Table 1.
HU-910 activates CB2 receptors in vitro
Competition binding assay | cAMP assay | [35S]GTPγS | ||||||
---|---|---|---|---|---|---|---|---|
CB2 receptor | CB1 receptor | CB2 receptor | CB1 receptor | CB2 receptor | ||||
Drug | Ki (nM) | Ki (µM) | IC50 (nM) | Emax (%) | IC50 (µM) | Emax | EC50 (nM) | Emax (%) |
HU-910 | 6 | 1.37 | 162 | 105 ± 12 | ND | – | 26.4 | 121 ± 7 |
HU-308 | 14 | ND | 117 | 100 ± 0 | ND | – | 18.3 | 100 ± 0 |
Data shown are IC50 values. Emax values were calculated as a percentage of the maximal response detected in parallel cAMP assays with HU-308. Data are displayed as the mean ± SEM. ND, no detectable inhibition of cAMP or displacement of radioactive binding up to 10 µM.