Cannabinoid GPCR Family Subtypes and Products

What Are Cannabinoid Receptors?

Cannabinoid receptors are a class of G protein-coupled receptors (GPCRs) found all throughout the body, and play a large role in mood, memory, pain-sensation and appetite. The cannabinoid receptor family can be broken down into two smaller subtypes of receptors: CB1 and CB2. CB1 receptors are mainly found in the central nervous system, as well as the kidneys, lungs, and liver. CB2 receptors are mainly found in hematopoietic cells and within the immune system. In 2007, however, the GPCR GPR55 was found to bind cannabinoids as well, leading to the discovery of novel cannabinoid receptors. The main component of cannabis, tetrahydrocannabinol (THC), is a cannabinoid receptor agonist used to treat vomiting and lack of appetite in patients with AIDS or cancer.

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Cannabinoid Receptor Information

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CB1

CB1a

CB1b

CB2

GPR55

Cannabinoid Receptor 1, CNR1 also known as CB1, is involved in cannabinoid induced CNS effects. It acts by inhibiting intracellular adenylate cyclase activity and could be a receptor for anandamide. CNR1 is a potential target for the development of novel therapeutic drugs in the treatment of various conditions, such as pain, feeding disorders, vascular disease, Parkinson’s disease, and other central nerve system disorders.

CB1A is a truncated isoform of CB1 mutant which is resulted from the removal of 89 amino acid in N-terminus and substituted with 28 amino acids by frame shift. This mutant is distributed throughout the brain and peripheral tissue together with CB1.

CB1b is an isoform of CB1, formed by internal deletion of 33 amino acids and preferentially expressed in B cells and Hepatocyte of Liver and is a more powerful modulator of adenyl cyclase activity.

Cannabinoid receptor 2 (CB2 or CNR2) is involved in cannabinoid- induced central nerve system effects. It could be a receptor for anandamide. The receptor is a potential therapeutic target in the treatment of various disease conditions, such as pain, multiple sclerosis, vascular disease, Parkinson’s disease, and other central nerve system disorders.

GPR55 is a putative cannabinoid receptor. Its gene was mapped to chromosome 2q37, using fluorescence in situ hybridization (FISH), and its mRNA transcripts have been detected in the caudate nucleus and putamen. Recently, GPR55 was identified as a receptor for the bioactive lipid lysophosphatidylinositol (LPI).

Cannabinoid Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
CannabinoidCB1humanHEK293TC1229DC1229MC1229
CB1human CHO-K1C1229-1aDC1229-1aMC1229-1a
CB1humanCHO-K1C1229-1DC1229-1MC1229-1
CB1ahumanCHO-K1C1512-1DC1512-1MC1512-1
CB1bhumanCHO-K1C1513-1DC1513-1MC1513-1
CB1mouseCHO-K1Cm1229-1ADCm1229-1AMCm1229-1A
CB1mouseCHO-K1Cm1229-1BDCm1229-1BMCm1229-1B
CB1dogHEK293TCd1229DCd1229MCd1229
CB1dogHEK293TCd1229aDCd1229aMCd1229a
CB1dogHEK293TCd1229bDCd1229bMCd1229b
CB1 MUTANT BhumanCHO-K1 β-Arrestin2CA1513BA2-1DCA1513BA2-1MCA1513BA2-1
CB2humanCHO-K1C1230-1DC1230-1MC1230-1
CB2humanCHO-K1C1230-1aDC1230-1aMC1230-1a
CB2humanCHO-K1 β-Arrestin2CA1230BA2-1DCA1230BA2-1MCA1230BA2-1
CB2ratCHO-K1Cr1230-1DCr1230-1MCr1230-1
CB2ratCHO-K1Cr1230-1aDCr1230-1aMCr1230-1a
CB2mouseCHO-K1 β-Arrestin2CAm1230BA2-1DCAm1230BA2-1MCAm1230BA2-1
CB2mouseCHO-K1Cm1230-1DCm1230-1MCm1230-1
CB2mouseCHO-K1Cm1230-1aDCm1230-1aMCm1230-1a
CB2ratCHO-K1 β-Arrestin2CAr1230BA2-1DCAr1230BA2-1MCAr1230BA2-1
CB2ratCHO-K1 β-Arrestin2CAr1230BA2-1aDCAr1230BA2-1aMCAr1230BA2-1a
GPR55humanHEK293TH1113H1113H1113
GPR55humanHEK293TC1113bDC1113bMC1113b
GPR55humanHEK293TC1113dDC1113dMC1113d

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