Table 3.
Inhibition constants (Ki) and selectivity of test compounds for CB1- and CB2-receptors in the order of their selectivity for CB2-receptors. Ki values are expressed as the mean ± SEM of n = 3 independent experiments.
| Test compound | Ki CB1 (nmol/L) | Ki CB2 (nmol/L) | Selectivity CB2/CB1 |
|---|---|---|---|
| HC (5) | 2,500 ± 900 | 67 ± 4 | 37.3 |
| 2-HECBDV (7) | 5,649.3 ± 3,896.2 | 168.2 ± 39.4 | 33.6 |
| NMSC (6) | 270 ± 40 | 12 ± 1 | 22.5 |
| 2-HEC (1) | 3,923 ± 1,547 | 374.5 ± 47.7 | 10.5 |
| 2-HPC (2 | 538.2 ± 53.9 | 66.7 ± 13.1 | 8.1 |
| GCBD (3) | 2,174 ± 1,149 | 277.1 ± 78.7 | 7.8 |
| CHCBDV (8) | 13.2 ± 0.9 | 4.62 ± 0.5 | 2.9 |
| CHC (4) | 870 ± 100 | 510 ± 290 | 1.7 |
| HCBDV (9) | 8.3 ± 0.69 | 9.9 ± 2.5 | 0.8 |
| WIN55,212-2 (reference compound) | 28.8 ± 41 | 3.7 ± 1 | - |
CB, cannabinoid; CHC, cyclohexyl cannabidiolate; CHCBDV, cyclohexyl cannabidivarinolate; GCBD, 2,3-dihydroxypropyl cannabidiolate; HC, n-hexyl-cannabidiolate; HCBDV, n-hexyl cannabidivarinolate; NMSC, 2-(methylsulfonamido)ethyl cannabidiolate; 2-HEC, 2-hydroxyethyl cannabidiolate; 2-HECBDV, 2-hydroxyethyl cannabidivarinolate; 2-HPC, 2-hydroxypentyl cannabidiolate.