Gene and Protein Information
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

adenosine receptor A2b | A2b | A2BR

Database Links
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
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 Value Parameter Reference BAY 60-6583 Hs Agonist 8.0 – 8.5 pKi 22 ⤷ pKi 8.0 – 8.5 (Ki 1x10-8 – 3x10-9 M) [22] 2-hexynyl-NECA Hs Full agonist 6.6 pKi 73 ⤷ pKi 6.6 [73] BAY 60-6583 Mm Agonist 6.5 pKi 48 ⤷ pKi 6.5 (Ki 3.3x10-7 M) [48] NECA 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 Mm Agonist 5.7 pKi 51 ⤷ pKi 5.7 (Ki 1.9x10-6 M) [51] adenosine Rn Agonist 5.3 pKi 80 ⤷ pKi 5.3 (Ki 5.1x10-6 M) [80] CGS 21680 Rn Agonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] Cl-IB-MECA Hs Agonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] Cl-IB-MECA Mm Agonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] TCPA Hs Agonist <5.0 pKi 8 ⤷ pKi <5.0 (Ki >1x10-5 M) [8] regadenoson Hs Agonist <5.0 pKi 36 ⤷ pKi <5.0 (Ki >1x10-5 M) [36] MRS3558 Hs Agonist <5.0 pKi 36 ⤷ pKi <5.0 (Ki >1x10-5 M) [36] adenosine Hs Agonist 4.8 pKi 29-30,80 ⤷ pKi 4.8 (Ki 1.5x10-5 M) [29-30,80] 2-chloroadenosine Hs Full agonist 4.6 – 5.0 pKi 7,13,50 ⤷ pKi 4.6 – 5.0 [7,13,50] (R)-PIA Mm Agonist 4.7 pKi 12 ⤷ pKi 4.7 (Ki 1.9x10-5 M) [12] (S)-PIA Hs Full agonist 4.2 – 5.2 pKi 50,73 ⤷ pKi 4.2 – 5.2 [50,73] AB-NECA Hs Full agonist 4.7 pKi 50 ⤷ pKi 4.7 [50] (R)-PIA Hs Full agonist 3.8 – 5.5 pKi 7,13,37,50,73 ⤷ pKi 3.8 – 5.5 [7,13,37,50,73] piclidenoson Hs Full agonist 4.3 – 4.9 pKi 36,50 ⤷ pKi 4.3 – 4.9 [36,50] cyclopentyladenosine Hs Full agonist 4.5 – 4.7 pKi 36,50 ⤷ pKi 4.5 – 4.7 [36,50] CCPA Hs Full agonist 4.4 – 4.7 pKi 36,50 ⤷ pKi 4.4 – 4.7 [36,50] HEMADO Hs Agonist <4.5 pKi 46,77 ⤷ pKi <4.5 (Ki >3x10-5 M) [46,77] GS9667 Hs Agonist <4.3 pKi 25 ⤷ pKi <4.3 (Ki >5x10-5 M) [25] CGS 21680 Hs Full agonist 3.4 – 5.0 pKi 7,36,50 ⤷ pKi 3.4 – 5.0 [7,36,50] N(6)-cyclohexyladenosine Hs Agonist 3.8 pKi 13 ⤷ pKi 3.8 (Ki 1.6x10-4 M) [13] binodenoson 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 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 37 ⤷ pKd 9.8 (Kd 1.58x10-10 M) [37] [3H]OSIP339391 Hs Antagonist 9.8 pKd 70 ⤷ pKd 9.8 [70] [3H]PSB603 Mm Antagonist 9.5 pKd 10 ⤷ pKd 9.5 [10] PSB603 Mm Antagonist 9.4 pKd 10 ⤷ pKd 9.4 (Kd 3.51x10-10 M) [10] [3H]PSB603 Hs Antagonist 9.4 pKd 10 ⤷ pKd 9.4 [10] PSB603 Hs Antagonist 9.4 pKd 10 ⤷ pKd 9.4 (Kd 4.03x10-10 M) [10] [3H]DPCPX Hs Antagonist 7.4 pKd 70 ⤷ pKd 7.4 [70] [125I]ABOPX Hs Antagonist 7.4 pKd 