–107) | |
| Org 27569 (10 nM) | 7.7 ± 0.2 | 83.1 (68–98) | 13.9 ± 8.4 | |
| Org 27569 (100 nM) | 8.0 ± 0.2 | 90.0 (75–105) | 8.7 ± 13.3 | |
| Org 27569 (1 μM) | 8.4 ± 0.3 | 35.9 (27–45)† | 63.6 ± 4.2 | |
| Anandamide | DMSO | 6.7 ± 0.1 | 61.4 (55–68) | |
| Org 27569 (10 nM) | 6.7 ± 0.4 | 56.6 (33–80) | 1.1 ± 12.5 | |
| Org 27569 (100 nM) | 6.4 ± 0.2 | 39.0 (30–48)† | 38.1 ± 3.8 | |
| Org 27569 (1 μM) | 7.6 ± 0.3 | 17.2 (13–22)† | 71.9 ± 3.4 | |
| CP55940 | DMSO | 7.0 ± 0.2 | 53.7 (47–60) | |
| PSN (10 nM) | 6.5 ± 0.2 | 48.7 (39–58) | 7.1 ± 12.7 | |
| PSN (100 nM) | 6.6 ± 0.4 | 32.6 (24–41)† | 41.8 ± 9.6 | |
| PSN (1 μM) | 6.0 ± 0.5 | 15.6 (6–25)† | 72.8 ± 8.4 | |
| WIN55212 | DMSO | 7.8 ± 0.1 | 75.9 (68–84) | |
| PSN (10 nM) | 7.2 ± 0.3 | 78.4 (55–102) | 0.4 ± 15.0 | |
| PSN (100 nM) | 7.1 ± 0.1 | 66.3 (58–74) | 11.0 ± 3.4 | |
| PSN (1 μM) | 6.8 ± 0.4 | 25.9 (13–39)† | 65.0 ± 10.7 |
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 control.