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

A₃ receptor

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	1,68,78,81
Mouse	7	319	3 46.45 cM	Adora3	adenosine A3 receptor	109
Rat	7	320	2q34	Adora3	adenosine A3 receptor	113

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	74,97
⤷	pK_d 9.0 – 9.1 (K_d 1x10^-9 – 6x10^-10 M) [74,97]
[³H]HEMADO		Hs	Full agonist	9.0	pK_d	55
⤷	pK_d 9.0 [55]
[¹²⁵I]AB-MECA		Rn	Full agonist	8.9	pK_d	73
⤷	pK_d 8.9 [73]
[³H]NECA		Hs	Full agonist	7.9 – 8.2	pK_d	26,56
⤷	pK_d 7.9 – 8.2 [26,56]
[¹²⁵I]APNEA		Hs	Full agonist	7.8	pK_d	113
⤷	pK_d 7.8 [113]
Cl-IB-MECA		Mm	Agonist	9.7	pK_i	61
⤷	pK_i 9.7 (K_i 1.8x10^-10 M) [61]
MRS3558		Hs	Agonist	9.5	pK_i	46
⤷	pK_i 9.5 (K_i 2.9x10^-10 M) [46]
Cl-IB-MECA		Rn	Agonist	9.5	pK_i	61
⤷	pK_i 9.5 (K_i 3.3x10^-10 M) [61]
(R,S)-PHPNECA		Hs	Full agonist	9.4	pK_i	101
⤷	pK_i 9.4 [101]
2-phenylethylyl-adenosine derivative		Hs	Agonist	9.4	pK_i	100
⤷	pK_i 9.4 (K_i 4.4x10^-10 M) [100]
MRS3558		Rn	Agonist	9.0	pK_i	61
⤷	pK_i 9.0 (K_i 1x10^-9 M) [61]
HEMADO		Hs	Agonist	9.0	pK_i	55,101
⤷	pK_i 9.0 (K_i 1.1x10^-9 M) [55,101]
piclidenoson		Hs	Full agonist	8.7 – 9.2	pK_i	26,32,56,97
⤷	pK_i 8.7 – 9.2 [26,32,56,97]
MRS3558		Mm	Agonist	8.8	pK_i	61
⤷	pK_i 8.8 (K_i 1.49x10^-9 M) [61]
MRS5151		Hs	Agonist	8.6	pK_i	66
⤷	pK_i 8.6 (K_i 2.38x10^-9 M) [66]
compound 6c [PMID: 34435786]		Hs	Agonist	8.6	pK_i	59
⤷	pK_i 8.6 (K_i 2.4x10^-9 M) [59]
2-hexynyl-NECA		Hs	Full agonist	8.6	pK_i	101
⤷	pK_i 8.6 [101]
MRS5698		Hs	Agonist	8.5	pK_i	90
⤷	pK_i 8.5 [90]
Cl-IB-MECA		Hs	Full agonist	8.0 – 8.9	pK_i	10,47,52
⤷	pK_i 8.0 – 8.9 [10,47,52]
CP608,039		Hs	Agonist	8.2	pK_i	91
⤷	pK_i 8.2 (K_i 5.8x10^-9 M) [91]
PENECA		Hs	Full agonist	8.2	pK_i	101
⤷	pK_i 8.2 [101]
I-ABA		Hs	Full agonist	8.0	pK_i	81
⤷	pK_i 8.0 [81]
MRE 3008F20		Hs	Full agonist	8.0	pK_i	97
⤷	pK_i 8.0 [97]
NECA		Hs	Full agonist	7.5 – 8.4	pK_i	9,33,47,81,97,104
⤷	pK_i 7.5 – 8.4 [9,33,47,81,97,104]
AB-MECA		Hs	Full agonist	7.7	pK_i	56,97
⤷	pK_i 7.7 [56,97]
MRS5151		Mm	Agonist	7.6	pK_i	66
⤷	pK_i 7.6 (K_i 2.44x10^-8 M) [66]
(R)-PIA		Hs	Full agonist	7.1 – 8.1	pK_i	33,47,56,81,97
⤷	pK_i 7.1 – 8.1 [33,47,56,81,97]
CCPA		Hs	Full agonist	7.4	pK_i	46,56
⤷	pK_i 7.4 [46,56]
apadenoson		Hs	Agonist	7.3	pK_i	46
⤷	pK_i 7.3 (K_i 4.5x10^-8 M) [46]
cyclopentyladenosine		Hs	Full agonist	7.0 – 7.4	pK_i	33,46,56,81
⤷	pK_i 7.0 – 7.4 [33,46,56,81]
(S)-PIA		Hs	Full agonist	6.3 – 7.4	pK_i	56,81,97
⤷	pK_i 6.3 – 7.4 [56,81,97]
MPC-MECA		Hs	Full agonist	6.8	pK_i	97
⤷	pK_i 6.8 [97]
NECA		Rn	Full agonist	6.6 – 6.9	pK_i	64,73
⤷	pK_i 6.6 – 6.9 [64,73]
N(6)-cyclohexyladenosine		Rn	Agonist	6.8	pK_i	92
⤷	pK_i 6.8 (K_i 1.76x10^-7 M) [92]
(R)-PIA		Rn	Full agonist	6.6 – 6.8	pK_i	16,73
⤷	pK_i 6.6 – 6.8 [16,73]
CCPA		Rn	Agonist	6.6	pK_i	61
⤷	pK_i 6.6 (K_i 2.37x10^-7 M) [61]
CGS 21680		Hs	Full agonist	6.0 – 7.2	pK_i	9,33,46,56,97
⤷	pK_i 6.0 – 7.2 [9,33,46,56,97]
adenosine		Hs	Agonist	6.5	pK_i	29-30,104
⤷	pK_i 6.5 (K_i 2.9x10^-7 M) [29-30,104]
CGS 21680		Rn	Agonist	6.2	pK_i	61
⤷	pK_i 6.2 (K_i 5.84x10^-7 M) [61]
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	46
⤷	pK_i 6.0 (K_i 9.03x10^-7 M) [46]
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	79
⤷	pK_i 6.0 (K_i 1.025x10^-6 M) [79]
2-chloroadenosine		Rn	Agonist	5.7	pK_i	92
⤷	pK_i 5.7 (K_i 1.89x10^-6 M) [92]
2'-Me-CCPA		Rn	Agonist	5.3	pK_i	28
⤷	pK_i 5.3 (K_i 5x10^-6 M) [28]
adenosine		Rn	Agonist	5.2	pK_i	104
⤷	pK_i 5.2 (K_i 6.5x10^-6 M) [104]
BAY 60-6583		Hs	Agonist	<5.0	pK_i	57
⤷	pK_i <5.0 (K_i >1x10^-5 M) [57]
regadenoson		Hs	Agonist	<5.0	pK_i	46
⤷	pK_i <5.0 (K_i >1x10^-5 M) [46]

