Potency and efficacy of ACPA and ACEA to increase [35S]GTPγS binding in rat cerebellar membranes3-a
| Ligand | EC50 | Emax |
|---|---|---|
| nM | % control | |
| CP55940 (4) | 31 ± 5 | 200 ± 7 |
| Win 55212-2 (10) | 120 ± 28 | 217 ± 8 |
| AEA (8) | 276 ± 533-b | 166 ± 63-c |
| ACPA (3) | 37 ± 8 | 187 ± 17 |
| ACEA (3) | 51 ± 6 | 201 ± 14 |
↵3-a Cerebellar membranes (5 μg/incubate) were incubated with 0.65 nM [35S]GTPγS for 30 min at 37°C. Control [35S]GTPγS binding was determined in the presence of DMSO vehicle (final concentration of DMSO, 0.4%). DMSO had no effect on [35S]GTPγS binding at this concentration. Phenylmethylsulfonyl fluoride (0.15 mM) was included in the incubates when the arachidonyl amides were used. EC50 andEmax values were determined in three separate experiments using nonlinear regression. Data shown are mean values ± S.E.M.
↵3-b Significantly different from CP55940 at p < .05.
↵3-c Significantly different from Win 552112-2 atp < .05.