Effect of CB1 receptor agonists on basal cAMP accumulation in CHO cells expressing the hCB1 cannabinoid receptor
| Ligand | Receptor binding affinity | Stimulation of basal cAMP accumulation | |
|---|---|---|---|
| pKi | pEC50 | % basal accumulation | |
| Anandamide | 6.2 ± 0.1 | 5.1 ± 0.1 | 627 ± 123 (141%)2-a |
| CP-55,940 | 8.6 ± 0.2 | 6.0 ± 0.3 | 374 ± 121 (84%) |
| HU-210 | 9.2 ± 0.3 | 6.9 ± 0.1 | 193 ± 13 (43%) |
| THC | 7.5 ± 0.2 | 6.6 ± 0.4 | 22.3 ± 2.5 (5%)2-a |
| WIN-55212-2 | 7.5 ± 0.4 | 6.5 ± 0.3 | 445 ± 66 (100%) |
Values are the mean and S.E. for values obtained from at least six concentration-response curves. Numbers in parentheses are activity values normalized to those of WIN-55212-2.
↵2-a An SR141716A-insensitive component of the response was subtracted so as to derive an estimate of CB1 receptor-mediated activity. pEC50 and pKi values are the negative log of the molar EC50 and Kivalues, respectively.