Nomenclature: A3 receptor

Family: Adenosine receptors

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

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 318 1p13.2 ADORA3 adenosine A3 receptor 1,64,73,76
Mouse 7 319 3 F2.3 Adora3 adenosine A3 receptor 100
Rat 7 320 2q34 Adora3 adenosine A3 receptor 104
Previous and Unofficial Names
adenosine A3 receptor
Adenosine receptor A3
TGPCR1
ARA3
A3AR
A3R
AA3R
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
adenosine
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]AB-MECA Hs Full agonist 9.0 – 9.1 pKd 69,90
pKd 9.0 – 9.1 (Kd 6x10-10 – 1x10-9 M) [69,90]
[3H]HEMADO Hs Full agonist 9.0 pKd 53
pKd 9.0 [53]
[125I]AB-MECA Rn Full agonist 8.9 pKd 68
pKd 8.9 [68]
[3H]NECA Hs Full agonist 7.9 – 8.2 pKd 25,52
pKd 7.9 – 8.2 [25,52]
[125I]APNEA Hs Full agonist 7.8 pKd 104
pKd 7.8 [104]
Cl-IB-MECA Mm Agonist 9.74 pKi 57
pKi 9.74 (Ki 1.8x10-10 M) [57]
MRS3558 Hs Agonist 9.54 pKi 43
pKi 9.54 (Ki 2.9x10-10 M) [43]
Cl-IB-MECA Rn Agonist 9.48 pKi 57
pKi 9.48 (Ki 3.3x10-10 M) [57]
(R,S)-PHPNECA Hs Full agonist 9.4 pKi 93
pKi 9.4 [93]
2-phenylethylyl-adenosine derivative Hs Agonist 9.36 pKi 92
pKi 9.36 (Ki 4.4x10-10 M) [92]
MRS3558 Rn Agonist 9.0 pKi 57
pKi 9.0 (Ki 1x10-9 M) [57]
HEMADO Hs Agonist 8.96 pKi 53,93
pKi 8.96 (Ki 1.1x10-9 M) [53,93]
IB-MECA Hs Full agonist 8.7 – 9.2 pKi 25,31,52,90
pKi 8.7 – 9.2 [25,31,52,90]
MRS3558 Mm Agonist 8.83 pKi 57
pKi 8.83 (Ki 1.49x10-9 M) [57]
MRS5151 Hs Agonist 8.62 pKi 62
pKi 8.62 (Ki 2.38x10-9 M) [62]
2-hexynyl-NECA Hs Full agonist 8.6 pKi 93
pKi 8.6 [93]
Cl-IB-MECA Hs Full agonist 8.0 – 8.9 pKi 10,44,49
pKi 8.0 – 8.9 [10,44,49]
CP608,039 Hs Agonist 8.24 pKi 84
pKi 8.24 (Ki 5.8x10-9 M) [84]
PENECA Hs Full agonist 8.2 pKi 93
pKi 8.2 [93]
MRE 3008F20 Hs Full agonist 8.0 pKi 90
pKi 8.0 [90]
I-ABA Hs Full agonist 8.0 pKi 76
pKi 8.0 [76]
NECA Hs Full agonist 7.5 – 8.4 pKi 9,32,44,76,90,96
pKi 7.5 – 8.4 [9,32,44,76,90,96]
AB-MECA Hs Full agonist 7.7 pKi 52,90
pKi 7.7 [52,90]
MRS5151 Mm Agonist 7.61 pKi 62
pKi 7.61 (Ki 2.44x10-8 M) [62]
(R)-PIA Hs Full agonist 7.1 – 8.1 pKi 32,44,52,76,90
pKi 7.1 – 8.1 [32,44,52,76,90]
CCPA Hs Full agonist 7.4 pKi 43,52
pKi 7.4 [43,52]
apadenoson Hs Agonist 7.35 pKi 43
pKi 7.35 (Ki 4.5x10-8 M) [43]
cyclopentyladenosine Hs Full agonist 7.0 – 7.4 pKi 32,43,52,76
pKi 7.0 – 7.4 [32,43,52,76]
(S)-PIA Hs Full agonist 6.3 – 7.4 pKi 52,76,90
pKi 6.3 – 7.4 [52,76,90]
MPC-MECA Hs Full agonist 6.8 pKi 90
pKi 6.8 [90]
N(6)-cyclohexyladenosine Rn Agonist 6.75 pKi 85
pKi 6.75 (Ki 1.76x10-7 M) [85]
NECA Rn Full agonist 6.6 – 6.9 pKi 60,68
pKi 6.6 – 6.9 [60,68]
(R)-PIA Rn Full agonist 6.6 – 6.8 pKi 16,68
pKi 6.6 – 6.8 [16,68]
