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A2B receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 20

Nomenclature: A2B receptor

Family: Adenosine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 332 17p12 ADORA2B adenosine A2b receptor 63
Mouse 7 332 11 B2 Adora2b adenosine A2b receptor 52
Rat 7 332 10q23 Adora2b adenosine A2B receptor 69
Previous and Unofficial Names Click here for help
adenosine receptor A2b | A2b | A2BR
Database Links Click here for help
Specialist databases
GPCRdb aa2br_human (Hs), aa2br_mouse (Mm), aa2br_rat (Rn)
Other databases
Alphafold P29275 (Hs), Q60614 (Mm), P29276 (Rn)
ChEMBL Target CHEMBL255 (Hs), CHEMBL2237 (Mm), CHEMBL2592 (Rn)
DrugBank Target P29275 (Hs)
Ensembl Gene ENSG00000170425 (Hs), ENSMUSG00000018500 (Mm), ENSRNOG00000002922 (Rn)
Entrez Gene 136 (Hs), 11541 (Mm), 29316 (Rn)
Human Protein Atlas ENSG00000170425 (Hs)
KEGG Gene hsa:136 (Hs), mmu:11541 (Mm), rno:29316 (Rn)
OMIM 600446 (Hs)
Pharos P29275 (Hs)
RefSeq Nucleotide NM_000676 (Hs), NM_007413 (Mm), NM_017161 (Rn)
RefSeq Protein NP_000667 (Hs), NP_031439 (Mm), NP_058857 (Rn)
UniProtKB P29275 (Hs), Q60614 (Mm), P29276 (Rn)
Wikipedia ADORA2B (Hs)
Natural/Endogenous Ligands Click here for help
adenosine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BAY 60-6583 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 8.0 – 8.5 pKi 22
⤷ pKi 8.0 – 8.5 (Ki 1x10-8 – 3x10-9 M) [22]
2-hexynyl-NECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.6 pKi 73
⤷ pKi 6.6 [73]
BAY 60-6583 Small molecule or natural product Ligand has a PDB structure Mm Agonist 6.5 pKi 48
⤷ pKi 6.5 (Ki 3.3x10-7 M) [48]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.7 – 6.9 pKi 7,11,37,50,70,73,80
⤷ pKi 5.7 – 6.9 [7,11,37,50,70,73,80]
NECA Small molecule or natural product Ligand has a PDB structure Mm Agonist 5.7 pKi 51
⤷ pKi 5.7 (Ki 1.9x10-6 M) [51]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Agonist 5.3 pKi 80
⤷ pKi 5.3 (Ki 5.1x10-6 M) [80]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Agonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Mm Agonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
TCPA Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 8
⤷ pKi <5.0 (Ki >1x10-5 M) [8]
regadenoson Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist <5.0 pKi 36
⤷ pKi <5.0 (Ki >1x10-5 M) [36]
MRS3558 Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 36
⤷ pKi <5.0 (Ki >1x10-5 M) [36]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 4.8 pKi 29-30,80
⤷ pKi 4.8 (Ki 1.5x10-5 M) [29-30,80]
2-chloroadenosine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.6 – 5.0 pKi 7,13,50
⤷ pKi 4.6 – 5.0 [7,13,50]
(R)-PIA Small molecule or natural product Mm Agonist 4.7 pKi 12
⤷ pKi 4.7 (Ki 1.9x10-5 M) [12]
(S)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.2 – 5.2 pKi 50,73
⤷ pKi 4.2 – 5.2 [50,73]
AB-NECA Small molecule or natural product Hs Full agonist 4.7 pKi 50
⤷ pKi 4.7 [50]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 3.8 – 5.5 pKi 7,13,37,50,73
⤷ pKi 3.8 – 5.5 [7,13,37,50,73]
piclidenoson Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 4.3 – 4.9 pKi 36,50
⤷ pKi 4.3 – 4.9 [36,50]
cyclopentyladenosine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 4.5 – 4.7 pKi 36,50
⤷ pKi 4.5 – 4.7 [36,50]
CCPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.4 – 4.7 pKi 36,50
⤷ pKi 4.4 – 4.7 [36,50]
HEMADO Small molecule or natural product Click here for species-specific activity table Hs Agonist <4.5 pKi 46,77
⤷ pKi <4.5 (Ki >3x10-5 M) [46,77]
GS9667 Small molecule or natural product Click here for species-specific activity table Hs Agonist <4.3 pKi 25
⤷ pKi <4.3 (Ki >5x10-5 M) [25]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 3.4 – 5.0 pKi 7,36,50
⤷ pKi 3.4 – 5.0 [7,36,50]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Hs Agonist 3.8 pKi 13
⤷ pKi 3.8 (Ki 1.6x10-4 M) [13]
binodenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 3.4 pKi 36
⤷ pKi 3.4 (Ki 4.3x10-4 M) [36]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
xanthine amine congener Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.9 pA2 2
⤷ pA2 7.9 [2]
