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Table 2 Radioligand competitive binding assays and GTPγ[35S] functional activity.

From: Functional characterization and analgesic effects of mixed cannabinoid receptor/T-type channel ligands

  Mean Ki (nM) GTPγ[35S] functional assays
Ligand Rat CB1 Human CB2 Human CB1 Human CB2
    EC 50 (nM) E max (%) EC 50 (nM) E max (%)
NMP4 12.8 ± 1.8 7.5 ± 0.7 118.3 ± 4 30.4 9.8 ± 0.3 -76.4
NMP7 ND ND 96.9 ± 11.9 73.6 10.5 ± 1.8 30.8
NMP139 NA 3594 ± 424 ND ND ND ND
NMP140 1252 ± 290 2874 ± 515 ND ND ND ND
NMP141 906.2 ± 211.3 480.7 ± 52.9 NA NA 112.4 ± 3.3 51.9
NMP144 1143 ± 264 706.2 ± 110.1 NA NA 35.7 ± 13.9 -48.1
  1. ND: not determined; NA: not active at 1 μM