TABLE 1.
Curve-fit values from CP55,940-stimulated [35S]GTPγS binding and [3H]SR141716A saturation binding
Values represent the mean ± S.E.M. and were derived from nonlinear fitting of the data shown in Fig. 1.
| JZL-184 Dose | CP55,940-Stimulated [35S]GTPγS Binding |
[3H]SR141716A Binding |
||
|---|---|---|---|---|
| Emax | EC50 | Bmax | KD | |
| % Stim. | nM | pmol/mg | nM | |
| Vehicle (mg/kg) | 74.3 ± 8.2 | 6.2 ± 1.0 | 4.84 ± 0.26 | 1.03 ± 0.10 |
| 1.6 | 65.3 ± 10.3 | 7.9 ± 2.0 | 5.07 ± 0.44 | 1.10 ± 0.09 |
| 2.5 | 78.3 ± 7.1 | 5.8 ± 0.7 | N.D. | N.D. |
| 4 | 64.4 ± 5.7 | 8.6 ± 1.7 | 4.55 ± 0.45 | 1.23 ± 0.14 |
| 8 | 49.7 ± 11.2 | 5.8 ± 1.3 | N.D. | N.D. |
| 16 | 41.7 ± 5.1* | 7.6 ± 0.8 | 3.40 ± 0.32* | 1.11 ± 0.14 |
| 40 | 33.9 ± 4.6** | 8.3 ± 1.7 | 3.16 ± 0.29* | 1.17 ± 0.16 |
N.D., not determined; % Stim., % stimulation.
*
P < 0.05; **P < 0.01 versus vehicle-treated (Dunnett’s post-hoc test).