| Assay Method Information | |
| | Binding Affinity Assay |
| Description: | The ability of some of the ligands to bind to the CB1/CB2 receptors with a tight/irreversible binding mode was determined by measuring reductions in the binding for the radioligand [3H]CP-55,940 when the receptor preparation was pretreated with the tight/irreversible ligand, and comparing it to the untreated sample as disclosed in Ogava et al.J. Med. Chem. (2015) 58, 3104. Reductions in the specific binding (Bmax) of [3H]CP-55,940 after ligand pretreatment indicate ability of the ligand to tight/irreversibly bind to the receptor. As detailed in Ogava et al.J Med. Chem. (2015) 58, 3104, the experiment was conducted by pretreating the sample with a concentration equal to 10-fold the compound's Ki value for the receptor in question and subsequently measuring the decrease of Bmax obtained from a saturation curve using [3H]CP-55,940. |
| Affinity data for this assay | |
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