A3 receptor

Target id: 21

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.  » Email us

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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 1,66,75,78
Mouse 7 319 3 F2.3 Adora3 adenosine A3 receptor 104
Rat 7 320 2q34 Adora3 adenosine A3 receptor 108
Previous and Unofficial Names
Adenosine receptor A3 | TGPCR1 | A3AR | ARA3
Database Links
Specialist databases
GPCRDB aa3r_human (Hs), aa3r_mouse (Mm), aa3r_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
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
[125I]AB-MECA Hs Full agonist 9.0 – 9.1 pKd 71,93
pKd 9.0 – 9.1 (Kd 1x10-9 – 6x10-10 M) [71,93]
[3H]HEMADO Hs Full agonist 9.0 pKd 55
pKd 9.0 [55]
[125I]AB-MECA Rn Full agonist 8.9 pKd 70
pKd 8.9 [70]
[3H]NECA Hs Full agonist 7.9 – 8.2 pKd 25,54
pKd 7.9 – 8.2 [25,54]
[125I]APNEA Hs Full agonist 7.8 pKd 108
pKd 7.8 [108]
Cl-IB-MECA Mm Agonist 9.7 pKi 59
pKi 9.7 (Ki 1.8x10-10 M) [59]
MRS3558 Hs Agonist 9.5 pKi 45
pKi 9.5 (Ki 2.9x10-10 M) [45]
Cl-IB-MECA Rn Agonist 9.5 pKi 59
pKi 9.5 (Ki 3.3x10-10 M) [59]
(R,S)-PHPNECA Hs Full agonist 9.4 pKi 97
pKi 9.4 [97]
2-phenylethylyl-adenosine derivative Hs Agonist 9.4 pKi 96
pKi 9.4 (Ki 4.4x10-10 M) [96]
MRS3558 Rn Agonist 9.0 pKi 59
pKi 9.0 (Ki 1x10-9 M) [59]
HEMADO Hs Agonist 9.0 pKi 55,97
pKi 9.0 (Ki 1.1x10-9 M) [55,97]
piclidenoson Hs Full agonist 8.7 – 9.2 pKi 25,31,54,93
pKi 8.7 – 9.2 [25,31,54,93]
MRS3558 Mm Agonist 8.8 pKi 59
pKi 8.8 (Ki 1.49x10-9 M) [59]
MRS5151 Hs Agonist 8.6 pKi 64
pKi 8.6 (Ki 2.38x10-9 M) [64]
2-hexynyl-NECA Hs Full agonist 8.6 pKi 97
pKi 8.6 [97]
MRS5698 Hs Agonist 8.5 pKi 86
pKi 8.5 [86]
Cl-IB-MECA Hs Full agonist 8.0 – 8.9 pKi 10,46,51
pKi 8.0 – 8.9 [10,46,51]
CP608,039 Hs Agonist 8.2 pKi 87
pKi 8.2 (Ki 5.8x10-9 M) [87]
PENECA Hs Full agonist 8.2 pKi 97
pKi 8.2 [97]
I-ABA Hs Full agonist 8.0 pKi 78
pKi 8.0 [78]
MRE 3008F20 Hs Full agonist 8.0 pKi 93
pKi 8.0 [93]
NECA Hs Full agonist 7.5 – 8.4 pKi 9,32,46,78,93,100
pKi 7.5 – 8.4 [9,32,46,78,93,100]
AB-MECA Hs Full agonist 7.7 pKi 54,93
pKi 7.7 [54,93]
MRS5151 Mm Agonist 7.6 pKi 64
pKi 7.6 (Ki 2.44x10-8 M) [64]
(R)-PIA Hs Full agonist 7.1 – 8.1 pKi 32,46,54,78,93
pKi 7.1 – 8.1 [32,46,54,78,93]
CCPA Hs Full agonist 7.4 pKi 45,54
pKi 7.4 [45,54]
apadenoson Hs Agonist 7.3 pKi 45
pKi 7.3 (Ki 4.5x10-8 M) [45]
cyclopentyladenosine Hs Full agonist 7.0 – 7.4 pKi 32,45,54,78
pKi 7.0 – 7.4 [32,45,54,78]
(S)-PIA Hs Full agonist 6.3 – 7.4 pKi 54,78,93
pKi 6.3 – 7.4 [54,78,93]
MPC-MECA Hs Full agonist 6.8 pKi 93
pKi 6.8 [93]
NECA Rn Full agonist 6.6 – 6.9 pKi 62,70
pKi 6.6 – 6.9 [62,70]
N(6)-cyclohexyladenosine Rn Agonist 6.8 pKi 88
pKi 6.8 (Ki 1.76x10-7 M) [88]
(R)-PIA Rn Full agonist 6.6 – 6.8 pKi 16,70
pKi 6.6 – 6.8 [16,70]
CCPA Rn Agonist 6.6 pKi 59
pKi 6.6 (Ki 2.37x10-7 M) [59]
CGS 21680 Hs Full agonist 6.0 – 7.2 pKi 9,32,45,54,93
pKi 6.0 – 7.2 [9,32,45,54,93]
adenosine Hs Agonist 6.5 pKi 28-29,100
pKi 6.5 (Ki 2.9x10-7 M) [28-29,100]
CGS 21680 Rn Agonist 6.2 pKi 59
pKi 6.2 (Ki 5.84x10-7 M) [59]
TCPA Hs Agonist 6.2 pKi 6
pKi 6.2 (Ki 6x10-7 M) [6]
binodenoson Hs Agonist 6.0 pKi 45
