Cannabinoid receptors can bind cannabinoids

Stable Identifier
R-HSA-419426
Type
Reaction [binding]
Species
Homo sapiens
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The cannabinoid receptors are a class of receptors within the G-protein coupled receptor superfamily. Their ligands are known as cannabinoids or endocannabinoids depending on whether they come from external or internal (endogenous) sources, respectively (Howlett et al. 2002). Endocannabinoids serve as intercellular lipid messengers, signaling molecules that are released from one cell and activate the cannabinoid receptors present on other cells.
Cannabinoid type 1 (CB1) receptors (Gerrard et al. 1990) are thought to be the most widely expressed G-protein coupled receptors in the brain, lungs, liver and kidneys. Endocannabinoids released from the depolarized neuron bind to CB1 receptors in the pre-synaptic neuron and cause a reduction in GABA release.
CB2 receptors (Munro et al. 1993) are mainly expressed on T cells of the immune system, on macrophages and B cells, and in hematopoietic cells. Current research suggests that these receptors play a role in nociception, or the perception of pain.
Both receptors' activity is mediated by coupling to the G protein alpha i/o subunit, which inhibits adenylyl cyclase (Bouaboula et al. 1995, Bayewitch et al. 1995).
GPR55 is activated by plant cannabinoids and the endocannabinoids 2-arachidonoyl glycerol (2-AG) and anandamide (AEA), leading to suggestions that it should be renamed CB3. However GPR55 has also been reported as a receptor for LPI and its derivative 2-Arachidonoyl-sn-glycero-3-phosphoinositol. 2-AG binds to the CB1 and CB2 receptors with similar affinity, acting as a full agonist.

Literature References
PubMed ID Title Journal Year
7775459 Stimulation of cannabinoid receptor CB1 induces krox-24 expression in human astrocytoma cells

Bouaboula, M, Bourrie, B, Rinaldi-Carmona, M, Shire, D, Le Fur, G, Casellas, P

J Biol Chem 1995
7689702 Molecular characterization of a peripheral receptor for cannabinoids

Munro, S, Thomas, KL, Abu-Shaar, M

Nature 1993
2263478 Nucleotide sequence of a human cannabinoid receptor cDNA

Gerard, C, Mollereau, C, Vassart, G, Parmentier, M

Nucleic Acids Res 1990
7498464 The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling

Bayewitch, M, Avidor-Reiss, T, Levy, R, Barg, J, Mechoulam, R, Vogel, Z

FEBS Lett 1995
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