CCPA Rn Agonist 6.63 pKi 57
pKi 6.63 (Ki 2.37x10-7 M) [57]
CGS 21680 Hs Full agonist 6.0 – 7.2 pKi 9,32,43,52,90
pKi 6.0 – 7.2 [9,32,43,52,90]
adenosine Hs Agonist 6.54 pKi 28-29,96
pKi 6.54 (Ki 2.9x10-7 M) [28-29,96]
CGS 21680 Rn Agonist 6.23 pKi 57
pKi 6.23 (Ki 5.84x10-7 M) [57]
TCPA Hs Agonist 6.22 pKi 6
pKi 6.22 (Ki 6x10-7 M) [6]
binodenoson Hs Agonist 6.04 pKi 43
pKi 6.04 (Ki 9.03x10-7 M) [43]
GS9667 Hs Agonist <6.0 pKi 22
pKi <6.0 (Ki >1x10-6 M) [22]
N(6)-cyclohexyladenosine Hs Agonist 5.99 pKi 74
pKi 5.99 (Ki 1.025x10-6 M) [74]
2-chloroadenosine Rn Agonist 5.72 pKi 85
pKi 5.72 (Ki 1.89x10-6 M) [85]
2'-Me-CCPA Rn Agonist 5.3 pKi 27
pKi 5.3 (Ki 5x10-6 M) [27]
adenosine Rn Agonist 5.19 pKi 96
pKi 5.19 (Ki 6.5x10-6 M) [96]
regadenoson Hs Agonist <5.0 pKi 43
pKi <5.0 (Ki >1x10-5 M) [43]
Bay60-6583 Hs Agonist <5.0 pKi 54
pKi <5.0 (Ki >1x10-5 M) [54]
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
[3H]MRE 3008F20 Hs Antagonist 9.1 pKd 4,90
pKd 9.1 [4,90]
PSB-11 Hs Antagonist 8.31 pKd 65
pKd 8.31 (Kd 4.9x10-9 M) [65]
[3H]PSB-11 Hs Antagonist 8.3 pKd 65
pKd 8.3 [65]
KF26777 Hs Antagonist 9.7 pKi 75
pKi 9.7 (Ki 2x10-10 M) [75]
PSB-10 Hs Antagonist 9.36 pKi 67
pKi 9.36 (Ki 4.41x10-10 M) [67]
MRE 3010F20 Hs Antagonist 9.3 pKi 90
pKi 9.3 [90]
MRE 3008F20 Hs Antagonist 9.0 – 9.5 pKi 43,89-90
pKi 9.0 – 9.5 [43,89-90]
MRS1220 Hs Antagonist 8.2 – 9.2 pKi 44,51,81,98
pKi 8.2 – 9.2 [44,51,81,98]
PSB-11 Hs Antagonist 8.63 pKi 70
pKi 8.63 (Ki 2.34x10-9 M) [70]
MRS1177 Hs Antagonist 8.5 pKi 51
pKi 8.5 [51]
VUF5574 Hs Antagonist 8.39 pKi 87
pKi 8.39 (Ki 4.03x10-9 M) [87]
MRS1505 Hs Antagonist 8.1 pKi 56
pKi 8.1 [56]
MRS1186 Hs Antagonist 8.1 pKi 51
pKi 8.1 [51]
VUF8504 Hs Antagonist 7.8 pKi 86
pKi 7.8 [86]
MRS1476 Hs Antagonist 7.7 pKi 56
pKi 7.7 [56]
MRS1523 Hs Antagonist 7.7 pKi 56
pKi 7.7 [56]
I-ABOPX Hs Antagonist 7.7 pKi 76
pKi 7.7 [76]
XAC Rn Antagonist 7.7 pKi 68
pKi 7.7 [68]
MRS1191 Hs Antagonist 7.5 pKi 44-45,57
pKi 7.5 [44-45,57]
MRS1486 Hs Antagonist 7.5 pKi 56
pKi 7.5 [56]
CGS 15943 Hs Antagonist 7.0 – 7.9 pKi 51-52,69,90
pKi 7.0 – 7.9 [51-52,69,90]
BW-A1433 Rn Antagonist 7.4 pKi 68
pKi 7.4 [68]
BW-A1433 Hs Antagonist 7.3 pKi 76
pKi 7.3 [76]
XAC Hs Antagonist 7.0 – 7.4 pKi 52,76,90
pKi 7.0 – 7.4 [52,76,90]
MRS1097 Hs Antagonist 7.0 pKi 44,88
pKi 7.0 [44,88]
MRS1523 Rn Antagonist 6.95 pKi 57
pKi 6.95 (Ki 1.13x10-7 M) [57]
VUF8507 Hs Antagonist 6.7 pKi 86
pKi 6.7 [86]
SLV320 Hs Antagonist 6.7 pKi 46
pKi 6.7 (Ki 2x10-7 M) [46]
MRS1042 Hs Antagonist 6.5 pKi 47
pKi 6.5 [47]
MRS1041 Hs Antagonist 6.4 pKi 47
pKi 6.4 [47]
MRS1754 Hs Antagonist 6.24 pKi 50
pKi 6.24 (Ki 5.7x10-7 M) [50]
LUF5981 Hs Antagonist 6.2 pKi 12
pKi 6.2 (Ki 6.37x10-7 M) [12]
