Table 2.
Antagonism of agonist stimulated [35S]-GTPγS binding
|
HEK293-hCB1 membranes |
Rat cerebellar membranes |
HEK293-hCB2 membranes |
|||
|---|---|---|---|---|---|
| Compound | CP55,940 IC50 (nM) | AEA IC50 (nM) | CP55,940 IC50 (nM) | AEA IC50 (nM) | CP55,940 IC50 (μM) |
| PSNCBAM-1 | 74.3±12.7 | 131±66 | 42.1±8.3 | 29.7±10.2 | >10* |
| SR141716A | 28±1.3 | 20±9.4 | 4.7±2.1 | 2.4±1 | 3.6* |
Abbreviations: AEA, arachidonoyl ethanolamide; HEK, human embryonic kidney; PSNCBAM-1, 1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl]urea; SR141716A, N-(piperidin-1-yl)-5-(4-cholrophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide.
Antagonism of agonist-stimulated [35S]-GTPγS binding in HEK293-hCB1 and rat cerebellar membranes by PSNCBAM-1 and SR141716A. [35S]-GTPγS and compounds were mixed with membranes and incubated at 30°C for 60 min. Plates were then filtered and the radioactivity counted. Mean IC50±s.e.m. from three experiments. AM630, a CB2 control antagonist, produced an IC50 value of 0.65 μM.
*
Data from a single experiment.