CB<sub>2</sub> receptor | Cannabinoid receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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CB2 receptor

target has curated data in GtoImmuPdb

Target id: 57

Nomenclature: CB2 receptor

Family: Cannabinoid receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 360 1p35-p36 CNR2 cannabinoid receptor 2 35,48
Mouse 7 347 4 D3 Cnr2 cannabinoid receptor 2 (macrophage) 50
Rat 7 410 5q36 Cnr2 cannabinoid receptor 2 8
Previous and Unofficial Names
rCB2 | cannabinoid receptor 2 (spleen) | CB2-R | Peripheral cannabinoid receptor | cannabinoid receptor 2 (macrophage)
Database Links
Specialist databases
GPCRDB cnr2_human (Hs), cnr2_mouse (Mm), cnr2_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
anandamide
2-arachidonoylglycerol
Comments: Endogenous ligands include other endocannabinoids

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]HU-243 Hs Full agonist 10.2 pKd 3
pKd 10.2 [3]
[3H]CP55940 Hs Full agonist 8.1 – 9.7 pKd 7,16,35,49-51
pKd 8.1 – 9.7 [7,16,35,49-51]
[3H]WIN55212-2 Hs Full agonist 8.4 – 8.7 pKd 35,52
pKd 8.4 – 8.7 [35,52]
AM7499 Mm Agonist 10.0 pKi 28
pKi 10.0 (Ki 1x10-10 M) [28]
MDMB-Fubinaca Hs Agonist 9.9 pKi 47
pKi 9.9 (Ki 1.3x10-10 M) [47]
HU-210 Hs Full agonist 9.3 – 9.8 pKi 16,43,51
pKi 9.3 – 9.8 [16,43,51]
Sch.336 Hs Inverse agonist 8.7 – 9.4 pKi 30,32
pKi 9.4 (Ki 4x10-10 M) [30]
pKi 8.7 (Ki 1.8x10-9 M) [32]
Description: Measuring competitin binding with [3H]CP55,940 for binding to human CB2 on Sf9 cell membranes.
WIN55212-2 Hs Full agonist 8.4 – 9.6 pKi 16,50-51
pKi 8.4 – 9.6 [16,50-51]
CP55940 Hs Full agonist 8.6 – 9.2 pKi 16,46,51
pKi 8.6 – 9.2 [16,46,51]
AM2201 Mm Agonist 8.6 pKi 33
pKi 8.6 (Ki 2.6x10-9 M) [33]
Description: Binding affinity vs. mouse spleen membranes.
AM7499 Hs Agonist 8.5 pKi 28
pKi 8.5 (Ki 3.1x10-9 M) [28]
JWH-133 Hs Full agonist 8.5 pKi 25,39
pKi 8.5 (Ki 3.16x10-9 M) [25,39]
JWH-018 Hs Full agonist 8.5 pKi 11
pKi 8.5 [11]
nabilone Hs Agonist 8.2 pKi 6
pKi 8.2 (Ki 6.31x10-9 M) [6]
AM1710 Mm Agonist 8.2 pKi 27
pKi 8.2 (Ki 6.7x10-9 M) [27]
AM1241 Hs Agonist 8.1 pKi 53
pKi 8.1 (Ki 7.94x10-9 M) [53]
L-759,633 Hs Full agonist 7.7 – 8.2 pKi 20,46
pKi 7.7 – 8.2 (Ki 1.99x10-8 – 6.31x10-9 M) [20,46]
L-759,656 Hs Full agonist 7.7 – 7.9 pKi 20,46
pKi 7.7 – 7.9 (Ki 1.99x10-8 – 1.26x10-8 M) [20,46]
HU-308 Hs Full agonist 7.6 pKi 23
pKi 7.6 (Ki 2.51x10-8 M) [23]
BAY-593074 Hs Partial agonist 7.3 pKi 13
pKi 7.3 (Ki 4.55x10-8 M) [13]
Δ9-tetrahydrocannabinol Hs Partial agonist 7.1 – 7.5 pKi 4,16,43,51
pKi 7.1 – 7.5 [4,16,43,51]
lenabasum Hs Agonist 6.8 pKi 21,41
pKi 6.8 (Ki 1.7x10-7 M) [21,41]
VCE-004.3 Hs Agonist 6.7 pKi 14
pKi 6.7 (Ki 2.04x10-7 M) [14]
taranabant Hs - 6.5 pKi 17
pKi 6.5 (Ki 2.9x10-7 M) [17]
phenylacetylrinvanil Hs Agonist 6.5 pKi 1
pKi 6.5 (Ki 3x10-7 M) [1]
Description: Binding affinity for recombinant human CB2 receptors expressed in COS cells, displacing [3H]-CP-55,940.
2-arachidonoylglycerol Hs Partial agonist 5.8 – 6.8 pKi 5,34
pKi 5.8 – 6.8 [5,34]
anandamide Hs Partial agonist 5.7 – 6.4 pKi 16,34,51
pKi 5.7 – 6.4 [16,34,51]
olorinab Hs Full agonist 8.2 pEC50 22
pEC50 8.2 (EC50 6.2x10-9 M) [22]
Description: In a DiscoverX PathHunter β-arrestin recruitment assay.
olorinab Rn Full agonist 8.1 pEC50 22
pEC50 8.1 (EC50 7.6x10-9 M) [22]
Description: In a DiscoverX PathHunter β-arrestin recruitment assay.
AM2201 Hs Agonist 7.2 pEC50 2
pEC50 7.2 (EC50 5.88x10-8 M) [2]
BMS-202 Hs Agonist 6.9 pEC50 2
pEC50 6.9 (EC50 1.31x10-7 M) [2]
View species-specific agonist tables
Agonist Comments
The higher pKi value for anandamide (6.43) was determined in the presence of phenylmethylsulfonyl fluoride to prevent enzymic hydrolysis. For reviews, see references [24,37-38]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AM10257 Hs Antagonist 10.1 pKi 31
pKi 10.1 (Ki 7.5x10-11 M) [31]
Description: Antagonism of [3H]CP55940 binding to human CB2.
SR144528 Hs Antagonist 8.3 – 9.2 pKi 45-46
pKi 8.3 – 9.2 (Ki 5.01x10-9 – 6.3x10-10 M) [45-46]
AM-630 Hs Antagonist 7.5 pKi 46
pKi 7.5 (Ki 3.16x10-8 M) [46]
surinabant Hs Full agonist 6.3 pKi 44
pKi 6.3 (Ki 4.42x10-7 M) [44]
Description: Inhbition of [3H]-CP 55,940 binding to human CB2 receptors expressed in CHO cells
ibipinabant Hs Antagonist 5.1 pKi 29
