Table 1.
The mean apparent KB values for antagonism of CP55940-induced [35S]GTPγS binding to membranes and the Ki values for the displacement of [3H]CP55940 from membranes
| Antagonist | Membrane preparation | Mean apparent KB (95% CI) | n | Ki for displacement of [3H]CP55940 (95% CI) | n |
|---|---|---|---|---|---|
| Rimonabant (10 nM) | Mouse brain | 0.09 nM (0.02 and 0.41 nM) | 4a | 2.2 nM (1.1 and 4.2 nM) | 6 |
| Cannabidiol (1 μM) | 79 nM (48 and 128 nM) | 5 | 4.9 μM (2.1 and 11.3 μM) | 5–12b | |
| O-2654 (1 μM) | 51 nM (34 and 74 nM) | 5 | 114 nM (96 and 137 nM) | 5–11b | |
| SR144528 (100 nM) | hCB2-CHO cell | 0.49 nM (0.26 and 0.85 nM) | 6a | 7.5 nM (5.8 and 9.8 nM) | 6–8 |
| Cannabidiol (1 μM) | 65 nM (16 and 228 nM) | 5 | 4.2 μM (2.9 and 6.2 μM) | 6–8 | |
| O-2654 (1 μM) | 30 nM (12 and 59 nM) | 5 | 48 nM (30 and 76 nM) | 6–8 |
Abbreviations: CI, confidence intervals; CP55940, (–)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol; hCB2-CHO, Chinese hamster ovary cells stably transfected with human CB2 receptors; SR144528, N-[(1S)-endo-1,3,3-trimethyl bicyclo [2.2.1] heptan-2-yl]-5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-pyrazole-3-carboxamide.
a
Data previously published in Thomas et al. (2005).
b
Data previously published in Thomas et al. (2004).