pKi 6.0 (Ki 9.03x10-7 M) [45]
GS9667 Hs Agonist <6.0 pKi 22
pKi <6.0 (Ki >1x10-6 M) [22]
N(6)-cyclohexyladenosine Hs Agonist 6.0 pKi 76
pKi 6.0 (Ki 1.025x10-6 M) [76]
2-chloroadenosine Rn Agonist 5.7 pKi 88
pKi 5.7 (Ki 1.89x10-6 M) [88]
2'-Me-CCPA Rn Agonist 5.3 pKi 27
pKi 5.3 (Ki 5x10-6 M) [27]
adenosine Rn Agonist 5.2 pKi 100
pKi 5.2 (Ki 6.5x10-6 M) [100]
BAY 60-6583 Hs Agonist <5.0 pKi 56
pKi <5.0 (Ki >1x10-5 M) [56]
regadenoson Hs Agonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
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 4,93
pKd 9.1 [4,93]
PSB-11 Hs Antagonist 8.3 pKd 67
pKd 8.3 (Kd 4.9x10-9 M) [67]
[3H]PSB-11 Hs Antagonist 8.3 pKd 67
pKd 8.3 [67]
KF26777 Hs Antagonist 9.7 pKi 77
pKi 9.7 (Ki 2x10-10 M) [77]
PSB-10 Hs Antagonist 9.4 pKi 69
pKi 9.4 (Ki 4.41x10-10 M) [69]
MRE 3010F20 Hs Antagonist 9.3 pKi 93
pKi 9.3 [93]
MRE 3008F20 Hs Antagonist 9.0 – 9.5 pKi 45,92-93
pKi 9.0 – 9.5 [45,92-93]
MRS1220 Hs Antagonist 8.2 – 9.2 pKi 46,53,83,102
pKi 8.2 – 9.2 (Ki 6.31x10-9 – 6.3x10-10 M) [46,53,83,102]
PSB-11 Hs Antagonist 8.6 pKi 72
pKi 8.6 (Ki 2.34x10-9 M) [72]
MRS1177 Hs Antagonist 8.5 pKi 53
pKi 8.5 [53]
VUF5574 Hs Antagonist 8.4 pKi 90
pKi 8.4 (Ki 4.03x10-9 M) [90]
MRS1186 Hs Antagonist 8.1 pKi 53
pKi 8.1 [53]
MRS1505 Hs Antagonist 8.1 pKi 58
pKi 8.1 [58]
VUF8504 Hs Antagonist 7.8 pKi 89
pKi 7.8 [89]
xanthine amine congener Rn Antagonist 7.7 pKi 70
pKi 7.7 [70]
I-ABOPX Hs Antagonist 7.7 pKi 78
pKi 7.7 [78]
MRS1476 Hs Antagonist 7.7 pKi 58
pKi 7.7 [58]
MRS1523 Hs Antagonist 7.7 pKi 58
pKi 7.7 (Ki 1.99x10-8 M) [58]
MRS1191 Hs Antagonist 7.5 pKi 46-47,59
pKi 7.5 [46-47,59]
MRS1486 Hs Antagonist 7.5 pKi 58
pKi 7.5 [58]
CGS 15943 Hs Antagonist 7.0 – 7.9 pKi 53-54,71,93
pKi 7.0 – 7.9 [53-54,71,93]
BW-A1433 Rn Antagonist 7.4 pKi 70
pKi 7.4 [70]
BW-A1433 Hs Antagonist 7.3 pKi 78
pKi 7.3 [78]
xanthine amine congener Hs Antagonist 7.0 – 7.4 pKi 54,78,93
pKi 7.0 – 7.4 [54,78,93]
MRS1097 Hs Antagonist 7.0 pKi 46,91
pKi 7.0 [46,91]
MRS1523 Rn Antagonist 6.9 pKi 59
pKi 6.9 (Ki 1.13x10-7 M) [59]
VUF8507 Hs Antagonist 6.7 pKi 89
pKi 6.7 [89]
derenofylline Hs Antagonist 6.7 pKi 48
pKi 6.7 (Ki 2x10-7 M) [48]
MRS1042 Hs Antagonist 6.5 pKi 49
pKi 6.5 [49]
MRS1041 Hs Antagonist 6.4 pKi 49
pKi 6.4 [49]
MRS1754 Hs Antagonist 6.2 pKi 52
pKi 6.2 (Ki 5.7x10-7 M) [52]
MRS1067 Hs Antagonist 6.2 pKi 46,49
pKi 6.2 [46,49]
LUF5981 Hs Antagonist 6.2 pKi 12
pKi 6.2 (Ki 6.37x10-7 M) [12]
MRS1523 Mm Antagonist 6.1 pKi 59
pKi 6.1 (Ki 7.31x10-7 M) [59]
ZM-241385 Hs Antagonist 6.1 pKi 45
pKi 6.1 (Ki 7.43x10-7 M) [45]
MRS1093 Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
MRS1088 Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
DPCPX Hs Antagonist 5.4 – 6.6 pKi 2,38,54,78,93,98
pKi 5.4 – 6.6 (Ki 3.96x10-6 – 2.43x10-7 M) [2,38,54,78,93,98]
MRE 2029F20 Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
vipadenant Hs Antagonist 6.0 pKi 34
pKi 6.0 (Ki 1.005x10-6 M) [34]
ST-1535 Hs Antagonist <6.0 pKi 65
pKi <6.0 (Ki >1x10-6 M) [65]
preladenant Hs Antagonist <6.0 pKi 68
pKi <6.0 (Ki >1x10-6 M) [68]
ATL802 Hs Antagonist <6.0 pKi 52
pKi <6.0 (Ki >1x10-6 M) [52]
