A<sub>3</sub> receptor | Adenosine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

A3 receptor

Target id: 21

Nomenclature: A3 receptor

Family: Adenosine receptors

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   GtoImmuPdb view: OFF :     A3 receptor has curated GtoImmuPdb data

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 1,66,76,79
Mouse 7 319 3 F2.3 Adora3 adenosine A3 receptor 105
Rat 7 320 2q34 Adora3 adenosine A3 receptor 109
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
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 72,94
pKd 9.0 – 9.1 (Kd 1x10-9 – 6x10-10 M) [72,94]
[3H]HEMADO Hs Full agonist 9.0 pKd 55
pKd 9.0 [55]
[125I]AB-MECA Rn Full agonist 8.9 pKd 71
pKd 8.9 [71]
[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 109
pKd 7.8 [109]
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 98
pKi 9.4 [98]
2-phenylethylyl-adenosine derivative Hs Agonist 9.4 pKi 97
pKi 9.4 (Ki 4.4x10-10 M) [97]
MRS3558 Rn Agonist 9.0 pKi 59
pKi 9.0 (Ki 1x10-9 M) [59]
HEMADO Hs Agonist 9.0 pKi 55,98
pKi 9.0 (Ki 1.1x10-9 M) [55,98]
piclidenoson Hs Full agonist 8.7 – 9.2 pKi 25,31,54,94
pKi 8.7 – 9.2 [25,31,54,94]
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 98
pKi 8.6 [98]
MRS5698 Hs Agonist 8.5 pKi 87
pKi 8.5 [87]
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 88
pKi 8.2 (Ki 5.8x10-9 M) [88]
PENECA Hs Full agonist 8.2 pKi 98
pKi 8.2 [98]
I-ABA Hs Full agonist 8.0 pKi 79
pKi 8.0 [79]
MRE 3008F20 Hs Full agonist 8.0 pKi 94
pKi 8.0 [94]
NECA Hs Full agonist 7.5 – 8.4 pKi 9,32,46,79,94,101
pKi 7.5 – 8.4 [9,32,46,79,94,101]
AB-MECA Hs Full agonist 7.7 pKi 54,94
pKi 7.7 [54,94]
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 32,46,54,79,94
pKi 7.1 – 8.1 [32,46,54,79,94]
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 32,45,54,79
pKi 7.0 – 7.4 [32,45,54,79]
(S)-PIA Hs Full agonist 6.3 – 7.4 pKi 54,79,94
pKi 6.3 – 7.4 [54,79,94]
MPC-MECA Hs Full agonist 6.8 pKi 94
pKi 6.8 [94]
NECA Rn Full agonist 6.6 – 6.9 pKi 62,71
pKi 6.6 – 6.9 [62,71]
N(6)-cyclohexyladenosine Rn Agonist 6.8 pKi 89
pKi 6.8 (Ki 1.76x10-7 M) [89]
(R)-PIA Rn Full agonist 6.6 – 6.8 pKi 16,71
pKi 6.6 – 6.8 [16,71]
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 9,32,45,54,94
pKi 6.0 – 7.2 [9,32,45,54,94]
adenosine Hs Agonist 6.5 pKi 28-29,101
pKi 6.5 (Ki 2.9x10-7 M) [28-29,101]
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 77
pKi 6.0 (Ki 1.025x10-6 M) [77]
2-chloroadenosine Rn Agonist 5.7 pKi 89
pKi 5.7 (Ki 1.89x10-6 M) [89]
2'-Me-CCPA Rn Agonist 5.3 pKi 27
pKi 5.3 (Ki 5x10-6 M) [27]
adenosine Rn Agonist 5.2 pKi 101
pKi 5.2 (Ki 6.5x10-6 M) [101]
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 4,94
pKd 9.1 [4,94]
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 78
pKi 9.7 (Ki 2x10-10 M) [78]
PSB-10 Hs Antagonist 9.4 pKi 69
pKi 9.4 (Ki 4.41x10-10 M) [69]
MRE 3010F20 Hs Antagonist 9.3 pKi 94
pKi 9.3 [94]
MRE 3008F20 Hs Antagonist 9.0 – 9.5 pKi 45,93-94
pKi 9.0 – 9.5 [45,93-94]
MRS1220 Hs Antagonist 8.2 – 9.2 pKi 46,53,84,103
pKi 8.2 – 9.2 (Ki 6.31x10-9 – 6.3x10-10 M) [46,53,84,103]
PSB-11 Hs Antagonist 8.6 pKi 73
pKi 8.6 (Ki 2.34x10-9 M) [73]
MRS1177 Hs Antagonist 8.5 pKi 53
pKi 8.5 [53]
VUF5574 Hs Antagonist 8.4 pKi 91
pKi 8.4 (Ki 4.03x10-9 M) [91]
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 90
pKi 7.8 [90]
xanthine amine congener Rn Antagonist 7.7 pKi 71
pKi 7.7 [71]
I-ABOPX Hs Antagonist 7.7 pKi 79
pKi 7.7 [79]
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 53-54,72,94
pKi 7.0 – 7.9 [53-54,72,94]
BW-A1433 Rn Antagonist 7.4 pKi 71
pKi 7.4 [71]
BW-A1433 Hs Antagonist 7.3 pKi 79
pKi 7.3 [79]
xanthine amine congener Hs Antagonist 7.0 – 7.4 pKi 54,79,94
pKi 7.0 – 7.4 [54,79,94]
MRS1097 Hs Antagonist 7.0 pKi 46,92
pKi 7.0 [46,92]
MRS1523 Rn Antagonist 6.9 pKi 59
pKi 6.9 (Ki 1.13x10-7 M) [59]
VUF8507 Hs Antagonist 6.7 pKi 90
pKi 6.7 [90]
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 2,38,54,79,94,99
pKi 5.4 – 6.6 (Ki 3.96x10-6 – 2.43x10-7 M) [2,38,54,79,94,99]
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 2,71,99
pKi 4.4 – 7.6 [2,71,99]
LAS38096 Hs Antagonist 6.0 pKi 20,96
pKi 6.0 (Ki 1.043x10-6 M) [20,96]
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 92
pKi 5.7 [92]
PSB36 Hs Antagonist 5.6 pKi 99
pKi 5.6 (Ki 2.3x10-6 M) [99]
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 92
pKi 5.5 [92]
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 99
pKi 5.2 (Ki 6.5x10-6 M) [99]
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 89
pKi <5.0 (Ki >1x10-5 M) [89]
MSX-2 Hs Antagonist <5.0 pKi 81
pKi <5.0 (Ki >1x10-5 M) [81]
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 44,89
pKi 4.0 – 4.1 (Ki 1x10-4 – 8.5x10-5 M) [44,89]
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]
Immunopharmacology Comments
Agonist stimulation of the A2A and A3 receptors down-regulates production of the pro-inflammatory mediators TNF-α and IL-8 in human synoviocytes [95], suggesting a role in controlling arthritic joint inflammation.
Cell Type Associations
Immuno Cell Type:  T cells
Cell Ontology Term:   type I NK T cell (CL:0000921)