A<sub>2B</sub> receptor | Adenosine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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A2B receptor

Target id: 20

Nomenclature: A2B receptor

Family: Adenosine receptors

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

   GtoImmuPdb view: OFF :     A2B receptor has curated data in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 332 17p12-p11.2 ADORA2B adenosine A2b receptor 60
Mouse 7 332 11 B2 Adora2b adenosine A2b receptor 49
Rat 7 332 10q23 Adora2b adenosine A2B receptor 66
Previous and Unofficial Names
adenosine receptor A2b | A2b | A2BR
Database Links
Specialist databases
GPCRDB aa2br_human (Hs), aa2br_mouse (Mm), aa2br_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
adenosine

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 Affinity Units Reference
BAY 60-6583 Hs Agonist 8.0 – 8.5 pKi 21
pKi 8.0 – 8.5 (Ki 1x10-8 – 3x10-9 M) [21]
2-hexynyl-NECA Hs Full agonist 6.6 pKi 70
pKi 6.6 [70]
BAY 60-6583 Mm Agonist 6.5 pKi 45
pKi 6.5 (Ki 3.3x10-7 M) [45]
NECA Hs Full agonist 5.7 – 6.9 pKi 7,10,34,47,67,70,77
pKi 5.7 – 6.9 [7,10,34,47,67,70,77]
NECA Mm Agonist 5.7 pKi 48
pKi 5.7 (Ki 1.9x10-6 M) [48]
adenosine Rn Agonist 5.3 pKi 77
pKi 5.3 (Ki 5.1x10-6 M) [77]
CGS 21680 Rn Agonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
Cl-IB-MECA Hs Agonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
Cl-IB-MECA Mm Agonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
TCPA Hs Agonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
regadenoson Hs Agonist <5.0 pKi 33
pKi <5.0 (Ki >1x10-5 M) [33]
MRS3558 Hs Agonist <5.0 pKi 33
pKi <5.0 (Ki >1x10-5 M) [33]
adenosine Hs Agonist 4.8 pKi 27-28,77
pKi 4.8 (Ki 1.5x10-5 M) [27-28,77]
2-chloroadenosine Hs Full agonist 4.6 – 5.0 pKi 7,12,47
pKi 4.6 – 5.0 [7,12,47]
(R)-PIA Mm Agonist 4.7 pKi 11
pKi 4.7 (Ki 1.9x10-5 M) [11]
(S)-PIA Hs Full agonist 4.2 – 5.2 pKi 47,70
pKi 4.2 – 5.2 [47,70]
AB-NECA Hs Full agonist 4.7 pKi 47
pKi 4.7 [47]
(R)-PIA Hs Full agonist 3.8 – 5.5 pKi 7,12,34,47,70
pKi 3.8 – 5.5 [7,12,34,47,70]
piclidenoson Hs Full agonist 4.3 – 4.9 pKi 33,47
pKi 4.3 – 4.9 [33,47]
cyclopentyladenosine Hs Full agonist 4.5 – 4.7 pKi 33,47
pKi 4.5 – 4.7 [33,47]
CCPA Hs Full agonist 4.4 – 4.7 pKi 33,47
pKi 4.4 – 4.7 [33,47]
HEMADO Hs Agonist <4.5 pKi 44,74
pKi <4.5 (Ki >3x10-5 M) [44,74]
GS9667 Hs Agonist <4.3 pKi 23
pKi <4.3 (Ki >5x10-5 M) [23]
CGS 21680 Hs Full agonist 3.4 – 5.0 pKi 7,33,47
pKi 3.4 – 5.0 [7,33,47]
N(6)-cyclohexyladenosine Hs Agonist 3.8 pKi 12
pKi 3.8 (Ki 1.6x10-4 M) [12]
binodenoson Hs Agonist 3.4 pKi 33
