Table 1. Central and peripheral CB1 receptor human isoforms differ in affinity for cannabinoid receptor inverse agonists.
Ligand | Receptor Isoform |
|
---|---|---|
CB1 (nM) | CB1b (nM) | |
Rimonabant | 2.30 ± 0.69 | 7.65 ± 3.79 |
(R2 = 0.973) | (R2 = 0.984) | |
JD-5037 | 8.16 ± 1.51 | 0.24 ± 0.12 |
(R2 = 0.994) | (R2 = 0.824) |
The Ki of rimonabant and JD-5037 for the CB1 and CB1b receptors as determined on the CHO-CB1 and CHO-CB1b open tubular columns, respectively, using frontal affinity chromatographic techniques.