A<sub>2A</sub> receptor | Adenosine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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A2A receptor

Target id: 19

Nomenclature: A2A 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

   GtoImmuPdb view: OFF :     Currently no data for A2A receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 412 22q11.23 ADORA2A adenosine A2a receptor 39,69,105
Mouse 7 410 10 Adora2a adenosine A2a receptor 82
Rat 7 410 20p12 Adora2a adenosine A2a receptor 18
Previous and Unofficial Names
RDC8 | A2-AR | adenosine receptor A2a
Database Links
Specialist databases
GPCRDB aa2ar_human (Hs), aa2ar_mouse (Mm), aa2ar_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human A2A adenosine receptor bound to an antagonist
PDB Id:  4EIY
Ligand:  ZM-241385
Resolution:  1.8Å
Species:  Human
References:  77
Image of receptor 3D structure from RCSB PDB
Description:  A2A receptor (thermostabilised) bound to its natural ligand adenosine
PDB Id:  2YDO
Ligand:  adenosine   This ligand is endogenous
Resolution:  3.0Å
Species:  Human
References:  71
Image of receptor 3D structure from RCSB PDB
Description:  Thermostabilised human A2A receptor with NECA bound
PDB Id:  2YDV
Ligand:  NECA
Resolution:  2.6Å
Species:  Human
References:  70
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with PSB36
PDB Id:  5N2R
Ligand:  PSB36
Resolution:  2.8Å
Species:  Human
References:  16
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein.
PDB Id:  6GDG
Ligand:  NECA
Resolution:  3.8Å
Species:  Human
References:  45
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
[3H]CGS 21680 Hs Full agonist 7.7 – 7.8 pKd 53,138
pKd 7.7 – 7.8 (Kd 2.2x10-8 – 1.6x10-8 M) [53,138]
[3H]NECA Hs Full agonist 7.7 pKd 63
pKd 7.7 [63]
apadenoson Hs Agonist 9.3 pKi 104
pKi 9.3 (Ki 5x10-10 M) [104]
(R,S)-PHPNECA Hs Full agonist 8.5 pKi 137
pKi 8.5 [137]
2-hexynyl-NECA Hs Full agonist 8.2 – 8.3 pKi 28,65,137
pKi 8.2 – 8.3 [28,65,137]
compound 4g [PMID: 22220592] Hs Agonist 8.1 pKi 20
pKi 8.1 (Ki 7.76x10-9 M) [20]
NECA Rn Agonist 8.0 pKi 79
pKi 8.0 (Ki 9.7x10-9 M) [79]
UK-432,097 Hs Agonist 7.7 – 8.3 pKi 47,141
pKi 7.7 – 8.3 [47,141]
NECA Hs Full agonist 6.9 – 8.7 pKi 10,28,43,60,65,142
pKi 6.9 – 8.7 [10,28,43,60,65,142]
CGS 21680 Rn Agonist 7.7 pKi 76
pKi 7.7 (Ki 1.9x10-8 M) [76]
CGS 21680 Hs Full agonist 6.7 – 8.1 pKi 10,28,43,52,60,63,65,98
pKi 6.7 – 8.1 (Ki 1.99x10-7 – 7.94x10-9 M) [10,28,43,52,60,63,65,98]
2-chloroadenosine Rn Agonist 7.1 pKi 24
pKi 7.1 (Ki 7.6x10-8 M) [24]
CV-1808 Hs Full agonist 7.1 pKi 28,65
pKi 7.1 [28,65]
adenosine Rn Agonist 6.8 pKi 142
pKi 6.8 (Ki 1.5x10-7 M) [142]
2-chloroadenosine Hs Full agonist 6.7 – 6.8 pKi 60,65
pKi 6.7 – 6.8 [60,65]
TCPA Hs Agonist 6.7 pKi 7
pKi 6.7 (Ki 2.1x10-7 M) [7]
(R)-PIA Rn Agonist 6.7 pKi 24
pKi 6.7 (Ki 2.2x10-7 M) [24]
binodenoson Hs Agonist 6.6 pKi 52
pKi 6.6 (Ki 2.7x10-7 M) [52]
regadenoson Hs Agonist 6.5 pKi 52
pKi 6.5 (Ki 2.9x10-7 M) [52]
adenosine Hs Agonist 6.5 pKi 35-36,142
pKi 6.5 (Ki 3.1x10-7 M) [35-36,142]
CGS 24012 Hs Full agonist 6.4 pKi 60
pKi 6.4 [60]
N(6)-cyclohexyladenosine Rn Agonist 6.3 pKi 24
pKi 6.3 (Ki 4.6x10-7 M) [24]
Cl-IB-MECA Rn Agonist 6.3 pKi 76
pKi 6.3 (Ki 4.7x10-7 M) [76]
PENECA Hs Full agonist 6.2 pKi 137
pKi 6.2 [137]
cyclopentyladenosine Hs Full agonist 6.1 pKi 43,52,63
pKi 6.1 [43,52,63]
(R)-PIA Hs Full agonist 6.0 – 6.2 pKi 28,43,60,63,65
pKi 6.0 – 6.2 [28,43,60,63,65]
CCPA Rn Agonist 6.0 pKi 76
pKi 6.0 (Ki 9.5x10-7 M) [76]
cyclopentyladenosine Rn Agonist 6.0 pKi 76
pKi 6.0 (Ki 9.5x10-7 M) [76]
MRS3558 Rn Agonist 6.0 pKi 76
pKi 6.0 (Ki 1.08x10-6 M) [76]
piclidenoson Hs Full agonist 5.6 – 6.3 pKi 52,60,63
pKi 5.6 – 6.3 [52,60,63]
HEMADO Hs Agonist 5.9 pKi 64,137
pKi 5.9 (Ki 1.2x10-6 M) [64,137]
N(6)-cyclohexyladenosine Hs Full agonist 5.9 pKi 28,65
pKi 5.9 [28,65]
GR79236 Hs Agonist 5.9 pKi 52
pKi 5.9 (Ki 1.3x10-6 M) [52]
CV-1674 Hs Full agonist 5.8 pKi 65
pKi 5.8 [65]
tecadenoson Pig Agonist 5.6 pKi 52,90
pKi 5.6 (Ki 2.315x10-6 M) [52,90]
MRS3558 Hs Agonist 5.6 pKi 52
pKi 5.6 (Ki 2.33x10-6 M) [52]
CCPA Hs Full agonist 5.6 pKi 52,63
pKi 5.6 [52,63]
metrifudil Hs Full agonist 5.5 pKi 65
pKi 5.5 [65]
AB-MECA Hs Full agonist 5.4 pKi 63
pKi 5.4 [63]
APNEA Hs Full agonist 5.3 pKi 65
pKi 5.3 [65]
Cl-IB-MECA Hs Agonist 5.3 pKi 52
pKi 5.3 (Ki 5.36x10-6 M) [52]
(S)-PIA Hs Full agonist 5.0 – 5.1 pKi 28,63
pKi 5.0 – 5.1 [28,63]
Cl-IB-MECA Mm Agonist ~5.0 pKi 76
pKi ~5.0 (Ki ~1x10-5 M) [76]
BAY 60-6583 Hs Agonist <5.0 pKi 67
pKi <5.0 (Ki >1x10-5 M) [67]
GS9667 Hs Agonist <5.0 pKi 33
pKi <5.0 (Ki >1x10-5 M) [33]
MRS5151 Hs Agonist <5.0 pKi 85
pKi <5.0 (Ki >1x10-5 M) [85]
MRS5151 Mm Agonist <5.0 pKi 85
pKi <5.0 (Ki >1x10-5 M) [85]
MRS3558 Mm Agonist 5.0 pKi 76
pKi 5.0 (Ki 1.04x10-5 M) [76]
View species-specific agonist tables
Agonist Comments
The INN-assigned compound evodenoson is an agonist of the A2A receptor but affinity data is not available.
