Table 1.
Comparison of CELT-335 affinity for CB1 and CB2 receptors measured by competition radioligand binding assay (Ki) and saturation Tag-lite® binding assay (Kd).
| pKi 1 | pKd 2 | |||
|---|---|---|---|---|
| CB1 3 | CB2 4 | CB1 5 | CB2 6 | |
| CELT-335 | 7.34 ± 0.11 | 8.13 ± 0.09 | 7.37 ± 0.06 | 7.62 ± 0.04 |
1 Competition radioligand binding assay. 2 Saturation assay by Tag-lite® binding assay. 3 Displacement of specific [3H]-CP55940 binding in human HEK-CB1 cells expressed as Ki ± SEM in nM (n = 3) or percentage displacement of specific binding at a concentration of 1 μM (n = 2). 4 Displacement of specific [3H]-CP55940 binding in human HEK-CB2 cells expressed as pKi ± SEM in nM (n = 3) or percentage displacement of specific binding at a concentration of 1 μM (n = 2). 5 pKd calculated through saturation of CELT-335 in human HEK-293T cells transiently expressing Tb-labeled SNAP-CB1R. 6 Kd calculated through saturation of CELT-335 in human HEK-293T cells transiently expressing Tb-labeled SNAP-CB2R.