A1 receptor

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

   GtoImmuPdb view: OFF :     Currently no data for A1 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 326 1q32.1 ADORA1 adenosine A1 receptor 82,112,135
Mouse 7 326 1 E4 Adora1 adenosine A1 receptor 90,144
Rat 7 326 13q13 Adora1 adenosine A1 receptor 89
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:  45
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:  15
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]CCPA Hs Full agonist 9.2 pKd 73,115
pKd 9.2 (Kd 6.31x10-10 M) [73,115]
5-Cl-5-deoxy-(±)-ENBA Hs Full agonist 9.3 pKi 32
pKi 9.3 (Ki 5.1x10-10 M) [32]
N(6)-cyclohexyladenosine Rn Agonist 9.1 pKi 21
pKi 9.1 (Ki 8.5x10-10 M) [21]
(R)-PIA Rn Agonist 8.9 pKi 21
pKi 8.9 (Ki 1.2x10-9 M) [21]
CCPA Rn Agonist 8.9 pKi 81
pKi 8.9 (Ki 1.3x10-9 M) [81]
(R,S)-PHPNECA Hs Full agonist 8.6 pKi 142
pKi 8.6 [142]
TCPA Hs Agonist 8.6 pKi 7
pKi 8.6 (Ki 2.8x10-9 M) [7]
GR79236 Rn Agonist 8.5 pKi 59
pKi 8.5 (Ki 3.1x10-9 M) [59]
NECA Rn Agonist 8.3 pKi 85
pKi 8.3 (Ki 5.1x10-9 M) [85]
tecadenoson Pig Agonist 8.2 pKi 59,99
pKi 8.2 (Ki 6.5x10-9 M) [59,99]
2-chloroadenosine Rn Agonist 8.2 pKi 21
pKi 8.2 (Ki 6.7x10-9 M) [21]
cyclopentyladenosine Hs Full agonist 6.5 – 9.4 pKi 19,22,37,50,59-60,115
pKi 6.5 – 9.4 [19,22,37,50,59-60,115]
CCPA Hs Full agonist 7.7 – 8.1 pKi 59,104
pKi 7.7 – 8.1 [59,104]
MRS3558 Mm Agonist 7.8 pKi 81
pKi 7.8 (Ki 1.58x10-8 M) [81]
LUF5831 Hs Partial agonist 7.7 pKi 50
pKi 7.7 [50]
(R)-PIA Hs Full agonist 6.4 – 8.7 pKi 37,60,73,115,134
pKi 6.4 – 8.7 [37,60,73,115,134]
Cl-IB-MECA Mm Agonist 7.5 pKi 81
pKi 7.5 (Ki 3.5x10-8 M) [81]
piclidenoson Hs Agonist 7.3 pKi 59
pKi 7.3 (Ki 5.1x10-8 M) [59]
GS9667 Hs Agonist 7.3 pKi 30
pKi 7.3 (Ki 5.5x10-8 M) [30]
2-hexynyl-NECA Hs Full agonist 7.2 pKi 142
pKi 7.2 [142]
adenosine Rn Agonist 7.1 pKi 147
pKi 7.1 (Ki 7.3x10-8 M) [147]
apadenoson Hs Agonist 7.1 pKi 59
pKi 7.1 (Ki 7.7x10-8 M) [59]
adenosine Hs Agonist ~7.0 pKi 147
pKi ~7.0 (Ki ~1x10-7 M) [147]
MRS3558 Rn Agonist 7.0 pKi 81
pKi 7.0 (Ki 1.05x10-7 M) [81]
NECA Hs Full agonist 5.3 – 8.2 pKi 37,60,115,134,147
pKi 5.3 – 8.2 [37,60,115,134,147]