pKi 3.4 (Ki 4.3x10-4 M) [33]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
xanthine amine congener Hs Antagonist 7.9 pA2 2
pA2 7.9 [2]
CGS 15943 Hs Antagonist 7.8 pA2 2
pA2 7.8 [2]
[3H]MRS1754 Hs Antagonist 9.8 pKd 34
pKd 9.8 (Kd 1.58x10-10 M) [34]
[3H]OSIP339391 Hs Antagonist 9.8 pKd 67
pKd 9.8 [67]
[3H]PSB603 Mm Antagonist 9.5 pKd 9
pKd 9.5 [9]
PSB603 Mm Antagonist 9.4 pKd 9
pKd 9.4 (Kd 3.51x10-10 M) [9]
[3H]PSB603 Hs Antagonist 9.4 pKd 9
pKd 9.4 [9]
PSB603 Hs Antagonist 9.4 pKd 9
pKd 9.4 (Kd 4.03x10-10 M) [9]
[3H]DPCPX Hs Antagonist 7.4 pKd 67
pKd 7.4 [67]
[125I]ABOPX Hs Antagonist 7.4 pKd 47
pKd 7.4 [47]
[3H]ZM 241385 Hs Antagonist 6.5 – 7.9 pKd 25,35,67
pKd 6.5 – 7.9 [25,35,67]
PSB-0788 Hs Antagonist 9.4 pKi 9
pKi 9.4 [9]
OSIP339391 Hs Antagonist 9.3 pKi 67
pKi 9.3 [67]
PSB603 Hs Antagonist 9.3 pKi 9
pKi 9.3 (Ki 5.53x10-10 M) [9]
MRS1706 ? Antagonist 8.9 pKi 42
pKi 8.9 [42]
MRS1754 Hs Antagonist 8.8 pKi 34,42
pKi 8.8 (Ki 1.58x10-9 M) [34,42]
ATL802 Hs Antagonist 8.6 pKi 42
pKi 8.6 (Ki 2.36x10-9 M) [42]
MRS1754 Mm Antagonist 8.5 pKi 4
pKi 8.5 (Ki 3.39x10-9 M) [4]
AS99 Hs Antagonist 8.4 pKi 70
pKi 8.4 [70]
AS101 Hs Antagonist 8.4 pKi 70
pKi 8.4 [70]
MRE 2029F20 Hs Antagonist 8.3 – 8.5 pKi 5,70
pKi 8.3 – 8.5 [5,70]
AS100 Hs Antagonist 8.2 pKi 70
pKi 8.2 [70]
AS70 Hs Antagonist 8.1 pKi 70
pKi 8.1 [70]
ATL802 Mm Antagonist 8.1 pKi 42
pKi 8.1 (Ki 8.58x10-9 M) [42]
CGS 15943 Mm Antagonist 8.0 pKi 4
pKi 8.0 (Ki 9.07x10-9 M) [4]
AS96 Hs Antagonist 8.0 pKi 70
pKi 8.0 [70]
DEPX Hs Antagonist 7.9 pKi 47
pKi 7.9 [47]
xanthine amine congener Hs Antagonist 6.9 – 8.8 pKi 7,34-35,43,47,67
pKi 6.9 – 8.8 [7,34-35,43,47,67]
MRS1754 Rn Antagonist 7.8 – 7.9 pKi 26,42
pKi 7.8 – 7.9 (Ki 1.66x10-8 – 1.28x10-8 M) [26,42]
AS94 Hs Antagonist 7.8 pKi 70
pKi 7.8 [70]
LAS38096 Hs Antagonist 7.8 pKi 19,72
pKi 7.8 (Ki 1.7x10-8 M) [19,72]
AS16 Hs Antagonist 7.7 pKi 70
pKi 7.7 [70]
AS95 Hs Antagonist 7.7 pKi 70
pKi 7.7 [70]
CVT-6883 Hs Antagonist 7.7 pKi 22
pKi 7.7 (Ki 2.2x10-8 M) [22]
AS74 Hs Antagonist 7.6 pKi 70
pKi 7.6 [70]
ZM-241385 Hs Antagonist 6.8 – 8.2 pKi 7,34,47,67
pKi 6.8 – 8.2 [7,34,47,67]
I-ABOPX Hs Antagonist 7.4 pKi 47
pKi 7.4 [47]
CPX Hs Antagonist 7.3 pKi 34,47
pKi 7.3 [34,47]
BW-A1433 Hs Antagonist 7.3 pKi 47
pKi 7.3 [47]
XCC Hs Antagonist 7.3 pKi 34
pKi 7.3 [34]
PSB1115 Hs Antagonist 7.3 pKi 31
pKi 7.3 (Ki 5.34x10-8 M) [31]
vipadenant Hs Antagonist 7.2 pKi 30
pKi 7.2 (Ki 6.3x10-8 M) [30]
DPCPX Hs Antagonist 6.9 – 7.3 pKi 41,58,67,75
pKi 6.9 – 7.3 [41,58,67,75]
DPCPX Mm Antagonist 7.1 pKi 4
pKi 7.1 (Ki 8.62x10-8 M) [4]
CGS 15943 Hs Antagonist 6.0 – 8.1 pKi 4,34-35,43,59,67
pKi 6.0 – 8.1 [4,34-35,43,59,67]
tonapofylline Hs Antagonist 7.1 pKi 39
pKi 7.1 (Ki 9x10-8 M) [39]
PSB36 Hs Antagonist 6.7 pKi 40
pKi 6.7 (Ki 1.87x10-7 M) [40]
DPCPX Rn Antagonist 6.7 – 6.7 pKi 26,41
pKi 6.7 – 6.7 (Ki 2x10-7 – 1.86x10-7 M) [26,41]
rolofylline Hs Antagonist 6.5 pKi 39
pKi 6.5 (Ki 2.96x10-7 M) [39]
LUF5981 Hs Antagonist <6.5 pKi 37
pKi <6.5 (Ki >3x10-7 M) [37]
MRS1220 Hs Antagonist 6.5 pKi 67
pKi 6.5 [67]
ST-1535 Hs Antagonist 6.4 pKi 51
pKi 6.4 (Ki 3.523x10-7 M) [51]
DAX Hs Antagonist 6.4 pKi 34
pKi 6.4 [34]
3-isobutyl-8-pyrrolidinoxanthine Hs Antagonist 6.3 pKi 25
pKi 6.3 [25]
derenofylline Rn Antagonist 6.3 pKi 36
pKi 6.3 (Ki 5.01x10-7 M) [36]
SCH 58261 Hs Antagonist 6.0 – 6.5 pKi 7,33
pKi 6.0 – 6.5 [7,33]
KF26777 Hs Antagonist 6.2 pKi 61
pKi 6.2 (Ki 6.2x10-7 M) [61]
FK-453 Hs Antagonist 6.0 pKi 33
pKi 6.0 (Ki 9.8x10-7 M) [33]
alloxazine Hs Antagonist 5.7 – 6.3 pKi 34-35
pKi 5.7 – 6.3 [34-35]
preladenant Hs Antagonist <6.0 pKi 53
pKi <6.0 (Ki >1x10-6 M) [53]
MRE 3008F20 Hs Antagonist 5.7 – 5.8 pKi 33,70-71
pKi 5.7 – 5.8 [33,70-71]
PSB-10 Mm Antagonist 5.7 pKi 54
pKi 5.7 (Ki 2.1x10-6 M) [54]
PSB-11 Mm Antagonist 5.7 pKi 54
pKi 5.7 (Ki 2.1x10-6 M) [54]
derenofylline Hs Antagonist 5.4 pKi 36
pKi 5.4 (Ki 3.981x10-6 M) [36]
pentoxifylline Hs Antagonist 5.3 pKi 41
pKi 5.3 (Ki 5.18x10-6 M) [41]
MSX-2 Hs Antagonist 5.0 – 5.5 pKi 63,65
pKi 5.0 – 5.5 (Ki 1x10-5 – 2.9x10-6 M) [63,65]
theophylline Mm Antagonist 5.3 pKi 4
pKi 5.3 (Ki 5.63x10-6 M) [4]
CSC Rn Antagonist 5.1 pKi 15
pKi 5.1 (Ki 8.2x10-6 M) [15]
MRS1191 Hs Antagonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
MRS1523 Hs Antagonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
MRS1523 Mm Antagonist <5.0 pKi 46
pKi <5.0 (Ki >1x10-5 M) [46]
SCH442416 Hs Antagonist <5.0 pKi 33
pKi <5.0 (Ki >1x10-5 M) [33]
istradefylline Hs Antagonist <5.0 pKi 29
pKi <5.0 (Ki >1x10-5 M) [29]
caffeine Mm Antagonist 4.9 pKi 11
pKi 4.9 (Ki 1.3x10-5 M) [11]
caffeine Hs Antagonist 4.5 – 5.0 pKi 6,9,41
pKi 4.5 – 5.0 (Ki 3.38x10-5 – 1.04x10-5 M) [6,9,41]
theophylline Hs Antagonist 4.1 – 5.0 pKi 6,25,41,70
pKi 4.1 – 5.0 (Ki 7.4x10-5 – 9.07x10-6 M) [6,25,41,70]
caffeine Rn Antagonist 4.5 pKi 11
pKi 4.5 (Ki 3x10-5 M) [11]
View species-specific antagonist tables
Antagonist Comments
pKi values for istradefylline relating to human targets are derived from unpublished data (Müller et al).
Immunopharmacology Comments
A2B receptor is discussed in this immuno-oncology review [1].
Cell Type Associations
Immuno Cell Type:  T cells