DPCPX Rn Antagonist 4.4 – 7.6 pKi 2,70,98
pKi 4.4 – 7.6 [2,70,98]
LAS38096 Hs Antagonist 6.0 pKi 20,95
pKi 6.0 (Ki 1.043x10-6 M) [20,95]
CVT-6883 Hs Antagonist 6.0 pKi 21
pKi 6.0 (Ki 1.07x10-6 M) [21]
SCH 58261 Hs Antagonist 5.9 pKi 45
pKi 5.9 (Ki 1.2x10-6 M) [45]
MRS928 Hs Antagonist 5.9 pKi 49
pKi 5.9 [49]
MRS1191 Rn Antagonist 5.8 pKi 58-59
pKi 5.8 [58-59]
dexniguldipine Hs Antagonist 5.7 pKi 91
pKi 5.7 [91]
PSB36 Hs Antagonist 5.6 pKi 98
pKi 5.6 (Ki 2.3x10-6 M) [98]
galangin Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
sakuranetin Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
nicardipine Hs Antagonist 5.5 pKi 91
pKi 5.5 [91]
rolofylline Hs Antagonist 5.4 pKi 50
pKi 5.4 (Ki 4.39x10-6 M) [50]
istradefylline Hs Antagonist 5.3 pKi 30
pKi 5.3 (Ki 4.47x10-6 M) [30]
PSB36 Rn Antagonist 5.2 pKi 98
pKi 5.2 (Ki 6.5x10-6 M) [98]
SCH442416 Hs Antagonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
PSB603 Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB1115 Hs Antagonist <5.0 pKi 38
pKi <5.0 (Ki >1x10-5 M) [38]
tonapofylline Hs Antagonist <5.0 pKi 50
pKi <5.0 (Ki >1x10-5 M) [50]
FK-453 Hs Antagonist 5.0 pKi 45
pKi 5.0 (Ki 1x10-5 M) [45]
CSC Rn Antagonist <5.0 pKi 88
pKi <5.0 (Ki >1x10-5 M) [88]
MSX-2 Hs Antagonist <5.0 pKi 80
pKi <5.0 (Ki >1x10-5 M) [80]
ATL802 Mm Antagonist <5.0 pKi 52
pKi <5.0 (Ki >1x10-5 M) [52]
caffeine Hs Antagonist 4.9 pKi 43
pKi 4.9 (Ki 1.33x10-5 M) [43]
flavone Hs Antagonist 4.8 pKi 49
pKi 4.8 [49]
theophylline Hs Antagonist 4.1 – 4.7 pKi 43,54
pKi 4.1 – 4.7 (Ki 8.64x10-5 – 2.23x10-5 M) [43,54]
flavanone Hs Antagonist 4.3 pKi 49
pKi 4.3 [49]
visnagin Hs Antagonist 4.2 pKi 49
pKi 4.2 [49]
theophylline Rn Antagonist 4.0 – 4.1 pKi 44,88
pKi 4.0 – 4.1 (Ki 1x10-4 – 8.5x10-5 M) [44,88]
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).
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
LUF6000 Hs Positive - - 36
[36]
LUF6096 Hs Positive - - 39
[39]
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  73,108
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Phospholipase C stimulation
References:  60,107
Tissue Distribution
Liver, lung, placenta.
Species:  Human
Technique:  Northern blotting.
References:  66
CNS: corpus callosum, substantia nigra, thalamus, subthalamic nucleus, spinal cord, hippocampus.
Species:  Human
Technique:  Northern blotting.
References:  1
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:  75
Liver, lung > brain, aorta.
Species:  Human
Technique:  Northern blotting.
References:  78
Lung mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  107
Testes: spermatocytes, round spermatids, elongating spermatids > Leydig cells.
Species:  Rat
Technique:  in situ hybridisation.
References:  74
Brain: hippocampus.
Species:  Rat
Technique:  Western blotting.
References:  61
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 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:  37,81
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:  60
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:  78
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:  108
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