Cl-IB-MECA Hs Agonist 6.7 pKi 59
pKi 6.7 (Ki 2.2x10-7 M) [59]
MRS3558 Hs Agonist 6.6 pKi 59
pKi 6.6 (Ki 2.6x10-7 M) [59]
Cl-IB-MECA Rn Agonist 6.6 pKi 81
pKi 6.6 (Ki 2.8x10-7 M) [81]
HEMADO Hs Agonist 6.5 pKi 74,142
pKi 6.5 (Ki 3.3x10-7 M) [74,142]
PENECA Hs Full agonist 6.2 pKi 142
pKi 6.2 [142]
CGS 21680 Hs Full agonist 5.8 – 6.4 pKi 37,59
pKi 5.8 – 6.4 [37,59]
CGS 21680 Rn Agonist 5.7 pKi 81
pKi 5.7 (Ki 1.8x10-6 M) [81]
2-chloroadenosine Hs Full agonist 5.2 – 5.6 pKi 60,115
pKi 5.2 – 5.6 [60,115]
(S)-PIA Hs Full agonist 4.6 – 6.0 pKi 60,134
pKi 4.6 – 6.0 [60,134]
CP608,039 Hs Agonist 5.1 pKi 59
pKi 5.1 (Ki 7.3x10-6 M) [59]
BAY 60-6583 Hs Agonist <5.0 pKi 77
pKi <5.0 (Ki >1x10-5 M) [77]
regadenoson Hs Agonist <5.0 pKi 59
pKi <5.0 (Ki >1x10-5 M) [59]
MRS5151 Mm Agonist 5.0 pKi 93
pKi 5.0 (Ki 1.05x10-5 M) [93]
MRS5151 Hs Agonist 4.8 pKi 93
pKi 4.8 (Ki 1.49x10-5 M) [93]
binodenoson Hs Agonist 4.3 pKi 59
pKi 4.3 (Ki 4.8x10-5 M) [59]
View species-specific agonist tables
Agonist Comments
The role for adenosine as endogenous ligand for the A1 receptor is described in [33] and [34].

Tecadenoson (CV-510) is a selective A1 agonist with potential therapeutic use in controlling paroxysmal supraventricular tachycardia [108].
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 Affinity Units Reference
[3H]DPCPX Hs Antagonist 8.4 – 9.2 pKd 19,31,73,106,115,134
pKd 8.4 – 9.2 (Kd 1.2x10-9 – 6x10-10 M) [19,31,73,106,115,134]
xanthine amine congener Hs Antagonist 7.5 pKd 32
pKd 7.5 [32]
PSB36 Rn Antagonist 9.9 pKi 1
pKi 9.9 (Ki 1.24x10-10 M) [1]
DPCPX Rn Antagonist 9.0 – 9.7 pKi 70,75,143
pKi 9.0 – 9.7 (Ki 1x10-9 – 1.8x10-10 M) [70,75,143]
CPFPX Rn Antagonist 9.2 pKi 53
pKi 9.2 (Ki 6.3x10-10 M) [53]
LUF5981 Hs Antagonist 9.1 pKi 14
pKi 9.1 (Ki 9x10-10 M) [14]
derenofylline Hs Antagonist 9.0 pKi 64
pKi 9.0 (Ki 1x10-9 M) [64]
FR194921 Hs Antagonist 8.9 pKi 88
pKi 8.9 [88]
CPFPX Hs Antagonist 8.9 pKi 53
pKi 8.9 (Ki 1.26x10-9 M) [53]
tonapofylline Rn Antagonist 8.9 pKi 69
pKi 8.9 (Ki 1.3x10-9 M) [69]
rolofylline Rn Antagonist 7.9 – 9.7 pKi 110
pKi 7.9 – 9.7 (Ki 1.26x10-8 – 1.9x10-10 M) [110]
WRC-0571 Hs Antagonist 8.8 pKi 91