MRS1067 Hs Antagonist 6.2 pKi 44,47
pKi 6.2 [44,47]
MRS1523 Mm Antagonist 6.14 pKi 57
pKi 6.14 (Ki 7.31x10-7 M) [57]
ZM-241385 Hs Antagonist 6.13 pKi 43
pKi 6.13 (Ki 7.43x10-7 M) [43]
MRS1088 Hs Antagonist 6.1 pKi 47
pKi 6.1 [47]
MRS1093 Hs Antagonist 6.1 pKi 47
pKi 6.1 [47]
DPCPX Hs Antagonist 5.4 – 6.61 pKi 2,37,52,76,90,94
pKi 5.4 – 6.61 (Ki 3.96x10-6 – 2.43x10-7 M) [2,37,52,76,90,94]
preladenant Hs Antagonist <6.0 pKi 66
pKi <6.0 (Ki >1x10-6 M) [66]
ST-1535 Hs Antagonist <6.0 pKi 63
pKi <6.0 (Ki >1x10-6 M) [63]
vipadenant Hs Antagonist 6.0 pKi 34
pKi 6.0 (Ki 1.005x10-6 M) [34]
MRE 2029F20 Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
ATL802 Hs Antagonist <6.0 pKi 50
pKi <6.0 (Ki >1x10-6 M) [50]
DPCPX Rn Antagonist 4.37 – 7.6 pKi 2,68,94
pKi 4.37 – 7.6 [2,68,94]
LAS38096 Hs Antagonist 5.98 pKi 20,91
pKi 5.98 (Ki 1.043x10-6 M) [20,91]
CVT-6883 Hs Antagonist 5.97 pKi 21
pKi 5.97 (Ki 1.07x10-6 M) [21]
SCH 58261 Hs Antagonist 5.92 pKi 43
pKi 5.92 (Ki 1.2x10-6 M) [43]
MRS928 Hs Antagonist 5.9 pKi 47
pKi 5.9 [47]
MRS1191 Rn Antagonist 5.8 pKi 56-57
pKi 5.8 [56-57]
dexniguldipine Hs Antagonist 5.7 pKi 88
pKi 5.7 [88]
PSB36 Hs Antagonist 5.64 pKi 94
pKi 5.64 (Ki 2.3x10-6 M) [94]
galangin Hs Antagonist 5.5 pKi 47
pKi 5.5 [47]
nicardipine Hs Antagonist 5.5 pKi 88
pKi 5.5 [88]
sakuranetin Hs Antagonist 5.5 pKi 47
pKi 5.5 [47]
rolofylline Hs Antagonist 5.36 pKi 48
pKi 5.36 (Ki 4.39x10-6 M) [48]
istradefylline Hs Antagonist 5.35 pKi 30
pKi 5.35 (Ki 4.47x10-6 M) [30]
PSB36 Rn Antagonist 5.19 pKi 94
pKi 5.19 (Ki 6.5x10-6 M) [94]
FK-453 Hs Antagonist 5.0 pKi 43
pKi 5.0 (Ki 1x10-5 M) [43]
tonapofylline Hs Antagonist <5.0 pKi 48
pKi <5.0 (Ki >1x10-5 M) [48]
PSB603 Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB1115 Hs Antagonist <5.0 pKi 37
pKi <5.0 (Ki >1x10-5 M) [37]
MSX-2 Hs Antagonist <5.0 pKi 78
pKi <5.0 (Ki >1x10-5 M) [78]
SCH442416 Hs Antagonist <5.0 pKi 43
pKi <5.0 (Ki >1x10-5 M) [43]
CSC Rn Antagonist <5.0 pKi 85
pKi <5.0 (Ki >1x10-5 M) [85]
ATL802 Mm Antagonist <5.0 pKi 50
pKi <5.0 (Ki >1x10-5 M) [50]
caffeine Hs Antagonist 4.88 pKi 41
pKi 4.88 (Ki 1.33x10-5 M) [41]
flavone Hs Antagonist 4.8 pKi 47
pKi 4.8 [47]
theophylline Hs Antagonist 4.06 – 4.65 pKi 41,52
pKi 4.06 – 4.65 (Ki 8.64x10-5 – 2.23x10-5 M) [41,52]
flavanone Hs Antagonist 4.3 pKi 47
pKi 4.3 [47]
visnagin Hs Antagonist 4.2 pKi 47
pKi 4.2 [47]
theophylline Rn Antagonist 4.0 – 4.07 pKi 42,85
pKi 4.0 – 4.07 (Ki 1x10-4 – 8.5x10-5 M) [42,85]
caffeine Rn Antagonist <4.0 pKi 8
pKi <4.0 (Ki >1x10-4 M) [8]
View species-specific antagonist tables
Antagonist Comments
Istradefylline pKi values at human receptor subtypes A1, A2B and A3 are derived from unpublished data (Müller et al).