Note that for tecadenoson, there is inconsistency between the two referenced articles (from the same group) as to the species origin of the ADORA2A used to generate the Ki value which is presented as identical in both articles. We have used the earlier paper as precedent, which indicates the use of the porcine receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]ZM-241385 Rn Antagonist 9.2 pKd 103
pKd 9.2 [103]
[3H]ZM 241385 Hs Antagonist 8.7 – 9.1 pKd 4,42
pKd 8.7 – 9.1 (Kd 1.8x10-9 – 8x10-10 M) [4,42]
[3H]SCH 58261 Hs Antagonist 8.6 – 9.0 pKd 65,101
pKd 8.6 – 9.0 [65,101]
[3H]XAC Hs Antagonist 8.0 pKd 60
pKd 8.0 [60]
SCH442416 Hs Antagonist 8.4 – 10.3 pKi 124,127
pKi 8.4 – 10.3 [124,127]
MRS1093 Hs Antagonist 9.2 pKi 57
pKi 9.2 [57]
preladenant Hs Antagonist 9.1 pKi 89
pKi 9.1 (Ki 9x10-10 M) [89]
ZM-241385 Hs Antagonist 8.8 – 9.1 pKi 101
pKi 8.8 – 9.1 [101]
vipadenant Hs Antagonist 8.9 pKi 46
pKi 8.9 (Ki 1.3x10-9 M) [46]
SCH 58261 Hs Antagonist 8.3 – 9.2 pKi 28,65,101
pKi 8.3 – 9.2 [28,65,101]
xanthine amine congener Hs Antagonist 8.4 – 9.0 pKi 28,63
pKi 8.4 – 9.0 [28,63]
CGS 15943 Hs Antagonist 7.7 – 9.4 pKi 28,60,63,101
pKi 7.7 – 9.4 [28,60,63,101]
istradefylline Rn Antagonist 8.4 – 8.7 pKi 110,123
pKi 8.4 – 8.7 (Ki 4.46x10-9 – 2.2x10-9 M) [110,123]
tozadenant Hs Antagonist 8.3 pKi 25
pKi 8.3 (Ki 5x10-9 M) [25]
ST-1535 Hs Antagonist 8.2 pKi 86
pKi 8.2 (Ki 6.6x10-9 M) [86]
MSX-2 Rn Antagonist 8.1 pKi 91,118
pKi 8.1 (Ki 8.04x10-9 M) [91,118]
MSX-2 Hs Antagonist 7.8 – 8.3 pKi 118
pKi 7.8 – 8.3 (Ki 1.45x10-8 – 5.38x10-9 M) [118]
KF 17837S Hs Antagonist 7.7 pKi 28
pKi 7.7 [28]
istradefylline Hs Antagonist 7.0 – 7.9 pKi 12,37
pKi 7.0 – 7.9 (Ki 9.12x10-8 – 1.2x10-8 M) [12,37]
CSC Rn Antagonist 7.3 pKi 51
pKi 7.3 (Ki 5.4x10-8 M) [51]
DPCPX Hs Antagonist 6.6 – 7.2 pKi 28,63,65,101,140
pKi 6.6 – 7.2 [28,63,65,101,140]
MRE 3008F20 Hs Antagonist 6.8 pKi 52,130-131
pKi 6.8 [52,130-131]
LUF5981 Hs Antagonist 6.7 pKi 12
pKi 6.7 (Ki 1.94x10-7 M) [12]
rolofylline Hs Antagonist 6.2 – 7.0 pKi 58,106
pKi 6.2 – 7.0 (Ki 6.37x10-7 – 1.08x10-7 M) [58,106]
DPCPX Rn Antagonist 6.3 – 6.8 pKi 61,91
pKi 6.3 – 6.8 (Ki 5x10-7 – 1.57x10-7 M) [61,91]
derenofylline Hs Antagonist 6.4 pKi 56
pKi 6.4 (Ki 3.98x10-7 M) [56]
rolofylline Rn Antagonist 6.3 – 6.4 pKi 59,107
pKi 6.3 – 6.4 (Ki 5.1x10-7 – 3.8x10-7 M) [59,107]
KF26777 Hs Antagonist 6.3 pKi 113
pKi 6.3 (Ki 4.7x10-7 M) [113]
MRS1754 Hs Antagonist 6.3 pKi 62