pKi 8.8 [91]
rolofylline Hs Antagonist 8.1 – 9.1 pKi 69,110
pKi 8.1 – 9.1 (Ki 8x10-9 – 7.2x10-10 M) [69,110]
derenofylline Rn Antagonist 8.6 pKi 64
pKi 8.6 (Ki 2.51x10-9 M) [64]
CGS 15943 Hs Antagonist 8.5 pKi 106
pKi 8.5 (Ki 3.5x10-9 M) [106]
DPCPX Hs Antagonist 7.4 – 9.2 pKi 22,56,104,115,143
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.3x10-10 M) [22,56,104,115,143]
CGS 15943 Rn Antagonist 8.2 pKi 84
pKi 8.2 (Ki 6.4x10-9 M) [84]
tonapofylline Hs Antagonist 8.1 pKi 69
pKi 8.1 (Ki 7.4x10-9 M) [69]
MRS1754 Rn Antagonist 7.8 pKi 71
pKi 7.8 (Ki 1.68x10-8 M) [71]
8-cyclopentyltheophylline Hs Antagonist 7.5 – 8.0 pKi 19
pKi 7.5 – 8.0 [19]
FK-453 Hs Antagonist 7.7 pKi 59
pKi 7.7 (Ki 1.8x10-8 M) [59]
xanthine amine congener Hs Antagonist 7.6 pKi 60
pKi 7.6 [60]
DU172 Hs Antagonist 7.4 pKi 45
pKi 7.4 [45]
vipadenant Hs Antagonist 7.2 pKi 42
pKi 7.2 (Ki 6.8x10-8 M) [42]
ST-1535 Hs Antagonist 7.1 pKi 96
pKi 7.1 (Ki 7.18x10-8 M) [96]
MRE 2029F20 Hs Antagonist 6.7 pKi 6,138
pKi 6.7 [6,138]
istradefylline Rn Antagonist 6.6 pKi 35
pKi 6.6 (Ki 2.3x10-7 M) [35]
AS70 Hs Antagonist 6.6 pKi 138
pKi 6.6 [138]
AS100 Hs Antagonist 6.5 pKi 138
pKi 6.5 [138]
ATL802 Hs Antagonist 6.4 pKi 71
pKi 6.4 (Ki 3.69x10-7 M) [71]
MRS1754 Hs Antagonist 6.4 pKi 71
pKi 6.4 (Ki 4.03x10-7 M) [71]
PSB-11 Rn Antagonist 6.4 pKi 107
pKi 6.4 (Ki 4.4x10-7 M) [107]
ZM-241385 Hs Antagonist 6.1 – 6.6 pKi 59,106
pKi 6.1 – 6.6 [59,106]
MRS928 Rn Antagonist 6.3 pKi 68
pKi 6.3 [68]
L-97-1 Hs Antagonist 6.2 pKi 104
pKi 6.2 [104]
MRS1041 Rn Antagonist 6.2 pKi 68
pKi 6.2 [68]
SCH 58261 Hs Antagonist 6.1 – 6.3 pKi 59,106,134
pKi 6.1 – 6.3 [59,106,134]
AS99 Hs Antagonist 6.1 pKi 138
pKi 6.1 [138]
galangin Rn Antagonist 6.1 pKi 68
pKi 6.1 [68]
PSB-10 Rn Antagonist 6.1 pKi 101
pKi 6.1 (Ki 8.05x10-7 M) [101]
istradefylline Hs Antagonist 6.1 pKi 35
pKi 6.1 (Ki 8.41x10-7 M) [35]
MSX-2 Rn Antagonist 6.1 pKi 120
pKi 6.1 (Ki 9x10-7 M) [120]
MRS1042 Rn Antagonist 6.0 pKi 68
pKi 6.0 [68]
preladenant Hs Antagonist <6.0 pKi 98
pKi <6.0 (Ki >1x10-6 M) [98]
MRE 3008F20 Hs Antagonist 5.9 – 6.0 pKi 59,138-139
pKi 5.9 – 6.0 [59,138-139]
SCH442416 Hs Antagonist 5.9 pKi 59
