Affinities of ACPA and ACEA for CB1 and CB2 receptors
| Ligand | KD/I, CB1 Receptor1-a | KD/I, CB2 Receptor1-b | Potency Ratio (CB2/CB1) |
|---|---|---|---|
| nM | |||
| CP55940 | 0.5 ± 0.1 (4) | 2.8 ± 0.4 (4) | 5.6 |
| Win 55212-2 | 4.4 ± 1.3 (3)1-c | 1.2 ± 0.25 (3) | 0.27 |
| AEA | 71.7 ± 7.3 (4)1-d | 279 ± 58 (3)1-d | 3.9 |
| ACPA | 2.2 ± 0.4 (4) | 715 ± 14 (2)1-d | 325 |
| ACEA | 1.4 ± 0.3 (4) | >2000 (2) | >1400 |
↵1-a Affinities for the CB1 receptor were determined either from saturation isotherms (CP55940) or from competition isotherms using [3H]CP55940 in rat cerebellar membranes. Membranes (10 μg of protein/incubate) were incubated with 0.5 to 1 nM [3H]CP55940 for 60 min at room temperature.
↵1-b Affinities for the CB2 receptor were determined either from saturation isotherms (CP55940) or from competition isotherms using [3H]CP55940 in rat spleen membranes. Membranes (10 μg of protein/incubate) were incubated with 0.5 to 1 nM [3H]CP55940 for 60 min at 30°C.
↵1-c Data are shown as mean ± S.E.M. Numbers in parentheses, number of replicate experiments.
↵1-d Significantly different from KD for CP55940 at p < .05 using Tukey’s test.