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

A₃ receptor

Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 21

Nomenclature: A₃ receptor

Gene and Protein Information
Previous and Unofficial Names
Database Links
Natural/Endogenous Ligands
Agonists
Antagonists
Allosteric Modulators
Immunopharmacology Comments
Immuno Cell Type Associations
Immuno Process Associations
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
General Comments
References
Contributors
How to cite this page

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	1,67,77,80
Mouse	7	319	3 46.45 cM	Adora3	adenosine A3 receptor	108
Rat	7	320	2q34	Adora3	adenosine A3 receptor	112

Previous and Unofficial Names
Adenosine receptor A3 \| TGPCR1 \| A3AR \| ARA3

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
Alphafold	P0DMS8 (Hs), Q61618 (Mm), P28647 (Rn)
ChEMBL Target	CHEMBL256 (Hs), CHEMBL1075269 (Mm), CHEMBL3360 (Rn)
DrugBank Target	P0DMS8 (Hs)
Ensembl Gene	ENSG00000282608 (Hs), ENSMUSG00000000562 (Mm), ENSRNOG00000015788 (Rn)
Entrez Gene	140 (Hs), 11542 (Mm), 25370 (Rn)
Human Protein Atlas	ENSG00000282608 (Hs)
KEGG Gene	hsa:140 (Hs), mmu:11542 (Mm), rno:25370 (Rn)
OMIM	600445 (Hs)
Pharos	P0DMS8 (Hs)
RefSeq Nucleotide	NM_000677 (Hs), NM_009631 (Mm), NM_012896 (Rn)
RefSeq Protein	NP_000668 (Hs), NP_033761 (Mm), NP_037028 (Rn)
UniProtKB	P0DMS8 (Hs), Q61618 (Mm), P28647 (Rn)
Wikipedia	ADORA3 (Hs)

