Cannabinoids

8 R.G. Pertwee

Table 2.Examples ofKivalues of certain cannabinoid CB 1 and/or CB 2 receptor agonists for the in vitro

displacement of [^3 H]CP55940, [^3 H]HU243 or [^3 H]BAY-38-7271 from CB 1 -andCB 2 -specific binding sites

(continuedonnextpage)

Agonist CB 1 CB 2 Reference

Kivalue (nM) Kivalue (nM)

• Abood, M.E. (Addresses stated at the beginning of the respective chapters)


• Bátkai, S.


• Bisogno, T.


• Cabral, G.A.


• Christie, M.J.


• Coutts, A.A.


• Davies, S.N.


• de Miguel, R.


• De Petrocellis, L.


• Di Marzo, V.


• Egertová, M.


• Elphick, M.R.


• Fernández-Ruiz, J.


• Gómez, M.


• Gatley, S.J.


• Glaser, S.T.


• González, S.


• Guzmán, M.


• Hillard, C.J.


• Ho, W.-S.V.


• Hohmann, A.G.


• Howlett, A.C.


• Huestis, M.A.


• Izzo, A.A.


• Karsak, M.
  
  
  • Kunos, G.
  
  
  • Li, C.
  
  
  • Lichtman, A.H.
  
  
  • Lindsey, K.P.
  
  
  • Maccarrone, M.
  
  
  • Mackie, K.
  
  
  • Makriyannis, A.
  
  
  • Martin, B.R.
  
  
  • Nikas, S.P.
  
  
  • Pacher, P.
  
  
  • Pertwee, R.G.
  
  
  • Ramos, J.A.
  
  
  • Reggio, P.H.
  
  
  • Riedel, G.
  
  
  • Robson, P.
  
  
  • Schlicker, E.
  
  
  • Staab, A.
  
  
  • Szabo, B.
  
  
  • Thakur, G.A.
  
  
  • Valverde, O.
  
  
  • Vaughan, C.W.
  
  
  • Walker, J.M.
  
  
  • Wenger, T.
  
  
  • Zimmer, A.
  
  
  
  


• HEP (2005) 168:1–


• ©cSpringer-Verlag


• 1Introduction.................................... [email protected]


• 2 Bioassays for Characterizing CB 1 and CB 2 Receptor Ligands..........


• 2.1 InVitroBindingAssays..............................


• 2.2 In Vitro Functional Bioassays


• 2.2.1AssaysUsingWholeCellsorCellMembranes


• 2.2.2IsolatedNerve–SmoothMusclePreparations


• 2.3 In Vivo Bioassays


• 2.4 CannabinoidReceptorKnockoutMice......................


• 3CB 1 and CB 2 Cannabinoid Receptor Ligands


• 3.1 CannabinoidReceptorAgonists


• 3.2 Cannabinoid CB 1 and CB 2 ReceptorAntagonists


• 3.2.1 Selective CB 1 ReceptorAntagonists


• 3.2.2 Selective CB 2 ReceptorAntagonists........................


• 3.3 InverseAgonismatCannabinoidReceptors


• 3.4 NeutralAntagonismatCannabinoidReceptors


• 4 Other Pharmacological Targets for Cannabinoids in Mammalian Tissues...


• 4.1 Receptors......................................


• 4.1.1VanilloidReceptors


• 4.1.2 CB 1 ReceptorSubtypes


• 4.1.3 CB 2 -LikeReceptors


• 4.1.4 Neuronal Non-CB 1 ,Non-CB 2 ,Non-TRPV1Receptors


• 4.1.5ReceptorsforAbnormal-Cannabidiol


• 4.2 AllostericSites...................................


• 4.3 Some CB 1 -andCB 2 -Independent Actions of Cannabidiol, HU-
  
  
  • andOtherPhenol-ContainingCannabinoids
  
  
  
  


• 4.3.1NeuroprotectiveActions


• 4.3.2OtherActionsofCannabidiol...........................


• 5CB 1 Receptor Oligomerization


• 6FutureDirections.................................


• References


• ACEA 1.4a,b >2,000a,b Hillard et al. CB 1 -selective agonists in order of decreasing CB 1 /CB 2 selectivity
  
  
  • 5.29a,b 195 c Lin et al.
  
  
  
  


• O-1812 3.4b 3,870b Di Marzo et al.


• ACPA 2.2a,b 715 a,b Hillard et al.


• 2-Arachidonyl glyceryl ether 21.2b >3,000d Hanus et al.


• R-(+)-methanandamide 17.9a,b 868 c Lin et al.
  
  
  • 20 a,b 815 c Khanolkar et al.
  
  
  • 28.3b 868 c Goutopoulos et al.
  
  
  
  


• Anandamide 61 a,b 1,930c Lin et al. Agonists without any marked CB 1 or CB 2 selectivity
  
  
  • 78.2a,b 1,926c Khanolkar et al.
  
  
  • 89 a 371 a Showalter et al.
  
  
  • 543 1,940 Felder et al.
    
    
    • 71.7a,b 279 a,b Hillard et al.
    
    
    
    
  
  
  • 252 e,d 581 e,d Mechoulam et al.
  
  
  
  


• BAY 38-7271 1.85f 5.96f Mauler et al.


• 2-Arachidonoyl glycerol 472 e,d 1,400e,d Mechoulam et al.
  
  
  • 58.3e,d 145 e,d Ben-Shabat et al.
  
  
  
  


• O-1057 4.4 11.2 Pertwee et al.


• HU-210 0.0608 0.524 Felder et al.
  
  
  • 0.1e,b 0.17e Rhee et al.
  
  
  • 0.73 0.22 Showalter et al.
  
  
  • 3.72 2.55 Felder et al. CP55940 5 1.8 Ross et al. 1999a
  
  
  • 1.37b 1.37b Rinaldi-Carmona et al.
  
  
  • 0.58 0.69 Showalter et al.
  
  
  • 0.50a,b 2.80a,b Hillard et al.
  
  
  
  


• ∆^9 -THC 53.3 75.3 Felder et al.
  
  
  • 39.5e,b 40 e Bayewitch et al.
  
  
  • 40.7 36.4 Showalter et al.
  
  
  • 80.3e,b 32.2e Rhee et al.
  
  
  • 35.3b 3.9b Rinaldi-Carmona et al.
    
    
    • 5.05 3.13 Iwamura et al.
    
    
    
    
  
  
  
  


• Nabilone 1.84 2.19 Gareau et al.


• ∆^8 -THC 47.6b 39.3c Busch-Petersen et al.
  
  
  • 44 b 44 Huffman et al.
  
  
  
  


• Cannabinol 211.2e,b 126.4e Rhee et al.
  
  
  • 308 96.3 Showalter et al.
  
  
  • 1,130 301 Felder et al.
  
  
  
  


• CP56667 61.7 23.6 Showalter et al.


• R-(+)-WIN55212 9.94b 16.2b Rinaldi-Carmona et al.
  
  
  • 4.4a,b 1.2a,b Hillard et al.