| Assay Method Information | |
| | Cannabinoid Receptors Displacement Assay |
| Description: | The highly potent and nonselective CB agonist CP55,940 binds to the same orthosteric active site where known CB agonists are known to bind. In preliminary screening, all 17 synthetic PBD compounds (4a-4q) were subjected to in vitro CB1 and CB2 binding assays at a single concentration of 10 μM. The observed percentage displacement (%) of the radioligand at the CB receptors of these analogs are summarized in Table 2. From the 17 compounds evaluated in the competitive radioligand assay, compounds 4h, 4j-4l, and 4q showed significant displacement (more than 60%). Among them, two structurally distinct PBD analogs (4k and 4q) displayed the greatest [3H]CP-55,940 displacement and selectivity for CB2 over CB1. Therefore, the most promising ligands (4k and 4q) were selected for assessment in full competition curves against CB1 and CB2. The binding assays revealed selective binding affinity of 4k and 4q with Ki values of 146 and 137 nM, respectively, toward CB2 receptors (Table 3). |
| Affinity data for this assay | |
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