Natural/Endogenous Ligands
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
[¹²⁵I]AB-MECA		Hs	Full agonist	9.0 – 9.1	pK_d	73,96
⤷	pK_d 9.0 – 9.1 (K_d 1x10^-9 – 6x10^-10 M) [73,96]
[³H]HEMADO		Hs	Full agonist	9.0	pK_d	54
⤷	pK_d 9.0 [54]
[¹²⁵I]AB-MECA		Rn	Full agonist	8.9	pK_d	72
⤷	pK_d 8.9 [72]
[³H]NECA		Hs	Full agonist	7.9 – 8.2	pK_d	25,55
⤷	pK_d 7.9 – 8.2 [25,55]
[¹²⁵I]APNEA		Hs	Full agonist	7.8	pK_d	112
⤷	pK_d 7.8 [112]
Cl-IB-MECA		Mm	Agonist	9.7	pK_i	60
⤷	pK_i 9.7 (K_i 1.8x10^-10 M) [60]
MRS3558		Hs	Agonist	9.5	pK_i	45
⤷	pK_i 9.5 (K_i 2.9x10^-10 M) [45]
Cl-IB-MECA		Rn	Agonist	9.5	pK_i	60
⤷	pK_i 9.5 (K_i 3.3x10^-10 M) [60]
(R,S)-PHPNECA		Hs	Full agonist	9.4	pK_i	100
⤷	pK_i 9.4 [100]
2-phenylethylyl-adenosine derivative		Hs	Agonist	9.4	pK_i	99
⤷	pK_i 9.4 (K_i 4.4x10^-10 M) [99]
MRS3558		Rn	Agonist	9.0	pK_i	60
⤷	pK_i 9.0 (K_i 1x10^-9 M) [60]
HEMADO		Hs	Agonist	9.0	pK_i	54,100
⤷	pK_i 9.0 (K_i 1.1x10^-9 M) [54,100]
piclidenoson		Hs	Full agonist	8.7 – 9.2	pK_i	25,31,55,96
⤷	pK_i 8.7 – 9.2 [25,31,55,96]
MRS3558		Mm	Agonist	8.8	pK_i	60
⤷	pK_i 8.8 (K_i 1.49x10^-9 M) [60]
MRS5151		Hs	Agonist	8.6	pK_i	65
⤷	pK_i 8.6 (K_i 2.38x10^-9 M) [65]
compound 6c [PMID: 34435786]		Hs	Agonist	8.6	pK_i	58
⤷	pK_i 8.6 (K_i 2.4x10^-9 M) [58]
2-hexynyl-NECA		Hs	Full agonist	8.6	pK_i	100
⤷	pK_i 8.6 [100]
MRS5698		Hs	Agonist	8.5	pK_i	89
⤷	pK_i 8.5 [89]
Cl-IB-MECA		Hs	Full agonist	8.0 – 8.9	pK_i	10,46,51
⤷	pK_i 8.0 – 8.9 [10,46,51]
CP608,039		Hs	Agonist	8.2	pK_i	90
⤷	pK_i 8.2 (K_i 5.8x10^-9 M) [90]
PENECA		Hs	Full agonist	8.2	pK_i	100
⤷	pK_i 8.2 [100]
I-ABA		Hs	Full agonist	8.0	pK_i	80
⤷	pK_i 8.0 [80]
MRE 3008F20		Hs	Full agonist	8.0	pK_i	96
⤷	pK_i 8.0 [96]
NECA		Hs	Full agonist	7.5 – 8.4	pK_i	9,32,46,80,96,103
⤷	pK_i 7.5 – 8.4 [9,32,46,80,96,103]
AB-MECA		Hs	Full agonist	7.7	pK_i	55,96
⤷	pK_i 7.7 [55,96]
MRS5151		Mm	Agonist	7.6	pK_i	65
⤷	pK_i 7.6 (K_i 2.44x10^-8 M) [65]
(R)-PIA		Hs	Full agonist	7.1 – 8.1	pK_i	32,46,55,80,96
⤷	pK_i 7.1 – 8.1 [32,46,55,80,96]
CCPA		Hs	Full agonist	7.4	pK_i	45,55
⤷	pK_i 7.4 [45,55]
apadenoson		Hs	Agonist	7.3	pK_i	45
⤷	pK_i 7.3 (K_i 4.5x10^-8 M) [45]
cyclopentyladenosine		Hs	Full agonist	7.0 – 7.4	pK_i	32,45,55,80
⤷	pK_i 7.0 – 7.4 [32,45,55,80]
(S)-PIA		Hs	Full agonist	6.3 – 7.4	pK_i	55,80,96
⤷	pK_i 6.3 – 7.4 [55,80,96]
MPC-MECA		Hs	Full agonist	6.8	pK_i	96
⤷	pK_i 6.8 [96]
NECA		Rn	Full agonist	6.6 – 6.9	pK_i	63,72
⤷	pK_i 6.6 – 6.9 [63,72]
N(6)-cyclohexyladenosine		Rn	Agonist	6.8	pK_i	91
⤷	pK_i 6.8 (K_i 1.76x10^-7 M) [91]
(R)-PIA		Rn	Full agonist	6.6 – 6.8	pK_i	16,72
⤷	pK_i 6.6 – 6.8 [16,72]
CCPA		Rn	Agonist	6.6	pK_i	60
⤷	pK_i 6.6 (K_i 2.37x10^-7 M) [60]
CGS 21680		Hs	Full agonist	6.0 – 7.2	pK_i	9,32,45,55,96
⤷	pK_i 6.0 – 7.2 [9,32,45,55,96]
adenosine		Hs	Agonist	6.5	pK_i	28-29,103