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  71,104
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Phospholipase C stimulation
References:  58,103
Tissue Distribution
Liver, lung, placenta.
Species:  Human
Technique:  Northern blotting.
References:  64
Adrenal cortex, adrenal medulla > spleen, small intestine.
Species:  Human
Technique:  Northern blotting.
References:  1
Jejunum, ileum, colon.
Species:  Human
Technique:  RT-PCR.
References:  14
Lung, liver, kidney, heart.
Species:  Human
Technique:  Northern blotting.
References:  73
Liver, lung > brain, aorta.
Species:  Human
Technique:  Northern blotting.
References:  76
CNS: corpus callosum, substantia nigra, thalamus, subthalamic nucleus, spinal cord, hippocampus.
Species:  Human
Technique:  Northern blotting.
References:  1
Lung mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  103
Brain: hippocampus.
Species:  Rat
Technique:  Western blotting.
References:  59
Testes: spermatocytes, round spermatids, elongating spermatids > Leydig cells.
Species:  Rat
Technique:  in situ hybridisation.
References:  72
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 IP3 levels in HEK 293 cells transfected with the human A3 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  PTX-sensitive increase in IP3 level.
References:  58
Measurement of cAMP levels in CHO cells transfected with the human A3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP accumulation.
References:  76
Measurement of cAMP levels in COS cells transfected with the rat A3 receptor.
Species:  Rat
Tissue:  COS cells.
Response measured:  PTX-sensitive inhibition of cAMP accumulation.
References:  104
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:  36,79
Measurement of cAMP levels and p42/p44 MAPK phosphorylation in a murine dendritic cell line, XS-106, which endogenously expresses A3 receptors.
Species:  Mouse
Tissue:  XS-106 cells.
Response measured:  Inhibition of cAMP and stimulation of p42/p44 MAPK phosphorylation.
References:  18
Measurement of PKB activity in cardiomyocytes endogenously expressing the A3 receptor.
Species:  Rat
Tissue:  Cardiomyocytes.
Response measured:  PKB phosphorylation via Gi/o.
References:  33
Cell number count of CHO cells transfected with the human A3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Reduction of cell number.
References:  10
Measurement of eosinophil peroxidase and superoxide anion release from human eosinophils endogenously expressing the human A3 receptor.
Species:  Human
Tissue:  Eosinophils.
Response measured:  Release of of eosinophil peroxidase and superoxide anion .
References:  23
Physiological Functions
Preconditioning.
Species:  Rat
Tissue:  Heart.
References:  17
Mast cell activation.
Species:  Mouse
Tissue:  Lung mast cells.
References:  103
Inhibition of noradrenaline release from peripheral sympathetic nerve terminals.
Species:  Rat
Tissue:  Mesenteric artery.
References:  19
Coronary vasodilation.
Species:  Rat
Tissue:  Heart.
References:  38
Protection from reperfusion/reoxygenation injury.
Species:  Rat
Tissue:  Heart.
References:  61
Localised inflammatory response in peripheral tissues.
Species:  Mouse
Tissue:  In vivo (hind paw).
References:  95
Regulation of intraocular pressure.
Species:  Mouse
Tissue:  In vivo (eye).
References:  3
Preconditioning.
Species:  Mouse
Tissue:  Heart.
References:  99
Modulation of synaptic plasticity.
Species:  Rat
Tissue:  Hippocampus.
References:  15
Modulation of ischemia/reperfusion injury.
Species:  Mouse
Tissue:  In vivo.
References:  11,35
Hypotension.
Species:  Rat
Tissue:  In vivo.
References:  80
Mast cell degranulation.
Species:  Rat
Tissue:  Mast cells.
References: