A<sub>1</sub> receptor | Adenosine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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A1 receptor

target has curated data in GtoImmuPdb

Target id: 18

Nomenclature: A1 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

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 326 1q32.1 ADORA1 adenosine A1 receptor 84,114,138
Mouse 7 326 1 E4 Adora1 adenosine A1 receptor 92,148
Rat 7 326 13q13 Adora1 adenosine A1 receptor 91
Previous and Unofficial Names
RDC7 | adenosine receptor A1 | A1-AR | A1R
Database Links
Specialist databases
GPCRDB aa1r_human (Hs), aa1r_mouse (Mm), aa1r_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the human adenosine A1 receptor A1AR-bRIL in complex with the covalent antagonist DU172 at 3.2A resolution
PDB Id:  5UEN
Ligand:  DU172
Resolution:  3.2Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of stabilized A1 receptor in complex with PSB36
PDB Id:  5N2S
Ligand:  PSB36
Resolution:  3.3Å
Species:  Human
References:  16
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the adenosine-bound human adenosine A1 receptor–Gi complex
PDB Id:  6D9H
Ligand:  adenosine
Resolution:  3.6Å
Species:  Human
References:  28
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 Value Parameter Reference
[3H]CCPA Hs Full agonist 9.2 pKd 76,117
pKd 9.2 (Kd 6.31x10-10 M) [76,117]
5-Cl-5-deoxy-(±)-ENBA Hs Full agonist 9.3 pKi 34
pKi 9.3 (Ki 5.1x10-10 M) [34]
N(6)-cyclohexyladenosine Rn Agonist 9.1 pKi 22
pKi 9.1 (Ki 8.5x10-10 M) [22]
(R)-PIA Rn Agonist 8.9 pKi 22
pKi 8.9 (Ki 1.2x10-9 M) [22]
CCPA Rn Agonist 8.9 pKi 83
pKi 8.9 (Ki 1.3x10-9 M) [83]
(R,S)-PHPNECA Hs Full agonist 8.6 pKi 145
pKi 8.6 [145]
TCPA Hs Agonist 8.6 pKi 8
pKi 8.6 (Ki 2.8x10-9 M) [8]
GR79236 Rn Agonist 8.5 pKi 61
pKi 8.5 (Ki 3.1x10-9 M) [61]
NECA Rn Agonist 8.3 pKi 87
pKi 8.3 (Ki 5.1x10-9 M) [87]
tecadenoson Pig Agonist 8.2 pKi 61,101
pKi 8.2 (Ki 6.5x10-9 M) [61,101]
2-chloroadenosine Rn Agonist 8.2 pKi 22
pKi 8.2 (Ki 6.7x10-9 M) [22]
compound 10 [PMID: 31306001] Hs Inverse agonist 8.1 pKi 7
pKi 8.1 (Ki 7.22x10-9 M) [7]
Description: Binding affinity calculated by measuring displacement of specific [3H]DPCPX binding at hA1ARs expressed in CHO cells.
cyclopentyladenosine Hs Full agonist 6.5 – 9.4 pKi 20,23,39,52,61-62,117
pKi 6.5 – 9.4 [20,23,39,52,61-62,117]
CCPA Hs Full agonist 7.7 – 8.1 pKi 61,106
pKi 7.7 – 8.1 [61,106]
MRS3558 Mm Agonist 7.8 pKi 83
pKi 7.8 (Ki 1.58x10-8 M) [83]
LUF5831 Hs Partial agonist 7.7 pKi 52
pKi 7.7 [52]
(R)-PIA Hs Full agonist 6.4 – 8.7 pKi 39,62,76,117,137
pKi 6.4 – 8.7 [39,62,76,117,137]
Cl-IB-MECA Mm Agonist 7.5 pKi 83
pKi 7.5 (Ki 3.5x10-8 M) [83]
piclidenoson Hs Agonist 7.3 pKi 61
pKi 7.3 (Ki 5.1x10-8 M) [61]
GS9667 Hs Agonist 7.3 pKi 32
pKi 7.3 (Ki 5.5x10-8 M) [32]
2-hexynyl-NECA Hs Full agonist 7.2 pKi 145
pKi 7.2 [145]
adenosine Rn Agonist 7.1 pKi 151
pKi 7.1 (Ki 7.3x10-8 M) [151]
apadenoson Hs Agonist 7.1 pKi 61
pKi 7.1 (Ki 7.7x10-8 M) [61]
adenosine Hs Agonist ~7.0 pKi 151
pKi ~7.0 (Ki ~1x10-7 M) [151]
MRS3558 Rn Agonist 7.0 pKi 83
pKi 7.0 (Ki 1.05x10-7 M) [83]
NECA Hs Full agonist 5.3 – 8.2 pKi 39,62,117,137,151
pKi 5.3 – 8.2 [39,62,117,137,151]
Cl-IB-MECA Hs Agonist 6.7 pKi 61
pKi 6.7 (Ki 2.2x10-7 M) [61]
MRS3558 Hs Agonist 6.6 pKi 61
pKi 6.6 (Ki 2.6x10-7 M) [61]
Cl-IB-MECA Rn Agonist 6.6 pKi 83
pKi 6.6 (Ki 2.8x10-7 M) [83]
HEMADO Hs Agonist 6.5 pKi 75,145
pKi 6.5 (Ki 3.3x10-7 M) [75,145]
PENECA Hs Full agonist 6.2 pKi 145
pKi 6.2 [145]
CGS 21680 Hs Full agonist 5.8 – 6.4 pKi 39,61
pKi 5.8 – 6.4 [39,61]
CGS 21680 Rn Agonist 5.7 pKi 83
pKi 5.7 (Ki 1.8x10-6 M) [83]
2-chloroadenosine Hs Full agonist 5.2 – 5.6 pKi 62,117
pKi 5.2 – 5.6 [62,117]
(S)-PIA Hs Full agonist 4.6 – 6.0 pKi 62,137
pKi 4.6 – 6.0 [62,137]
CP608,039 Hs Agonist 5.1 pKi 61
pKi 5.1 (Ki 7.3x10-6 M) [61]
BAY 60-6583 Hs Agonist <5.0 pKi 79
pKi <5.0 (Ki >1x10-5 M) [79]
regadenoson Hs Agonist <5.0 pKi 61
pKi <5.0 (Ki >1x10-5 M) [61]
MRS5151 Mm Agonist 5.0 pKi 95
pKi 5.0 (Ki 1.05x10-5 M) [95]
MRS5151 Hs Agonist 4.8 pKi 95
pKi 4.8 (Ki 1.49x10-5 M) [95]
binodenoson Hs Agonist 4.3 pKi 61
pKi 4.3 (Ki 4.8x10-5 M) [61]
MRS7469 Hs Agonist - - 136
[136]
View species-specific agonist tables
Agonist Comments
The role for adenosine as endogenous ligand for the A1 receptor is described in [35] and [36].

Tecadenoson (CV-510) is a selective A1 agonist with potential therapeutic use in controlling paroxysmal supraventricular tachycardia [110].
Primary target mapping: we have tagged the adenosine A1 receptor as the primary target for this endogenous ligand as the affinity is marginally higher at this receptor isoform. However, adenosine is likely to exert clinical effects via other adenosine receptor family members.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]DPCPX Hs Antagonist 8.4 – 9.2 pKd 20,33,76,108,117,137
pKd 8.4 – 9.2 (Kd 1.2x10-9 – 6x10-10 M) [20,33,76,108,117,137]
xanthine amine congener Hs Antagonist 7.5 pKd 34
pKd 7.5 [34]
PSB36 Rn Antagonist 9.9 pKi 1
pKi 9.9 (Ki 1.24x10-10 M) [1]