Cell Ontology Term:   type I NK T cell (CL:0000921)
CD4-positive, alpha-beta T cell (CL:0000624)
CD8-positive, alpha-beta T cell (CL:0000625)
Comment:  An anti-A2B receptor antibody shows expression in CD4+ and CD8+ T-cell subpopulations. More than 95% of Jurkat T cells were shown to be A2B receptor positive. A2B receptor is expressed by mouse iNKT cells.
References:  52,56
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  A2B receptor is expressed by LAD2 mast cells at the mRNA and protein levels. Flow cytometry of permeabilised cells detected receptor protein in intracellular pools. By mRNA expression level, the A2A receptor was the most abundantly expressed of the four adenosine receptor subtypes (A2A > A2B > A3; A1 mRNA not detected).
References:  3
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002882 positive regulation of chronic inflammatory response to non-antigenic stimulus IEA
GO:0043306 positive regulation of mast cell degranulation IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002882 positive regulation of chronic inflammatory response to non-antigenic stimulus IEA
GO:0043306 positive regulation of mast cell degranulation IEA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0010575 positive regulation of vascular endothelial growth factor production IEA
GO:0032722 positive regulation of chemokine production IEA
GO:0032755 positive regulation of interleukin-6 production IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0032722 positive regulation of chemokine production IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0043306 positive regulation of mast cell degranulation IEA
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  24,47
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  24,47
Tissue Distribution
Low levels found in the brain, heart, kidney and lung.
Species:  Human
Technique:  Northern blotting.
References:  62
Jejunum, ileum, colon.
Species:  Human
Technique:  RT-PCR.
References:  14
Bronchial smooth muscle cells.
Species:  Human
Technique:  RT-PCR.
References:  79
Large intestine, cecum, urinary bladder.
Species:  Human
Technique:  Northern blotting.
References:  66
Type II epithelial cells
Species:  Mouse
Technique:  Reporter gene
References:  13
Bone marrow-derived mast cells.
Species:  Mouse
Technique:  in situ hybridisation.
References:  49
Kidney: cortical tubular structures.
Species:  Mouse
Technique:  RNAse protection and RT-PCR.
References:  73
Hypophyseal pars tuberalis.
Species:  Rat
Technique:  in situ hybridisation.
References:  66
Kidney: cortical tubular structures.