pKi 5.9 (Ki 1.11x10-6 M) [59]
PSB-11 Hs Antagonist 5.8 pKi 107
pKi 5.8 (Ki 1.64x10-6 M) [107]
PSB-10 Hs Antagonist 5.8 pKi 107
pKi 5.8 (Ki 1.7x10-6 M) [107]
KF26777 Hs Antagonist 5.7 pKi 116
pKi 5.7 (Ki 1.8x10-6 M) [116]
CVT-6883 Hs Antagonist 5.7 pKi 29
pKi 5.7 (Ki 1.94x10-6 M) [29]
MRS1093 Rn Antagonist 5.7 pKi 68
pKi 5.7 [68]
PSB1115 Rn Antagonist 5.7 pKi 100
pKi 5.7 (Ki 2.2x10-6 M) [100]
MRS1132 Rn Antagonist 5.6 pKi 68
pKi 5.6 [68]
MSX-2 Hs Antagonist 5.6 pKi 120
pKi 5.6 (Ki 2.5x10-6 M) [120]
LAS38096 Hs Antagonist 5.6 pKi 28,140
pKi 5.6 (Ki 2.821x10-6 M) [28,140]
flavone Rn Antagonist 5.5 pKi 68
pKi 5.5 [68]
isobutylmethylxanthine Hs Antagonist 5.1 pKi 60
pKi 5.1 [60]
sakuranetin Rn Antagonist 5.1 pKi 68
pKi 5.1 [68]
theophylline Hs Antagonist 4.9 – 5.2 pKi 31,60,73,138
pKi 4.9 – 5.2 [31,60,73,138]
ATL802 Mm Antagonist 5.0 pKi 71
pKi 5.0 (Ki 9.583x10-6 M) [71]
MRS1191 Hs Antagonist <5.0 pKi 81
pKi <5.0 (Ki >1x10-5 M) [81]
MRS1523 Hs Antagonist <5.0 pKi 81
pKi <5.0 (Ki >1x10-5 M) [81]
VUF5574 Rn Antagonist >5.0 pKi 137
pKi >5.0 (Ki <1x10-5 M) [137]
PSB603 Hs Antagonist <5.0 pKi 10
pKi <5.0 (Ki >1x10-5 M) [10]
PSB603 Rn Antagonist <5.0 pKi 10
pKi <5.0 (Ki >1x10-5 M) [10]
PSB1115 Hs Antagonist <5.0 pKi 49
pKi <5.0 (Ki >1x10-5 M) [49]
theophylline Rn Antagonist 4.8 – 5.1 pKi 57,100
pKi 4.8 – 5.1 (Ki 1.4x10-5 – 8.74x10-6 M) [57,100]
morin Rn Antagonist 4.9 pKi 68
pKi 4.9 [68]
MRS1523 Rn Antagonist 4.8 pKi 81
pKi 4.8 (Ki 1.56x10-5 M) [81]
caffeine Hs Antagonist 4.3 – 5.0 pKi 1,24,57
pKi 4.3 – 5.0 (Ki 4.49x10-5 – 1.07x10-5 M) [1,24,57]
MRS923 Rn Antagonist 4.6 pKi 68
pKi 4.6 [68]
CSC Rn Antagonist 4.6 pKi 58
pKi 4.6 (Ki 2.8x10-5 M) [58]
MRS1065 Rn Antagonist 4.5 pKi 68
pKi 4.5 [68]
MRS1086 Rn Antagonist 4.5 pKi 68
pKi 4.5 [68]
flavanone Rn Antagonist 4.5 pKi 68
pKi 4.5 [68]
MRS1066 Rn Antagonist 4.4 pKi 68
pKi 4.4 [68]
MRS1084 Rn Antagonist 4.4 pKi 68
pKi 4.4 [68]
MRS1191 Rn Antagonist 4.4 pKi 81
pKi 4.4 (Ki 4.01x10-5 M) [81]
caffeine Rn Antagonist 4.4 – 4.4 pKi 20,47
pKi 4.4 – 4.4 (Ki 4.4x10-5 – 4.1x10-5 M) [20,47]
MRS1062 Rn Antagonist 4.3 pKi 68
pKi 4.3 [68]
LUF5962 Hs Antagonist 7.1 pIC50 48
pIC50 7.1 [48]