⤷	pK_i 6.5 (K_i 2.9x10^-7 M) [28-29,103]
CGS 21680		Rn	Agonist	6.2	pK_i	60
⤷	pK_i 6.2 (K_i 5.84x10^-7 M) [60]
TCPA		Hs	Agonist	6.2	pK_i	6
⤷	pK_i 6.2 (K_i 6x10^-7 M) [6]
binodenoson		Hs	Agonist	6.0	pK_i	45
⤷	pK_i 6.0 (K_i 9.03x10^-7 M) [45]
GS9667		Hs	Agonist	<6.0	pK_i	22
⤷	pK_i <6.0 (K_i >1x10^-6 M) [22]
N(6)-cyclohexyladenosine		Hs	Agonist	6.0	pK_i	78
⤷	pK_i 6.0 (K_i 1.025x10^-6 M) [78]
2-chloroadenosine		Rn	Agonist	5.7	pK_i	91
⤷	pK_i 5.7 (K_i 1.89x10^-6 M) [91]
2'-Me-CCPA		Rn	Agonist	5.3	pK_i	27
⤷	pK_i 5.3 (K_i 5x10^-6 M) [27]
adenosine		Rn	Agonist	5.2	pK_i	103
⤷	pK_i 5.2 (K_i 6.5x10^-6 M) [103]
BAY 60-6583		Hs	Agonist	<5.0	pK_i	56
⤷	pK_i <5.0 (K_i >1x10^-5 M) [56]
regadenoson		Hs	Agonist	<5.0	pK_i	45
⤷	pK_i <5.0 (K_i >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	Value	Parameter	Reference
[³H]MRE 3008F20		Hs	Antagonist	9.1	pK_d	4,96
⤷	pK_d 9.1 [4,96]
PSB-11		Hs	Antagonist	8.3	pK_d	68
⤷	pK_d 8.3 (K_d 4.9x10^-9 M) [68]
[³H]PSB-11		Hs	Antagonist	8.3	pK_d	68
⤷	pK_d 8.3 [68]
KF26777		Hs	Antagonist	9.7	pK_i	79
⤷	pK_i 9.7 (K_i 2x10^-10 M) [79]
PSB-10		Hs	Antagonist	9.4	pK_i	70
⤷	pK_i 9.4 (K_i 4.41x10^-10 M) [70]
MRE 3010F20		Hs	Antagonist	9.3	pK_i	96
⤷	pK_i 9.3 [96]
MRE 3008F20		Hs	Antagonist	9.0 – 9.5	pK_i	45,95-96
⤷	pK_i 9.0 – 9.5 [45,95-96]
MRS1220		Hs	Antagonist	8.2 – 9.2	pK_i	46,53,86,106
⤷	pK_i 8.2 – 9.2 (K_i 6.31x10^-9 – 6.3x10^-10 M) [46,53,86,106]
PSB-11		Hs	Antagonist	8.6	pK_i	74
⤷	pK_i 8.6 (K_i 2.34x10^-9 M) [74]
MRS1177		Hs	Antagonist	8.5	pK_i	53
⤷	pK_i 8.5 [53]
VUF5574		Hs	Antagonist	8.4	pK_i	93
⤷	pK_i 8.4 (K_i 4.03x10^-9 M) [93]
MRS1186		Hs	Antagonist	8.1	pK_i	53
⤷	pK_i 8.1 [53]
MRS1505		Hs	Antagonist	8.1	pK_i	59
⤷	pK_i 8.1 [59]
LUF7602		Hs	Antagonist	8.0	pK_i	105
⤷	pK_i 8.0 (K_i 1x10^-8 M) [105] Description: Displacement of [³H]PSB-11 binding from the hA₃AR (in membranes from stably transfected CHO cells) following preincubation for 4 h,
LJ-4517		Hs	Antagonist	7.8	pK_i	84
⤷	pK_i 7.8 (K_i 1.56x10^-8 M) [84]
VUF8504		Hs	Antagonist	7.8	pK_i	92
⤷	pK_i 7.8 [92]
xanthine amine congener		Rn	Antagonist	7.7	pK_i	72
⤷	pK_i 7.7 [72]
I-ABOPX		Hs	Antagonist	7.7	pK_i	80
⤷	pK_i 7.7 [80]
MRS1476		Hs	Antagonist	7.7	pK_i	59
⤷	pK_i 7.7 [59]
MRS1523		Hs	Antagonist	7.7	pK_i	59
⤷	pK_i 7.7 (K_i 1.99x10^-8 M) [59]
MRS1191		Hs	Antagonist	7.5	pK_i	46-47,60
⤷	pK_i 7.5 [46-47,60]
MRS1486		Hs	Antagonist	7.5	pK_i	59
⤷	pK_i 7.5 [59]
CGS 15943		Hs	Antagonist	7.0 – 7.9	pK_i	53,55,73,96
⤷	pK_i 7.0 – 7.9 [53,55,73,96]
BW-A1433		Rn	Antagonist	7.4	pK_i	72
⤷	pK_i 7.4 [72]
BW-A1433		Hs	Antagonist	7.3	pK_i	80
⤷	pK_i 7.3 [80]
xanthine amine congener		Hs	Antagonist	7.0 – 7.4	pK_i	55,80,96
⤷	pK_i 7.0 – 7.4 [55,80,96]
MRS1097		Hs	Antagonist	7.0	pK_i	46,94
⤷	pK_i 7.0 [46,94]