Species:  Rat
Technique:  RNAse protection and RT-PCR.
References:  73
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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Functional Assays
Measurement of cAMP levels in HEK 293 cells transfected with the human A2B receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  47
Measurement of IP3 levels in HEK 293 cells transfected with the human A2B receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  PTX-insensitive increase in IP3 levels.
References:  47
Measurement of cAMP levels in COS-6M cells transfected with the rat A2B receptor.
Species:  Rat
Tissue:  COS-6M cells.
Response measured:  Stimulation of cAMP accumulation.
References:  66
Measurement of cAMP levels in CHO cells transfected with the human A2B receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of cAMP accumulation.
References:  10,60
Measurement of extracellular-regulated kinase 1/2 (ERK1/2) phosphorylation in CHO cells transfected with the human A1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Phosphorylation of ERK1/2.
References:  64
Measurement of IL-6 and MCP-1 expression in human bronchial smooth muscle cells endogenously expressing the A2B receptor.
Species:  Human
Tissue:  Bronchial smooth muscle cells.
Response measured:  IL-6 and MCP-1 production via cAMP accumulation.
References:  79
Measurement of Il-8 production by the HMC-1 mast cell line endogenously expressing the A2B receptor.
Species:  Human
Tissue:  HMC-1 mast cell line.
Response measured:  Il-8 production.
References:  24,50
Measurement of NF-κB activity in CHO cells transfected with the human A2B receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of NF-κB activity via cAMP.
References: 
Measurement of IL-6 and IL-8 release
Species:  Human
Tissue:  Airway epithelial cells
Response measured:  Polarized release of IL-6 and IL-8 by ELISA
References:  68
Measurement of tube formation and VEGF transcription
Species:  Human
Tissue:  Microvascular endothelial cells
Response measured:  Tube formation and VEGF transcription by tube formation assay and PCR
References:  17
Physiological Functions
Vasodilation.
Species:  Human
Tissue:  Small coronary arteries.
References:  38
Vasoconstriction.
Species:  Human
Tissue:  Chorionic vessels.
References:  16
Inhibition of macrophage proliferation.
Species:  Mouse
Tissue:  Bone marrow-derived macrophages.
References:  76
Cytokine production.
Species:  Mouse
Tissue:  Macrophages.
References:  57
Cytokine production.
Species:  Human
Tissue:  Bronchial smooth muscle cells.
References:  79
Inhibition of cell proliferation.
Species:  Human
Tissue:  Glomerular mesangial cells.
References:  18
Inhibition of cell proliferation.
Species:  Rat
Tissue:  Glomerular mesangial cells.
References:  18
Coronary vasodilation.
Species:  Rat
Tissue:  Heart.
References:  32
Regulation of cerebral blood flow (vasodilation).
Species:  Rat
Tissue:  Cerebral cortex.
References:  55
Regulation of coronary flow.
Species:  Mouse
Tissue:  Heart.
References:  69
Physiological Consequences of Altering Gene Expression
A2B receptor knock-out mice show increased leukocyte adhesion to vascular endothelium and increased inflammation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  78
A2B receptor KO mice show increased vascular leakiness.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  20
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b
MGI:99403  MP:0009858 abnormal cellular extravasation PMID: 17200408 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0008713 abnormal cytokine level PMID: 16823489 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
B6.129P2-Adora2b
MGI:99403  MP:0002376 abnormal dendritic cell physiology PMID: 18559975 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0001845 abnormal inflammatory response PMID: 16823489 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0008751 abnormal interleukin level PMID: 16823489 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0003628 abnormal leukocyte adhesion PMID: 16823489 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0003156 abnormal leukocyte migration PMID: 16823489 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J
MGI:99403  MP:0003627 abnormal leukocyte tethering or rolling PMID: 16823489 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
B6.129P2-Adora2b
MGI:99403  MP:0001379 abnormal penile erection function PMID: 18340377 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
B6.129P2-Adora2b
MGI:99403  MP:0005164 abnormal response to injury PMID: 18056839