TABLE 1

Summary of the ligand-directed signaling of CB1

LigandGiGoGsGq/11References
Classic
    HU-210++++++N.E.Bonhaus et al., 1998; Glass and Northup, 1999; Lauckner et al.,2005
    THC+++N.E.
Nonclassic
    CP 55,940++a×+N.E.Bonhaus et al., 1998; Glass and Northup, 1999; Lauckner et al.,2005;McIntosh et al., 2007; Georgieva et al., 2008
Eicosanoid
    AEA++a++N.E.bBonhaus et al., 1998; Glass and Northup, 1999; Mukhopadhyay et al.,2005;McIntosh et al., 2007
Aminoalkylindole
    WIN++++++Bonhaus et al., 1998; Glass and Northup, 1999; Lauckner et al.,2005; Mukhopadhyay et al., 2005; McIntosh et al., 2007
Diarylpyrazole
    SR 141716×N.E.cAbadji et al., 1999; Lauckner et al., 2005; Mukhopadhyay et al.,2005
  • + agonist effect; −, inverse agonist effect; N.E., no agonist or inverse effect (compounds probably act as neutral antagonists); ×, has not been directly tested for Go-specific coupling.

  • a Acts as full Gi agonist but has reduced affinity or efficacy to specific Gi subtypes.

  • b Data obtained with MAEA instead of AEA.

  • c SR 141716 acted as an antagonist to the Gq/11 pathway but was not tested as an inverse agonist.