Cannabinoid receptor 1 (CB1 receptor), Cannabinoid receptor 2 (CB2 receptor) (CB1R (for Cannabinoid receptor 1), CB2R (for Cannabinoid receptor 2))

The endocannabinoid system related receptors mainly include Cannabinoid receptor 1 and Cannabinoid receptor 2, which are G protein-coupled receptors activated by endogenous ligands (anandamide, 2-arachidonoylglycerol) and exogenous cannabinoids (THC). CB1 receptor is heavily expressed in the central nervous system and modulates neurotransmission, synaptic plasticity, and neuroprotection. CB2 receptor is predominantly found in immune cells and modulates inflammation and immune response. Both receptors are implicated in numerous physiological and pathological processes including pain, neurodegeneration, psychiatric disease, and metabolic syndrome. They are targets for many therapeutic and recreational drugs. The term "endocannabinoid system related receptors" is non-standard and should generally be replaced by their precise names (CB1, CB2).

Other names

CB1CNR1CB1Rcentral cannabinoid receptorCB2CNR2CB2Rperipheral cannabinoid receptor

Agonism: Activation of CB1R or CB2R by endogenous (anandamide, 2-arachidonoylglycerol) or exogenous cannabinoids (THC, synthetic cannabinoids) leads to inhibition of adenylyl cyclase, reduced cAMP, inhibition of calcium channels, activation of potassium channels, and recruitment of beta-arrestins. Antagonism/inverse agonism: Blockade (rimonabant, SR144528) prevents receptor activity and downstream signaling