pKi 5.1 (Ki 7.943x10-6 M) [29]
Description: Displacement of specific CP-55,940 binding in CHO cells stably transfected with human CB2 receptor
TM-38837 Hs Antagonist 6.2 pIC50 26
pIC50 6.2 (IC50 6.05x10-7 M) [26]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
pepcan-12 Hs Positive ~7.3 pKi 40
pKi ~7.3 (Ki ~5x10-8 M) [40]
compound C2 [PMID: 29990428] Hs Positive - - 18
[18]
Immunopharmacology Comments
CB2 receptor on eosinophils mainly mediates anti-inflammatory and immunomodulatory actions e.g. downregulation of pro-inflammatory mediator release. Pharmacological targeting with the CB2 receptor selective antagonist SR144528 attenuates the recruitment of eosinophils and ear swelling in a murine chronic contact dermatitis model [36].
Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  Mast cells express both cannabinoid receptors.
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
Comment:  Eosinophils do not express CB1 receptor.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 4 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA
GO:0030595 leukocyte chemotaxis IEA
GO:0033004 negative regulation of mast cell activation IEA
GO:0050728 negative regulation of inflammatory response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0033004 negative regulation of mast cell activation IEA
GO:0050728 negative regulation of inflammatory response IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0030595 leukocyte chemotaxis IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0033004 negative regulation of mast cell activation IEA
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Other - See Comments
Comments:  Activation of MAP kinase leading to immediate early gene expression[24,49].
References:  7-8,16,24,50-52
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  24,42
Tissue Distribution
Spleen, tonsils, bone marrow and peripheral blood leukocytes
Species:  Human
Technique:  RT-PCR
References:  19,24,35,37
Monocytes, macrophages, and microglial cells,
Species:  Rat
Technique:  RT-PCR
References:  10,12,15,24,35
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Physiological Consequences of Altering Gene Expression
This has been little investigated. There is one report that cannabinoid-induced inhibition of helper T cell activation is lost in macrophages obtained from CB2 knockout mice.
Species:  Mouse
Tissue: 
Technique:  Induced mutation.
References:  9
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cnr2tm1Zim Cnr2tm1Zim/Cnr2tm1Zim
involves: 129 * C57BL/6
MGI:104650  MP:0002451 abnormal macrophage physiology PMID: 10822068 
Cnr2tm1Dgen Cnr2tm1Dgen/Cnr2tm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:104650  MP:0000414 alopecia
General Comments
Techniques used include Northern blot, in situ hybridization and receptor autoradiography[24,37]

References

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2. Banister SD, Stuart J, Kevin RC, Edington A, Longworth M, Wilkinson SM, Beinat C, Buchanan AS, Hibbs DE, Glass M et al.. (2015) Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135. ACS Chem Neurosci, 6 (8): 1445-58. [PMID:25921407]

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4. Bayewitch M, Rhee MH, Avidor-Reiss T, Breuer A, Mechoulam R, Vogel Z. (1996) (-)-Delta9-tetrahydrocannabinol antagonizes the peripheral cannabinoid receptor-mediated inhibition of adenylyl cyclase. J. Biol. Chem., 271 (17): 9902-5. [PMID:8626625]

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22. Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J et al.. (2017) Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. ACS Med Chem Lett, 8 (12): 1309-1313. [PMID:29259753]

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26. Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, Wu CH, Kuo PC, Amancha PK, Wong YC et al.. (2010) Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. ChemMedChem, 5 (9): 1439-43. [PMID:20652930]

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28. Kulkarni S, Nikas SP, Sharma R, Jiang S, Paronis CA, Leonard MZ, Zhang B, Honrao C, Mallipeddi S, Raghav JG et al.. (2016) Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues. J. Med. Chem., 59 (14): 6903-19. [PMID:27367336]

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