Table 1 Radioligand competitive binding assays and GTPγ[ 35 S] functional activity
From: Analgesic effect of a mixed T-type channel inhibitor/CB2 receptor agonist
Ligand | Mean Ki | GTPγ[35S] functional assays | ||||
|---|---|---|---|---|---|---|
Rat CB1(nM) | Human CB2 (nM) | Human CB1 | Human CB2 | |||
EC50(μM) | Emax(%) | EC50(μM) | % activation average at 1 μM | |||
NMP181 | 2238 ± 515 | 123 ± 28 | NA | ND | >1 | 24% |