Table 2.
Effect of repeated JZL184 administration on CB1 receptor desensitization in mice. Repeated treatment with JZL184 does not produce CB1 receptor desensitization in PFC, NAc, HIPP, and VTA. Data are presented as means ± S.E.M. n = 6 tissue samples per group, run in separate experiments with each individual sample run in triplicate for [35 S] GTPγS binding, and each individual sample run in duplicate for receptor binding.
| Vehicle | JZL184 (24 mg/kg) | |
|---|---|---|
| Prefrontal Cortex | ||
| Bmax (pM) | 2.2 ± 0.2 | 1.8 ± 0.2 |
| Kd (nM) | 1.6 ± 0.5 | 1.3 ± 0.4 |
| Nucleus Accumbens | ||
| Bmax (pM) | 1.6 ± 0.6 | 1.2 ± 0.7 |
| Kd (nM) | 4.3 ± 2.5 | 1.8 ± 0.9 |
| Hippocampus | ||
| Bmax (pM) | 2.2 ± 0.6 | 2.1 ± 0.6 |
| Kd (nM) | 0.95 ± 0.25 | 1.85 ± 1.0 |
| Ventral Tegmental Area | ||
| Bmax (pM) | 0.53 ± 0.16 | 0.7 ± 0.2 |
| Kd (nM) | 0.99 ± 0.35 | 1.7 ± 1.2 |
| Vehicle | JZL184 (24 mg/kg) | |
|---|---|---|
| Prefrontal Cortex | ||
| Emax (% stim.) | 62.8 ± 20.2 | 64.5 ± 24.6 |
| EC50 (nM) | 6.0 ± 1.2 | 7.9 ± 1.9 |
| Nucleus Accumbens | ||
| Emax (% stim.) | 56.3 ± 3.8 | 45.5 ± 6.0 |
| EC50 (nM) | 15.11 ± 3.1 | 22.5 ± 4.5 |
| Hippocampus | ||
| Emax (% stim.) | 61.9 ± 12.4 | 63.0 ± 14.6 |
| EC50 (nM) | 8.5 ± 2.7 | 6.2 ± 0.3 |
| Ventral Tegmental Area | ||
| Emax (% stim.) | 51.54 ± 6.61 | 36.4 ± 10.6 |
| EC50 (nM) | 18.7 ± 8.7 | 19.4 ± 5.6 |