CGS 15943 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 pA2 2
⤷ pA2 7.8 [2]
[3H]MRS1754 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKd 37
⤷ pKd 9.8 (Kd 1.58x10-10 M) [37]
[3H]OSIP339391 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKd 70
⤷ pKd 9.8 [70]
[3H]PSB603 Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Antagonist 9.5 pKd 10
⤷ pKd 9.5 [10]
PSB603 Small molecule or natural product Mm Antagonist 9.4 pKd 10
⤷ pKd 9.4 (Kd 3.51x10-10 M) [10]
[3H]PSB603 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.4 pKd 10
⤷ pKd 9.4 [10]
PSB603 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKd 10
⤷ pKd 9.4 (Kd 4.03x10-10 M) [10]
[3H]DPCPX Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 7.4 pKd 70
⤷ pKd 7.4 [70]
[125I]ABOPX Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 7.4 pKd 50
⤷ pKd 7.4 [50]
[3H]ZM 241385 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 6.5 – 7.9 pKd 27,38,70
⤷ pKd 6.5 – 7.9 [27,38,70]
PSB-0788 Small molecule or natural product Hs Antagonist 9.4 pKi 10
⤷ pKi 9.4 [10]
OSIP339391 Small molecule or natural product Hs Antagonist 9.3 pKi 70
⤷ pKi 9.3 [70]
PSB603 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.3 pKi 10
⤷ pKi 9.3 (Ki 5.53x10-10 M) [10]
MRS1706 Small molecule or natural product ? Antagonist 8.9 pKi 45
⤷ pKi 8.9 [45]
MRS1754 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 37,45
⤷ pKi 8.8 (Ki 1.58x10-9 M) [37,45]
ATL802 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 45
⤷ pKi 8.6 (Ki 2.36x10-9 M) [45]
MRS1754 Small molecule or natural product Mm Antagonist 8.5 pKi 4
⤷ pKi 8.5 (Ki 3.39x10-9 M) [4]
ISAM-140 Small molecule or natural product Hs Antagonist 8.5 pKi 23
⤷ pKi 8.5 (Ki 3.49x10-9 M) [23]
AS99 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 pKi 73
⤷ pKi 8.4 [73]
AS101 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.4 pKi 73
⤷ pKi 8.4 [73]
MRE 2029F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 – 8.5 pKi 5,73
⤷ pKi 8.3 – 8.5 [5,73]
AS100 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 73
⤷ pKi 8.2 [73]
AS70 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 pKi 73
⤷ pKi 8.1 [73]
ATL802 Small molecule or natural product Click here for species-specific activity table Mm Antagonist 8.1 pKi 45
⤷ pKi 8.1 (Ki 8.58x10-9 M) [45]
CGS 15943 Small molecule or natural product Ligand has a PDB structure Mm Antagonist 8.0 pKi 4
⤷ pKi 8.0 (Ki 9.07x10-9 M) [4]
AS96 Small molecule or natural product Hs Antagonist 8.0 pKi 73
⤷ pKi 8.0 [73]
DEPX Small molecule or natural product Hs Antagonist 7.9 pKi 50
⤷ pKi 7.9 [50]
xanthine amine congener Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 – 8.8 pKi 7,37-38,47,50,70
⤷ pKi 6.9 – 8.8 [7,37-38,47,50,70]
MRS1754 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.8 – 7.9 pKi 28,45
⤷ pKi 7.8 – 7.9 (Ki 1.66x10-8 – 1.28x10-8 M) [28,45]
AS94 Small molecule or natural product Hs Antagonist 7.8 pKi 73
⤷ pKi 7.8 [73]
LAS38096 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 pKi 20,75
⤷ pKi 7.8 (Ki 1.7x10-8 M) [20,75]
AS16 Small molecule or natural product Hs Antagonist 7.7 pKi 73
⤷ pKi 7.7 [73]
AS95 Small molecule or natural product Hs Antagonist 7.7 pKi 73
⤷ pKi 7.7 [73]
CVT-6883 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 24
⤷ pKi 7.7 (Ki 2.2x10-8 M) [24]
AS74 Small molecule or natural product Hs Antagonist 7.6 pKi 73
⤷ pKi 7.6 [73]
ZM-241385 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 – 8.2 pKi 7,37,50,70
⤷ pKi 6.8 – 8.2 [7,37,50,70]
I-ABOPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.4 pKi 50
⤷ pKi 7.4 [50]
CPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.3 pKi 37,50
⤷ pKi 7.3 [37,50]
BW-A1433 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.3 pKi 50
⤷ pKi 7.3 [50]
XCC Small molecule or natural product Hs Antagonist 7.3 pKi 37
⤷ pKi 7.3 [37]
PSB1115 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 7.3 pKi 33
⤷ pKi 7.3 (Ki 5.34x10-8 M) [33]
vipadenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 7.2 pKi 32
⤷ pKi 7.2 (Ki 6.3x10-8 M) [32]
imaradenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 7.2 pKi 9
⤷ pKi 7.2 (Ki 6.4x10-8 M) [9]
Description: Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.
DPCPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 – 7.3 pKi 44,61,70,78
⤷ pKi 6.9 – 7.3 [44,61,70,78]
DPCPX Small molecule or natural product Mm Antagonist 7.1 pKi 4
⤷ pKi 7.1 (Ki 8.62x10-8 M) [4]
CGS 15943 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.0 – 8.1 pKi 4,37-38,47,62,70
⤷ pKi 6.0 – 8.1 [4,37-38,47,62,70]
tonapofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 42
⤷ pKi 7.1 (Ki 9x10-8 M) [42]
BAY-545 Small molecule or natural product Hs Antagonist 7.0 pKi 35
⤷ pKi 7.0 (Ki 9.7x10-8 M) [35]
PSB36 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 43
⤷ pKi 6.7 (Ki 1.87x10-7 M) [43]
DPCPX Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.7 – 6.7 pKi 28,44
⤷ pKi 6.7 – 6.7 (Ki 2x10-7 – 1.86x10-7 M) [28,44]
rolofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 42
⤷ pKi 6.5 (Ki 2.96x10-7 M) [42]
LUF5981 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.5 pKi 40
⤷ pKi <6.5 (Ki >3x10-7 M) [40]
MRS1220 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 70
⤷ pKi 6.5 [70]
ST-1535 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 54
⤷ pKi 6.4 (Ki 3.523x10-7 M) [54]
DAX Small molecule or natural product Hs Antagonist 6.4 pKi 37
⤷ pKi 6.4 [37]
3-isobutyl-8-pyrrolidinoxanthine Small molecule or natural product Hs Antagonist 6.3 pKi 27
⤷ pKi 6.3 [27]
derenofylline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 pKi 39
⤷ pKi 6.3 (Ki 5.01x10-7 M) [39]
SCH 58261 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 – 6.5 pKi 7,36
⤷ pKi 6.0 – 6.5 [7,36]
KF26777 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 64
⤷ pKi 6.2 (Ki 6.2x10-7 M) [64]
FK-453 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 36
⤷ pKi 6.0 (Ki 9.8x10-7 M) [36]
alloxazine Small molecule or natural product Hs Antagonist 5.7 – 6.3 pKi 37-38
⤷ pKi 5.7 – 6.3 [37-38]
preladenant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <6.0 pKi 56
⤷ pKi <6.0 (Ki >1x10-6 M) [56]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.7 – 5.8 pKi 36,73-74
⤷ pKi 5.7 – 5.8 [36,73-74]
PSB-10 Small molecule or natural product Mm Antagonist 5.7 pKi 57
⤷ pKi 5.7 (Ki 2.1x10-6 M) [57]
PSB-11 Small molecule or natural product Mm Antagonist 5.7 pKi 57
⤷ pKi 5.7 (Ki 2.1x10-6 M) [57]
derenofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 pKi 39
⤷ pKi 5.4 (Ki 3.981x10-6 M) [39]
pentoxifylline Small molecule or natural product Approved drug Ligand has a PDB structure Hs Antagonist 5.3 pKi 44
⤷ pKi 5.3 (Ki 5.18x10-6 M) [44]
MSX-2 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 – 5.5 pKi 66,68
⤷ pKi 5.0 – 5.5 (Ki 1x10-5 – 2.9x10-6 M) [66,68]
theophylline Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Mm Antagonist 5.3 pKi 4
⤷ pKi 5.3 (Ki 5.63x10-6 M) [4]
CSC Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.1 pKi 16
⤷ pKi 5.1 (Ki 8.2x10-6 M) [16]
MRS1191 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
MRS1523 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
MRS1523 Small molecule or natural product Click here for species-specific activity table Mm Antagonist <5.0 pKi 49
⤷ pKi <5.0 (Ki >1x10-5 M) [49]
SCH442416 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 36
⤷ pKi <5.0 (Ki >1x10-5 M) [36]
istradefylline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist <5.0 pKi 31
⤷ pKi <5.0 (Ki >1x10-5 M) [31]
caffeine Small molecule or natural product Approved drug Ligand has a PDB structure Mm Antagonist 4.9 pKi 12
⤷ pKi 4.9 (Ki 1.3x10-5 M) [12]
caffeine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 4.5 – 5.0 pKi 6,10,44
⤷ pKi 4.5 – 5.0 (Ki 3.38x10-5 – 1.04x10-5 M) [6,10,44]
theophylline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 4.1 – 5.0 pKi 6,27,44,73
⤷ pKi 4.1 – 5.0 (Ki 7.4x10-5 – 9.07x10-6 M) [6,27,44,73]
caffeine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 4.5 pKi 12
⤷ pKi 4.5 (Ki 3x10-5 M) [12]
BAY-545 Small molecule or natural product Rn Antagonist 6.6 pIC50 35
⤷ pIC50 6.6 (IC50 2.8x10-7 M) [35]
BAY-545 Small molecule or natural product Mm Antagonist 6.4 pIC50 35
⤷ pIC50 6.4 (IC50 4x10-7 M) [35]
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:   CD4-positive, alpha-beta T cell (CL:0000624)
CD8-positive, alpha-beta T cell (CL:0000625)
type I NK T cell (CL:0000921)
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:  55,59
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
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  26,50
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  26,50
Tissue Distribution Click here for help
Low levels found in the brain, heart, kidney and lung.
