Some Ki values of cannabinoid CB1/CB2 receptor ligands for the in vitro displacement of a tritiated compounda from specific binding sites on rat, mouse, or human CB1 and CB2 receptors

Unless otherwise indicated in the Reference column, see Pertwee, 2005a for references. Structures of the compounds listed are shown in Figs. 1 to 5.

Cannabinoid Receptor LigandKiReference
Section II.C.1
    (−)-Δ9-THC5.05–80.33.13–75.3See Pertwee, 2008a for references
    2-AG58.3, 472145, 1400
Section II.C.2
    Agonists with higher CB1 than CB2 affinity
        ACEA1.4, 5.29195, >2000
        Noladin ether21.2>3000
    Agonists with higher CB2 than CB1 affinity
Section II.C.3
    Rimonabant (SR141716A)1.8–12.3514–13,200
    Taranabant0.13, 0.27170, 310Fong et al., 2007
    NESS 03270.0003521
    O-20502.5, 1.71.5Martin et al., 2002; A. Thomas and R. G. Pertwee, unpublished data
Section II.C.4
Section II.C.5
    Ajulemic acid5.7, 32.356.1, 170.5Dyson et al., 2005; see also Pertwee, 2005a, for references
    Cannabinol120–113096–301See Pertwee, 2008 for references
    Cannabigerol812600Cascio et al., 2010
    Cannabidiol4350–>10,0002399–>10,000See Pertwee, 2008 for references
    N-Arachidonoyl dopamine25012,000Bisogno et al., 2000
    Virodhamine912N.D.Steffens et al., 2005
  • N.D., no data.

  • a Usually [3H]CP55940, but sometimes [3H]SR141716A, [3H]R-(+)-WIN55212, or HU-243 (i.e., [3H]HU-210).