pKi 6.3 (Ki 5.03x10-7 M) [62]
PSB36 Rn Antagonist 6.3 pKi 140
pKi 6.3 (Ki 5.52x10-7 M) [140]
MRS1754 Rn Antagonist 6.2 pKi 62
pKi 6.2 (Ki 6.12x10-7 M) [62]
CPX Hs Antagonist 6.2 pKi 60
pKi 6.2 [60]
ATL802 Hs Antagonist 6.2 pKi 62
pKi 6.2 (Ki 6.54x10-7 M) [62]
CPFPX Rn Antagonist 6.1 pKi 48
pKi 6.1 (Ki 8.12x10-7 M) [48]
CPFPX Hs Antagonist 6.0 pKi 48
pKi 6.0 (Ki 9.4x10-7 M) [48]
PSB36 Hs Antagonist 6.0 pKi 140
pKi 6.0 (Ki 9.8x10-7 M) [140]
MRE 2029F20 Hs Antagonist <6.0 pKi 6
pKi <6.0 (Ki >1x10-6 M) [6]
galangin Hs Antagonist 6.0 pKi 57
pKi 6.0 [57]
LAS38096 Hs Antagonist <6.0 pKi 30,135
pKi <6.0 (Ki >1x10-6 M) [30,135]
FK-453 Hs Antagonist 5.9 pKi 52
pKi 5.9 (Ki 1.3x10-6 M) [52]
PSB-11 Hs Antagonist 5.9 pKi 102
pKi 5.9 (Ki 1.28x10-6 M) [102]
MRS1523 Rn Antagonist 5.7 pKi 76
pKi 5.7 (Ki 2.05x10-6 M) [76]
PSB-11 Rn Antagonist 5.7 pKi 102
pKi 5.7 (Ki 2.1x10-6 M) [102]
tonapofylline Rn Antagonist 5.6 pKi 58
pKi 5.6 (Ki 2.44x10-6 M) [58]
PSB-10 Hs Antagonist 5.6 pKi 102
pKi 5.6 (Ki 2.7x10-6 M) [102]
MRS1041 Hs Antagonist 5.5 pKi 57
pKi 5.5 [57]
MRS1042 Hs Antagonist 5.5 pKi 57
pKi 5.5 [57]
flavone Hs Antagonist 5.5 pKi 57
pKi 5.5 [57]
theophylline Hs Antagonist 5.2 – 5.8 pKi 28,50,63,130
pKi 5.2 – 5.8 [28,50,63,130]
CVT-6883 Hs Antagonist 5.5 pKi 32
pKi 5.5 (Ki 3.28x10-6 M) [32]
MRS1523 Hs Antagonist 5.4 pKi 76
pKi 5.4 (Ki 3.66x10-6 M) [76]
PSB-10 Rn Antagonist 5.2 pKi 93
pKi 5.2 (Ki 6.04x10-6 M) [93]
MRS928 Hs Antagonist 5.2 pKi 57
pKi 5.2 [57]
tonapofylline Hs Antagonist 5.2 pKi 58
pKi 5.2 (Ki 6.41x10-6 M) [58]
caffeine Hs Antagonist 4.6 – 5.6 pKi 1,50,65
pKi 4.6 – 5.6 [1,50,65]
ATL802 Mm Antagonist 5.1 pKi 62
pKi 5.1 (Ki 8.393x10-6 M) [62]
MRS1191 Hs Antagonist <5.0 pKi 76
pKi <5.0 (Ki >1x10-5 M) [76]
MRS1191 Rn Antagonist <5.0 pKi 76
pKi <5.0 (Ki >1x10-5 M) [76]
VUF5574 Rn Antagonist >5.0 pKi 128
pKi >5.0 (Ki <1x10-5 M) [128]
PSB603 Hs Antagonist <5.0 pKi 9
pKi <5.0 (Ki >1x10-5 M) [9]
PSB603 Rn Antagonist <5.0 pKi 9
pKi <5.0 (Ki >1x10-5 M) [9]
MRS1065 Hs Antagonist 4.9 pKi 57
pKi 4.9 [57]
morin Hs Antagonist 4.8 pKi 57
pKi 4.8 [57]
theophylline Rn Antagonist 4.6 – 4.7 pKi 50,92
pKi 4.6 – 4.7 (Ki 2.53x10-5 – 2.2x10-5 M) [50,92]
PSB1115 Rn Antagonist 4.6 pKi 92
pKi 4.6 (Ki 2.4x10-5 M) [92]
MRS1086 Hs Antagonist 4.6 pKi 57
pKi 4.6 [57]
MRS1132 Hs Antagonist 4.6 pKi 57
pKi 4.6 [57]
MRS1066 Hs Antagonist 4.5 pKi 57
pKi 4.5 [57]
caffeine Rn Antagonist 4.3 – 4.5 pKi 23,50,91