DPCPX Rn Antagonist 9.0 – 9.7 pKi 72,77,147
pKi 9.0 – 9.7 (Ki 1x10-9 – 1.8x10-10 M) [72,77,147]
CPFPX Rn Antagonist 9.2 pKi 55
pKi 9.2 (Ki 6.3x10-10 M) [55]
LUF5981 Hs Antagonist 9.1 pKi 15
pKi 9.1 (Ki 9x10-10 M) [15]
derenofylline Hs Antagonist 9.0 pKi 66
pKi 9.0 (Ki 1x10-9 M) [66]
FR194921 Hs Antagonist 8.9 pKi 90
pKi 8.9 [90]
CPFPX Hs Antagonist 8.9 pKi 55
pKi 8.9 (Ki 1.26x10-9 M) [55]
tonapofylline Rn Antagonist 8.9 pKi 71
pKi 8.9 (Ki 1.3x10-9 M) [71]
rolofylline Rn Antagonist 7.9 – 9.7 pKi 112
pKi 7.9 – 9.7 (Ki 1.26x10-8 – 1.9x10-10 M) [112]
WRC-0571 Hs Antagonist 8.8 pKi 93
pKi 8.8 [93]
rolofylline Hs Antagonist 8.1 – 9.1 pKi 71,112
pKi 8.1 – 9.1 (Ki 8x10-9 – 7.2x10-10 M) [71,112]
derenofylline Rn Antagonist 8.6 pKi 66
pKi 8.6 (Ki 2.51x10-9 M) [66]
CGS 15943 Hs Antagonist 8.5 pKi 108
pKi 8.5 (Ki 3.5x10-9 M) [108]
DPCPX Hs Antagonist 7.4 – 9.2 pKi 23,58,106,117,147
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.3x10-10 M) [23,58,106,117,147]
CGS 15943 Rn Antagonist 8.2 pKi 86
pKi 8.2 (Ki 6.4x10-9 M) [86]
tonapofylline Hs Antagonist 8.1 pKi 71
pKi 8.1 (Ki 7.4x10-9 M) [71]
MRS1754 Rn Antagonist 7.8 pKi 73
pKi 7.8 (Ki 1.68x10-8 M) [73]
8-cyclopentyltheophylline Hs Antagonist 7.5 – 8.0 pKi 20
pKi 7.5 – 8.0 [20]
FK-453 Hs Antagonist 7.7 pKi 61
pKi 7.7 (Ki 1.8x10-8 M) [61]
xanthine amine congener Hs Antagonist 7.6 pKi 62
pKi 7.6 [62]
DU172 Hs Antagonist 7.4 pKi 47
pKi 7.4 [47]
vipadenant Hs Antagonist 7.2 pKi 44
pKi 7.2 (Ki 6.8x10-8 M) [44]
ST-1535 Hs Antagonist 7.1 pKi 98
pKi 7.1 (Ki 7.18x10-8 M) [98]
MRE 2029F20 Hs Antagonist 6.7 pKi 6,141
pKi 6.7 [6,141]
istradefylline Rn Antagonist 6.6 pKi 37
pKi 6.6 (Ki 2.3x10-7 M) [37]
AS70 Hs Antagonist 6.6 pKi 141
pKi 6.6 [141]
AS100 Hs Antagonist 6.5 pKi 141
pKi 6.5 [141]
ATL802 Hs Antagonist 6.4 pKi 73
pKi 6.4 (Ki 3.69x10-7 M) [73]
MRS1754 Hs Antagonist 6.4 pKi 73
pKi 6.4 (Ki 4.03x10-7 M) [73]
PSB-11 Rn Antagonist 6.4 pKi 109
pKi 6.4 (Ki 4.4x10-7 M) [109]
ZM-241385 Hs Antagonist 6.1 – 6.6 pKi 61,108
pKi 6.1 – 6.6 [61,108]
MRS928 Rn Antagonist 6.3 pKi 70
pKi 6.3 [70]
L-97-1 Hs Antagonist 6.2 pKi 106
pKi 6.2 [106]
MRS1041 Rn Antagonist 6.2 pKi 70
pKi 6.2 [70]
SCH 58261 Hs Antagonist 6.1 – 6.3 pKi 61,108,137
pKi 6.1 – 6.3 [61,108,137]
mefloquine Hs Antagonist 6.2 pKi 146
pKi 6.2 (Ki 6.75x10-7 M) [146]
Description: Binding affinity determined by displacement of [3H]-DPCPX from human A1 receptors by increasing concentrations of racemic mefloquine.
AS99 Hs Antagonist 6.1 pKi 141
pKi 6.1 [141]
galangin Rn Antagonist 6.1 pKi 70
pKi 6.1 [70]
LUF7602 Hs Antagonist 6.1 pKi 153
pKi 6.1 (Ki 7.94x10-7 M) [153]
Description: Affinity determined from the displacement of specific [3H]DPCPX binding on CHO cell membranes stably expressing human adenosine A1 receptors at 25 °C during 2 h of incubation.