Species:  Human
Technique:  Northern blotting.
References:  65
Jejunum, ileum, colon.
Species:  Human
Technique:  RT-PCR.
References:  15
Bronchial smooth muscle cells.
Species:  Human
Technique:  RT-PCR.
References:  82
Large intestine, cecum, urinary bladder.
Species:  Human
Technique:  Northern blotting.
References:  69
Type II epithelial cells
Species:  Mouse
Technique:  Reporter gene
References:  14
Bone marrow-derived mast cells.
Species:  Mouse
Technique:  in situ hybridisation.
References:  52
Kidney: cortical tubular structures.
Species:  Mouse
Technique:  RNAse protection and RT-PCR.
References:  76
Hypophyseal pars tuberalis.
Species:  Rat
Technique:  in situ hybridisation.
References:  69
Kidney: cortical tubular structures.
Species:  Rat
Technique:  RNAse protection and RT-PCR.
References:  76
Expression Datasets Click here for help

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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 Click here for help
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:  11,63
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:  50
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:  50
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:  69
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:  67
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:  82
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:  26,53
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:  71
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:  18
Physiological Functions Click here for help
Coronary vasodilation.
Species:  Rat
Tissue:  Heart.
References:  34
Vasodilation.
Species:  Human
Tissue:  Small coronary arteries.
References:  41
Vasoconstriction.
Species:  Human
Tissue:  Chorionic vessels.
References:  17
Inhibition of macrophage proliferation.
Species:  Mouse
Tissue:  Bone marrow-derived macrophages.
References:  79
Cytokine production.
Species:  Mouse
Tissue:  Macrophages.
References:  60
Cytokine production.
Species:  Human
Tissue:  Bronchial smooth muscle cells.
References:  82
Inhibition of cell proliferation.
Species:  Human
Tissue:  Glomerular mesangial cells.
References:  19
Inhibition of cell proliferation.
Species:  Rat
Tissue:  Glomerular mesangial cells.
References:  19
Regulation of cerebral blood flow (vasodilation).
Species:  Rat
Tissue:  Cerebral cortex.
References:  58
Regulation of coronary flow.
Species:  Mouse
Tissue:  Heart.
References:  72
Physiological Consequences of Altering Gene Expression Click here for help
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:  81
A2B receptor KO mice show increased vascular leakiness.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  21
Phenotypes, Alleles and Disease Models Click here for help 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 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J		 MGI:99403  MP:0008752 abnormal tumor necrosis factor level PMID: 16823489 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
involves: 129P2/OlaHsd		 MGI:99403  MP:0000343 altered response to myocardial infarction PMID: 17353435 
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b		 MGI:99403  MP:0005534 decreased body temperature PMID: 17200408 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J		 MGI:99403  MP:0008661 decreased interleukin-10 secretion PMID: 16823489 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
B6.129P2-Adora2b		 MGI:99403  MP:0008661 decreased interleukin-10 secretion PMID: 17525287 
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b		 MGI:99403  MP:0008874 decreased physiological sensitivity to xenobiotic PMID: 17200408 
Adora2btm1Kra Adora2btm1Kra/Adora2btm1Kra
involves: 129/Sv * C57BL/6J		 MGI:99403  MP:0008596 increased circulating interleukin-6 level PMID: 16823489 
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b		 MGI:99403  MP:0008705 increased interleukin-6 secretion PMID: 17200408 
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b		 MGI:99403  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 17200408 
Adora2btm1Till Adora2btm1Till/Adora2btm1Till
B6.129P2-Adora2b		 MGI:99403  MP:0005596 increased susceptibility to type I hypersensitivity reaction PMID: 17200408 
Adora2btm1Dgen Adora2btm1Dgen/Adora2btm1Dgen
B6.129P2-Adora2b		 MGI:99403  MP:0003070 increased vascular permeability PMID: 18056839 
General Comments
For a review of the effects of adenosine receptor knockout on nervous system function see reference [30].

References

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