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	4,97
⤷	pK_d 9.1 [4,97]
PSB-11		Hs	Antagonist	8.3	pK_d	69
⤷	pK_d 8.3 (K_d 4.9x10^-9 M) [69]
[³H]PSB-11		Hs	Antagonist	8.3	pK_d	69
⤷	pK_d 8.3 [69]
KF26777		Hs	Antagonist	9.7	pK_i	80
⤷	pK_i 9.7 (K_i 2x10^-10 M) [80]
PSB-10		Hs	Antagonist	9.4	pK_i	71
⤷	pK_i 9.4 (K_i 4.41x10^-10 M) [71]
MRE 3010F20		Hs	Antagonist	9.3	pK_i	97
⤷	pK_i 9.3 [97]
MRE 3008F20		Hs	Antagonist	9.0 – 9.5	pK_i	46,96-97
⤷	pK_i 9.0 – 9.5 [46,96-97]
MRS1220		Hs	Antagonist	8.2 – 9.2	pK_i	47,54,87,107
⤷	pK_i 8.2 – 9.2 (K_i 6.31x10^-9 – 6.3x10^-10 M) [47,54,87,107]
PSB-11		Hs	Antagonist	8.6	pK_i	75
⤷	pK_i 8.6 (K_i 2.34x10^-9 M) [75]
MRS1177		Hs	Antagonist	8.5	pK_i	54
⤷	pK_i 8.5 [54]
VUF5574		Hs	Antagonist	8.4	pK_i	94
⤷	pK_i 8.4 (K_i 4.03x10^-9 M) [94]
MRS1186		Hs	Antagonist	8.1	pK_i	54
⤷	pK_i 8.1 [54]
MRS1505		Hs	Antagonist	8.1	pK_i	60
⤷	pK_i 8.1 [60]
LUF7602		Hs	Antagonist	8.0	pK_i	106
⤷	pK_i 8.0 (K_i 1x10^-8 M) [106] 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	85
⤷	pK_i 7.8 (K_i 1.56x10^-8 M) [85]
VUF8504		Hs	Antagonist	7.8	pK_i	93
⤷	pK_i 7.8 [93]
xanthine amine congener		Rn	Antagonist	7.7	pK_i	73
⤷	pK_i 7.7 [73]
I-ABOPX		Hs	Antagonist	7.7	pK_i	81
⤷	pK_i 7.7 [81]
MRS1476		Hs	Antagonist	7.7	pK_i	60
⤷	pK_i 7.7 [60]
MRS1523		Hs	Antagonist	7.7	pK_i	60
⤷	pK_i 7.7 (K_i 1.99x10^-8 M) [60]
MRS1191		Hs	Antagonist	7.5	pK_i	47-48,61
⤷	pK_i 7.5 [47-48,61]
MRS1486		Hs	Antagonist	7.5	pK_i	60
⤷	pK_i 7.5 [60]
CGS 15943		Hs	Antagonist	7.0 – 7.9	pK_i	54,56,74,97
⤷	pK_i 7.0 – 7.9 [54,56,74,97]
BW-A1433		Rn	Antagonist	7.4	pK_i	73
⤷	pK_i 7.4 [73]
BW-A1433		Hs	Antagonist	7.3	pK_i	81
⤷	pK_i 7.3 [81]
xanthine amine congener		Hs	Antagonist	7.0 – 7.4	pK_i	56,81,97
⤷	pK_i 7.0 – 7.4 [56,81,97]
MRS1097		Hs	Antagonist	7.0	pK_i	47,95
⤷	pK_i 7.0 [47,95]
MRS1523		Rn	Antagonist	6.9	pK_i	61
⤷	pK_i 6.9 (K_i 1.13x10^-7 M) [61]
VUF8507		Hs	Antagonist	6.7	pK_i	93
⤷	pK_i 6.7 [93]
derenofylline		Hs	Antagonist	6.7	pK_i	49
⤷	pK_i 6.7 (K_i 2x10^-7 M) [49]
MRS1042		Hs	Antagonist	6.5	pK_i	50
⤷	pK_i 6.5 [50]
MRS1041		Hs	Antagonist	6.4	pK_i	50
⤷	pK_i 6.4 [50]
MRS1754		Hs	Antagonist	6.2	pK_i	53
⤷	pK_i 6.2 (K_i 5.7x10^-7 M) [53]
