Table 1.
Binding and G-protein-stimulation properties of ABK5 derivatives.
| CP55,940 | GTPγS | ||
|---|---|---|---|
| Ki (nM) a | EC50 (nM) b | ||
| Compound | CB2 | CB1 | CB2 |
| ABK5-1 | 28 ± 5 | N.B. c | 11 ± 14 |
| ABK5-2 | 69 ± 19 | N.B. c | 24 ± 25 |
| ABK5-5 | N.D. d | N.D. d | N.D. d |
| ABK5-6 | 14 ± 2 | >1000 | 10 ± 5 |
| ABK5 e | 16 ± 14 | N.B. c | 4 ± 3 |
a Ki values were determined from competition binding assays using [3H]CP55,940. b EC50 values were determined from stimulation of [35S]GTPγS binding. c N.B.: No specific binding detected up to 10 μM of test compounds. d N.D.: Ki or EC50 value was not determined. e Parameters of ABK5 were determined previously and are shown for comparison [23].