50 ⤷ pKd 7.4 [50] [3H]ZM 241385 Hs Antagonist 6.5 – 7.9 pKd 27,38,70 ⤷ pKd 6.5 – 7.9 [27,38,70] PSB-0788 Hs Antagonist 9.4 pKi 10 ⤷ pKi 9.4 [10] OSIP339391 Hs Antagonist 9.3 pKi 70 ⤷ pKi 9.3 [70] PSB603 Hs Antagonist 9.3 pKi 10 ⤷ pKi 9.3 (Ki 5.53x10-10 M) [10] MRS1706 ? Antagonist 8.9 pKi 45 ⤷ pKi 8.9 [45] MRS1754 Hs Antagonist 8.8 pKi 37,45 ⤷ pKi 8.8 (Ki 1.58x10-9 M) [37,45] ATL802 Hs Antagonist 8.6 pKi 45 ⤷ pKi 8.6 (Ki 2.36x10-9 M) [45] MRS1754 Mm Antagonist 8.5 pKi 4 ⤷ pKi 8.5 (Ki 3.39x10-9 M) [4] ISAM-140 Hs Antagonist 8.5 pKi 23 ⤷ pKi 8.5 (Ki 3.49x10-9 M) [23] AS99 Hs Antagonist 8.4 pKi 73 ⤷ pKi 8.4 [73] AS101 Hs Antagonist 8.4 pKi 73 ⤷ pKi 8.4 [73] MRE 2029F20 Hs Antagonist 8.3 – 8.5 pKi 5,73 ⤷ pKi 8.3 – 8.5 [5,73] AS100 Hs Antagonist 8.2 pKi 73 ⤷ pKi 8.2 [73] AS70 Hs Antagonist 8.1 pKi 73 ⤷ pKi 8.1 [73] ATL802 Mm Antagonist 8.1 pKi 45 ⤷ pKi 8.1 (Ki 8.58x10-9 M) [45] CGS 15943 Mm Antagonist 8.0 pKi 4 ⤷ pKi 8.0 (Ki 9.07x10-9 M) [4] AS96 Hs Antagonist 8.0 pKi 73 ⤷ pKi 8.0 [73] DEPX Hs Antagonist 7.9 pKi 50 ⤷ pKi 7.9 [50] xanthine amine congener 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 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 Hs Antagonist 7.8 pKi 73 ⤷ pKi 7.8 [73] LAS38096 Hs Antagonist 7.8 pKi 20,75 ⤷ pKi 7.8 (Ki 1.7x10-8 M) [20,75] AS16 Hs Antagonist 7.7 pKi 73 ⤷ pKi 7.7 [73] AS95 Hs Antagonist 7.7 pKi 73 ⤷ pKi 7.7 [73] CVT-6883 Hs Antagonist 7.7 pKi 24 ⤷ pKi 7.7 (Ki 2.2x10-8 M) [24] AS74 Hs Antagonist 7.6 pKi 73 ⤷ pKi 7.6 [73] ZM-241385 Hs Antagonist 6.8 – 8.2 pKi 7,37,50,70 ⤷ pKi 6.8 – 8.2 [7,37,50,70] I-ABOPX Hs Antagonist 7.4 pKi 50 ⤷ pKi 7.4 [50] CPX Hs Antagonist 7.3 pKi 37,50 ⤷ pKi 7.3 [37,50] BW-A1433 Hs Antagonist 7.3 pKi 50 ⤷ pKi 7.3 [50] XCC Hs Antagonist 7.3 pKi 37 ⤷ pKi 7.3 [37] PSB1115 Hs Antagonist 7.3 pKi 33 ⤷ pKi 7.3 (Ki 5.34x10-8 M) [33] vipadenant Hs Antagonist 7.2 pKi 32 ⤷ pKi 7.2 (Ki 6.3x10-8 M) [32] imaradenant 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 Hs Antagonist 6.9 – 7.3 pKi 44,61,70,78 ⤷ pKi 6.9 – 7.3 [44,61,70,78] 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 4,37-38,47,62,70 ⤷ pKi 6.0 – 8.1 [4,37-38,47,62,70] tonapofylline Hs Antagonist 7.1 pKi 42 ⤷ pKi 7.1 (Ki 9x10-8 M) [42] BAY-545 Hs Antagonist 7.0 pKi 35 ⤷ pKi 7.0 (Ki 9.7x10-8 M) [35] PSB36 Hs Antagonist 6.7 pKi 43 ⤷ pKi 6.7 (Ki 1.87x10-7 M) [43] DPCPX Rn Antagonist 6.7 – 6.7 pKi 28,44 ⤷ pKi 6.7 – 6.7 (Ki 2x10-7 – 1.86x10-7 M) [28,44] rolofylline Hs Antagonist 6.5 pKi 42 ⤷ pKi 6.5 (Ki 2.96x10-7 M) [42] LUF5981 Hs Antagonist <6.5 pKi 40 ⤷ pKi <6.5 (Ki >3x10-7 M) [40] MRS1220 Hs Antagonist 6.5 pKi 70 ⤷ pKi 6.5 [70] ST-1535 Hs Antagonist 6.4 pKi 54 ⤷ pKi 6.4 (Ki 3.523x10-7 M) [54] DAX Hs Antagonist 6.4 pKi 37 ⤷ pKi 6.4 [37] 3-isobutyl-8-pyrrolidinoxanthine Hs Antagonist 6.3 pKi 27 ⤷ pKi 6.3 [27] derenofylline Rn Antagonist 6.3 pKi 39 ⤷ pKi 6.3 (Ki 5.01x10-7 M) [39] SCH 58261 Hs Antagonist 6.0 – 6.5 pKi 7,36 ⤷ pKi 6.0 – 6.5 [7,36] KF26777 Hs Antagonist 6.2 pKi 64 ⤷ pKi 6.2 (Ki 6.2x10-7 M) [64] FK-453 Hs Antagonist 6.0 pKi 36 ⤷ pKi 6.0 (Ki 9.8x10-7 M) [36] alloxazine Hs Antagonist 5.7 – 6.3 pKi 37-38 ⤷ pKi 5.7 – 6.3 [37-38] preladenant Hs Antagonist <6.0 pKi 56 ⤷ pKi <6.0 (Ki >1x10-6 M) [56] MRE 3008F20 Hs Antagonist 5.7 – 5.8 pKi 36,73-74 ⤷ pKi 5.7 – 5.8 [36,73-74] PSB-10 Mm Antagonist 5.7 pKi 57 ⤷ pKi 5.7 (Ki 2.1x10-6 M) [57] PSB-11 Mm Antagonist 5.7 pKi 57 ⤷ pKi 5.7 (Ki 2.1x10-6 M) [57] derenofylline Hs Antagonist 5.4 pKi 39 ⤷ pKi 5.4 (Ki 3.981x10-6 M) [39] pentoxifylline Hs Antagonist 5.3 pKi 44 ⤷ pKi 5.3 (Ki 5.18x10-6 M) [44] MSX-2 Hs Antagonist 5.0 – 5.5 pKi 66,68 ⤷ pKi 5.0 – 5.5 (Ki 1x10-5 – 2.9x10-6 M) [66,68] theophylline Mm Antagonist 5.3 pKi 4 ⤷ pKi 5.3 (Ki 5.63x10-6 M) [4] CSC Rn Antagonist 5.1 pKi 16 ⤷ pKi 5.1 (Ki 8.2x10-6 M) [16] MRS1191 Hs Antagonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] MRS1523 Hs Antagonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] MRS1523 Mm Antagonist <5.0 pKi 49 ⤷ pKi <5.0 (Ki >1x10-5 M) [49] SCH442416 Hs Antagonist <5.0 pKi 36 ⤷ pKi <5.0 (Ki >1x10-5 M) [36] istradefylline Hs Antagonist <5.0 pKi 31 ⤷ pKi <5.0 (Ki >1x10-5 M) [31] caffeine Mm Antagonist 4.9 pKi 12 ⤷ pKi 4.9 (Ki 1.3x10-5 M) [12] caffeine 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 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 Rn Antagonist 4.5 pKi 12 ⤷ pKi 4.5 (Ki 3x10-5 M) [12] BAY-545 Rn Antagonist 6.6 pIC50 35 ⤷ pIC50 6.6 (IC50 2.8x10-7 M) [35] BAY-545 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
Transducer	Effector/Response
Gs family	Adenylyl cyclase stimulation
References:  26,50

Secondary Transduction Mechanisms
Transducer	Effector/Response
Gq/G11 family	Phospholipase C stimulation
References:  26,50

Tissue Distribution
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
Show »« Hide 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] There should be a chart of expression data here, you may need to enable JavaScript!

Functional Assays
Measurement of cAMP levels in CHO cells transfected with the human A2B receptor.