MRS1067		Hs	Antagonist	6.2	pK_i	47,50
⤷	pK_i 6.2 [47,50]
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	61
⤷	pK_i 6.1 (K_i 7.31x10^-7 M) [61]
ZM-241385		Hs	Antagonist	6.1	pK_i	46
⤷	pK_i 6.1 (K_i 7.43x10^-7 M) [46]
MRS1093		Hs	Antagonist	6.1	pK_i	50
⤷	pK_i 6.1 [50]
MRS1088		Hs	Antagonist	6.1	pK_i	50
⤷	pK_i 6.1 [50]
DPCPX		Hs	Antagonist	5.4 – 6.6	pK_i	2,39,56,81,97,102
⤷	pK_i 5.4 – 6.6 (K_i 3.96x10^-6 – 2.43x10^-7 M) [2,39,56,81,97,102]
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	35
⤷	pK_i 6.0 (K_i 1.005x10^-6 M) [35]
ST-1535		Hs	Antagonist	<6.0	pK_i	67
⤷	pK_i <6.0 (K_i >1x10^-6 M) [67]
preladenant		Hs	Antagonist	<6.0	pK_i	70
⤷	pK_i <6.0 (K_i >1x10^-6 M) [70]
ATL802		Hs	Antagonist	<6.0	pK_i	53
⤷	pK_i <6.0 (K_i >1x10^-6 M) [53]
DPCPX		Rn	Antagonist	4.4 – 7.6	pK_i	2,73,102
⤷	pK_i 4.4 – 7.6 [2,73,102]
LAS38096		Hs	Antagonist	6.0	pK_i	20,99
⤷	pK_i 6.0 (K_i 1.043x10^-6 M) [20,99]
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	46
⤷	pK_i 5.9 (K_i 1.2x10^-6 M) [46]
MRS928		Hs	Antagonist	5.9	pK_i	50
⤷	pK_i 5.9 [50]
MRS1191		Rn	Antagonist	5.8	pK_i	60-61
⤷	pK_i 5.8 [60-61]
dexniguldipine		Hs	Antagonist	5.7	pK_i	95
⤷	pK_i 5.7 [95]
PSB36		Hs	Antagonist	5.6	pK_i	102
⤷	pK_i 5.6 (K_i 2.3x10^-6 M) [102]
galangin		Hs	Antagonist	5.5	pK_i	50
⤷	pK_i 5.5 [50]
sakuranetin		Hs	Antagonist	5.5	pK_i	50
⤷	pK_i 5.5 [50]
nicardipine		Hs	Antagonist	5.5	pK_i	95
⤷	pK_i 5.5 [95]
rolofylline		Hs	Antagonist	5.4	pK_i	51
⤷	pK_i 5.4 (K_i 4.39x10^-6 M) [51]
istradefylline		Hs	Antagonist	5.3	pK_i	31
⤷	pK_i 5.3 (K_i 4.47x10^-6 M) [31]
PSB36		Rn	Antagonist	5.2	pK_i	102
⤷	pK_i 5.2 (K_i 6.5x10^-6 M) [102]
SCH442416		Hs	Antagonist	<5.0	pK_i	46
⤷	pK_i <5.0 (K_i >1x10^-5 M) [46]
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	39
⤷	pK_i <5.0 (K_i >1x10^-5 M) [39]
tonapofylline		Hs	Antagonist	<5.0	pK_i	51
⤷	pK_i <5.0 (K_i >1x10^-5 M) [51]
FK-453		Hs	Antagonist	5.0	pK_i	46
⤷	pK_i 5.0 (K_i 1x10^-5 M) [46]
CSC		Rn	Antagonist	<5.0	pK_i	92
⤷	pK_i <5.0 (K_i >1x10^-5 M) [92]
MSX-2		Hs	Antagonist	<5.0	pK_i	83
⤷	pK_i <5.0 (K_i >1x10^-5 M) [83]
ATL802		Mm	Antagonist	<5.0	pK_i	53

A3 receptor

Contents:

A₃ receptor