MRS1523		Rn	Antagonist	6.9	pK_i	60
⤷	pK_i 6.9 (K_i 1.13x10^-7 M) [60]
VUF8507		Hs	Antagonist	6.7	pK_i	92
⤷	pK_i 6.7 [92]
derenofylline		Hs	Antagonist	6.7	pK_i	48
⤷	pK_i 6.7 (K_i 2x10^-7 M) [48]
MRS1042		Hs	Antagonist	6.5	pK_i	49
⤷	pK_i 6.5 [49]
MRS1041		Hs	Antagonist	6.4	pK_i	49
⤷	pK_i 6.4 [49]
MRS1754		Hs	Antagonist	6.2	pK_i	52
⤷	pK_i 6.2 (K_i 5.7x10^-7 M) [52]
MRS1067		Hs	Antagonist	6.2	pK_i	46,49
⤷	pK_i 6.2 [46,49]
LUF5981		Hs	Antagonist	6.2	pK_i	12
⤷	pK_i 6.2 (K_i 6.37x10^-7 M) [12]
MRS1523		Mm	Antagonist	6.1	pK_i	60
⤷	pK_i 6.1 (K_i 7.31x10^-7 M) [60]
ZM-241385		Hs	Antagonist	6.1	pK_i	45
⤷	pK_i 6.1 (K_i 7.43x10^-7 M) [45]
MRS1093		Hs	Antagonist	6.1	pK_i	49
⤷	pK_i 6.1 [49]
MRS1088		Hs	Antagonist	6.1	pK_i	49
⤷	pK_i 6.1 [49]
DPCPX		Hs	Antagonist	5.4 – 6.6	pK_i	2,38,55,80,96,101
⤷	pK_i 5.4 – 6.6 (K_i 3.96x10^-6 – 2.43x10^-7 M) [2,38,55,80,96,101]
MRE 2029F20		Hs	Antagonist	<6.0	pK_i	5
⤷	pK_i <6.0 (K_i >1x10^-6 M) [5]
vipadenant		Hs	Antagonist	6.0	pK_i	34
⤷	pK_i 6.0 (K_i 1.005x10^-6 M) [34]
ST-1535		Hs	Antagonist	<6.0	pK_i	66
⤷	pK_i <6.0 (K_i >1x10^-6 M) [66]
preladenant		Hs	Antagonist	<6.0	pK_i	69
⤷	pK_i <6.0 (K_i >1x10^-6 M) [69]
ATL802		Hs	Antagonist	<6.0	pK_i	52
⤷	pK_i <6.0 (K_i >1x10^-6 M) [52]
DPCPX		Rn	Antagonist	4.4 – 7.6	pK_i	2,72,101
⤷	pK_i 4.4 – 7.6 [2,72,101]
LAS38096		Hs	Antagonist	6.0	pK_i	20,98
⤷	pK_i 6.0 (K_i 1.043x10^-6 M) [20,98]
CVT-6883		Hs	Antagonist	6.0	pK_i	21
⤷	pK_i 6.0 (K_i 1.07x10^-6 M) [21]
SCH 58261		Hs	Antagonist	5.9	pK_i	45
⤷	pK_i 5.9 (K_i 1.2x10^-6 M) [45]
MRS928		Hs	Antagonist	5.9	pK_i	49
⤷	pK_i 5.9 [49]
MRS1191		Rn	Antagonist	5.8	pK_i	59-60
⤷	pK_i 5.8 [59-60]
dexniguldipine		Hs	Antagonist	5.7	pK_i	94
⤷	pK_i 5.7 [94]
PSB36		Hs	Antagonist	5.6	pK_i	101
⤷	pK_i 5.6 (K_i 2.3x10^-6 M) [101]
galangin		Hs	Antagonist	5.5	pK_i	49
⤷	pK_i 5.5 [49]
sakuranetin		Hs	Antagonist	5.5	pK_i	49
⤷	pK_i 5.5 [49]
nicardipine		Hs	Antagonist	5.5	pK_i	94
⤷	pK_i 5.5 [94]
rolofylline		Hs	Antagonist	5.4	pK_i	50
⤷	pK_i 5.4 (K_i 4.39x10^-6 M) [50]
istradefylline		Hs	Antagonist	5.3	pK_i	30
⤷	pK_i 5.3 (K_i 4.47x10^-6 M) [30]
PSB36		Rn	Antagonist	5.2	pK_i	101
⤷	pK_i 5.2 (K_i 6.5x10^-6 M) [101]
SCH442416		Hs	Antagonist	<5.0	pK_i	45
⤷	pK_i <5.0 (K_i >1x10^-5 M) [45]
PSB603		Hs	Antagonist	<5.0	pK_i	8
⤷	pK_i <5.0 (K_i >1x10^-5 M) [8]
PSB1115		Hs	Antagonist	<5.0	pK_i	38
⤷	pK_i <5.0 (K_i >1x10^-5 M) [38]
tonapofylline		Hs	Antagonist	<5.0	pK_i	50
⤷	pK_i <5.0 (K_i >1x10^-5 M) [50]
FK-453		Hs	Antagonist	5.0	pK_i	45
⤷	pK_i 5.0 (K_i 1x10^-5 M) [45]
CSC		Rn	Antagonist	<5.0	pK_i	91
⤷	pK_i <5.0 (K_i >1x10^-5 M) [91]
MSX-2		Hs	Antagonist	<5.0	pK_i	82
⤷	pK_i <5.0 (K_i >1x10^-5 M) [82]
ATL802		Mm	Antagonist	<5.0	pK_i	52
⤷	pK_i <5.0 (K_i >1x10^-5 M) [52]
caffeine

A3 receptor

Contents:

A₃ receptor