Cannabinoids Biology: The Search for New Therapeutic Targets

Table 1a.

Biological Characteristics of the CB1 and CB2 Receptors

CB1 CB2
a Adapted with permission from Sigma-RBI Handbook of Receptor Classification and Signal Transduction.
Size (amino acid residues) 472 360
Tissue expression Brain (cerebellum, basal ganglia, cerebral cortex), liver, testes Peripheral immune cells, sparse in brain
Physiological function Presynaptic heteroreceptor; inhibits neurotransmitter release Suppress immune cell function
Disease relevance Pain, appetite regulation, anxiety, craving, emesis Pain, immune system regulation, muscle spasms
Signal transduction mechanisms i (cAMP modulation)
 Inhibits voltage-sensitive Ca2+ channels (N-, Q-type)
 Activates Kir and KA conductance i (cAMP modulation)
Endogenous agonists (common to both CB1 and CB2) Arachidonoyl ethanolamide (anandamide)
2-Arachidonoyl glycerol (2-AG)
2-Arachidonoyl glyceryl ether (Nolandin ether)
N-Arachidonoyl dopamine
O-Arachidonoyl ethanolamine (Virodhamine)

This Article

  1. MI June 2006 vol. 6 no. 3 149-161