PSB-10 Rn Antagonist 6.1 pKi 103
pKi 6.1 (Ki 8.05x10-7 M) [103]
istradefylline Hs Antagonist 6.1 pKi 37
pKi 6.1 (Ki 8.41x10-7 M) [37]
MSX-2 Rn Antagonist 6.1 pKi 122
pKi 6.1 (Ki 9x10-7 M) [122]
MRS1042 Rn Antagonist 6.0 pKi 70
pKi 6.0 [70]
preladenant Hs Antagonist <6.0 pKi 100
pKi <6.0 (Ki >1x10-6 M) [100]
MRE 3008F20 Hs Antagonist 5.9 – 6.0 pKi 61,141-142
pKi 5.9 – 6.0 [61,141-142]
SCH442416 Hs Antagonist 5.9 pKi 61
pKi 5.9 (Ki 1.11x10-6 M) [61]
PSB-11 Hs Antagonist 5.8 pKi 109
pKi 5.8 (Ki 1.64x10-6 M) [109]
PSB-10 Hs Antagonist 5.8 pKi 109
pKi 5.8 (Ki 1.7x10-6 M) [109]
KF26777 Hs Antagonist 5.7 pKi 118
pKi 5.7 (Ki 1.8x10-6 M) [118]
CVT-6883 Hs Antagonist 5.7 pKi 31
pKi 5.7 (Ki 1.94x10-6 M) [31]
MRS1093 Rn Antagonist 5.7 pKi 70
pKi 5.7 [70]
PSB1115 Rn Antagonist 5.7 pKi 102
pKi 5.7 (Ki 2.2x10-6 M) [102]
MRS1132 Rn Antagonist 5.6 pKi 70
pKi 5.6 [70]
MSX-2 Hs Antagonist 5.6 pKi 122
pKi 5.6 (Ki 2.5x10-6 M) [122]
LAS38096 Hs Antagonist 5.6 pKi 30,143
pKi 5.6 (Ki 2.821x10-6 M) [30,143]
flavone Rn Antagonist 5.5 pKi 70
pKi 5.5 [70]
isobutylmethylxanthine Hs Antagonist 5.1 pKi 62
pKi 5.1 [62]
sakuranetin Rn Antagonist 5.1 pKi 70
pKi 5.1 [70]
theophylline Hs Antagonist 4.9 – 5.2 pKi 33,62,76,141
pKi 4.9 – 5.2 [33,62,76,141]
ATL802 Mm Antagonist 5.0 pKi 73
pKi 5.0 (Ki 9.583x10-6 M) [73]
MRS1191 Hs Antagonist <5.0 pKi 83
pKi <5.0 (Ki >1x10-5 M) [83]
MRS1523 Hs Antagonist <5.0 pKi 83
pKi <5.0 (Ki >1x10-5 M) [83]
VUF5574 Rn Antagonist >5.0 pKi 140
pKi >5.0 (Ki <1x10-5 M) [140]
PSB603 Hs Antagonist <5.0 pKi 11
pKi <5.0 (Ki >1x10-5 M) [11]
PSB603 Rn Antagonist <5.0 pKi 11
pKi <5.0 (Ki >1x10-5 M) [11]
PSB1115 Hs Antagonist <5.0 pKi 51
pKi <5.0 (Ki >1x10-5 M) [51]
theophylline Rn Antagonist 4.8 – 5.1 pKi 59,102
pKi 4.8 – 5.1 (Ki 1.4x10-5 – 8.74x10-6 M) [59,102]
morin Rn Antagonist 4.9 pKi 70
pKi 4.9 [70]
MRS1523 Rn Antagonist 4.8 pKi 83
pKi 4.8 (Ki 1.56x10-5 M) [83]
caffeine Hs Antagonist 4.3 – 5.0 pKi 1,25,59
pKi 4.3 – 5.0 (Ki 4.49x10-5 – 1.07x10-5 M) [1,25,59]
MRS923 Rn Antagonist 4.6 pKi 70
pKi 4.6 [70]
CSC Rn Antagonist 4.6 pKi