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 83,113,136
Mouse 7 326 1 E4 Adora1 adenosine A1 receptor 91,145
Rat 7 326 13q13 Adora1 adenosine A1 receptor 90
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:  46
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
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:  27
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 74,116
pKd 9.2 (Kd 6.31x10-10 M) [74,116]
5-Cl-5-deoxy-(±)-ENBA Hs Full agonist 9.3 pKi 33
pKi 9.3 (Ki 5.1x10-10 M) [33]
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 82
pKi 8.9 (Ki 1.3x10-9 M) [82]
(R,S)-PHPNECA Hs Full agonist 8.6 pKi 143
pKi 8.6 [143]
TCPA Hs Agonist 8.6 pKi 7
pKi 8.6 (Ki 2.8x10-9 M) [7]
GR79236 Rn Agonist 8.5 pKi 60
pKi 8.5 (Ki 3.1x10-9 M) [60]
NECA Rn Agonist 8.3 pKi 86
pKi 8.3 (Ki 5.1x10-9 M) [86]
tecadenoson Pig Agonist 8.2 pKi 60,100
pKi 8.2 (Ki 6.5x10-9 M) [60,100]
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 19,22,38,51,60-61,116
pKi 6.5 – 9.4 [19,22,38,51,60-61,116]
CCPA Hs Full agonist 7.7 – 8.1 pKi 60,105
pKi 7.7 – 8.1 [60,105]
MRS3558 Mm Agonist 7.8 pKi 82
pKi 7.8 (Ki 1.58x10-8 M) [82]
LUF5831 Hs Partial agonist 7.7 pKi 51
pKi 7.7 [51]
(R)-PIA Hs Full agonist 6.4 – 8.7 pKi 38,61,74,116,135
pKi 6.4 – 8.7 [38,61,74,116,135]
Cl-IB-MECA Mm Agonist 7.5 pKi 82
pKi 7.5 (Ki 3.5x10-8 M) [82]
piclidenoson Hs Agonist 7.3 pKi 60
pKi 7.3 (Ki 5.1x10-8 M) [60]
GS9667 Hs Agonist 7.3 pKi 31
pKi 7.3 (Ki 5.5x10-8 M) [31]
2-hexynyl-NECA Hs Full agonist 7.2 pKi 143
pKi 7.2 [143]
adenosine Rn Agonist 7.1 pKi 148
pKi 7.1 (Ki 7.3x10-8 M) [148]
apadenoson Hs Agonist 7.1 pKi 60
pKi 7.1 (Ki 7.7x10-8 M) [60]
adenosine Hs Agonist ~7.0 pKi 148
pKi ~7.0 (Ki ~1x10-7 M) [148]
MRS3558 Rn Agonist 7.0 pKi 82
pKi 7.0 (Ki 1.05x10-7 M) [82]
NECA Hs Full agonist 5.3 – 8.2 pKi 38,61,116,135,148
pKi 5.3 – 8.2 [38,61,116,135,148]
Cl-IB-MECA Hs Agonist 6.7 pKi 60
pKi 6.7 (Ki 2.2x10-7 M) [60]
MRS3558 Hs Agonist 6.6 pKi 60
pKi 6.6 (Ki 2.6x10-7 M) [60]
Cl-IB-MECA Rn Agonist 6.6 pKi 82
pKi 6.6 (Ki 2.8x10-7 M) [82]
HEMADO Hs Agonist 6.5 pKi 75,143
pKi 6.5 (Ki 3.3x10-7 M) [75,143]
PENECA Hs Full agonist 6.2 pKi 143
pKi 6.2 [143]
CGS 21680 Hs Full agonist 5.8 – 6.4 pKi 38,60
pKi 5.8 – 6.4 [38,60]
CGS 21680 Rn Agonist 5.7 pKi 82
pKi 5.7 (Ki 1.8x10-6 M) [82]
2-chloroadenosine Hs Full agonist 5.2 – 5.6 pKi 61,116
pKi 5.2 – 5.6 [61,116]
(S)-PIA Hs Full agonist 4.6 – 6.0 pKi 61,135
pKi 4.6 – 6.0 [61,135]
CP608,039 Hs Agonist 5.1 pKi 60
pKi 5.1 (Ki 7.3x10-6 M) [60]
BAY 60-6583 Hs Agonist <5.0 pKi 78
pKi <5.0 (Ki >1x10-5 M) [78]
regadenoson Hs Agonist <5.0 pKi 60
pKi <5.0 (Ki >1x10-5 M) [60]
MRS5151 Mm Agonist 5.0 pKi 94
pKi 5.0 (Ki 1.05x10-5 M) [94]
MRS5151 Hs Agonist 4.8 pKi 94
pKi 4.8 (Ki 1.49x10-5 M) [94]
binodenoson Hs Agonist 4.3 pKi 60
pKi 4.3 (Ki 4.8x10-5 M) [60]
View species-specific agonist tables
Agonist Comments
The role for adenosine as endogenous ligand for the A1 receptor is described in [34] and [35].

Tecadenoson (CV-510) is a selective A1 agonist with potential therapeutic use in controlling paroxysmal supraventricular tachycardia [109].
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 19,32,74,107,116,135
pKd 8.4 – 9.2 (Kd 1.2x10-9 – 6x10-10 M) [19,32,74,107,116,135]
xanthine amine congener Hs Antagonist 7.5 pKd 33
pKd 7.5 [33]
PSB36 Rn Antagonist 9.9 pKi 1
pKi 9.9 (Ki 1.24x10-10 M) [1]
DPCPX Rn Antagonist 9.0 – 9.7 pKi 71,76,144
pKi 9.0 – 9.7 (Ki 1x10-9 – 1.8x10-10 M) [71,76,144]
CPFPX Rn Antagonist 9.2 pKi 54
pKi 9.2 (Ki 6.3x10-10 M) [54]
LUF5981 Hs Antagonist 9.1 pKi 14
pKi 9.1 (Ki 9x10-10 M) [14]
derenofylline Hs Antagonist 9.0 pKi 65
pKi 9.0 (Ki 1x10-9 M) [65]
FR194921 Hs Antagonist 8.9 pKi 89
pKi 8.9 [89]
CPFPX Hs Antagonist 8.9 pKi 54
pKi 8.9 (Ki 1.26x10-9 M) [54]
tonapofylline Rn Antagonist 8.9 pKi 70
pKi 8.9 (Ki 1.3x10-9 M) [70]
rolofylline Rn Antagonist 7.9 – 9.7 pKi 111
pKi 7.9 – 9.7 (Ki 1.26x10-8 – 1.9x10-10 M) [111]
WRC-0571 Hs Antagonist 8.8 pKi 92
pKi 8.8 [92]
rolofylline Hs Antagonist 8.1 – 9.1 pKi 70,111
pKi 8.1 – 9.1 (Ki 8x10-9 – 7.2x10-10 M) [70,111]
derenofylline Rn Antagonist 8.6 pKi 65
pKi 8.6 (Ki 2.51x10-9 M) [65]
CGS 15943 Hs Antagonist 8.5 pKi 107
pKi 8.5 (Ki 3.5x10-9 M) [107]
DPCPX Hs Antagonist 7.4 – 9.2 pKi 22,57,105,116,144
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.3x10-10 M) [22,57,105,116,144]
CGS 15943 Rn Antagonist 8.2 pKi 85
pKi 8.2 (Ki 6.4x10-9 M) [85]
tonapofylline Hs Antagonist 8.1 pKi 70
pKi 8.1 (Ki 7.4x10-9 M) [70]
MRS1754 Rn Antagonist 7.8 pKi 72
pKi 7.8 (Ki 1.68x10-8 M) [72]
8-cyclopentyltheophylline Hs Antagonist 7.5 – 8.0 pKi 19
pKi 7.5 – 8.0 [19]
FK-453 Hs Antagonist 7.7 pKi 60
pKi 7.7 (Ki 1.8x10-8 M) [60]
xanthine amine congener Hs Antagonist 7.6 pKi 61
pKi 7.6 [61]
DU172 Hs Antagonist 7.4 pKi 46
pKi 7.4 [46]
vipadenant Hs Antagonist 7.2 pKi 43
pKi 7.2 (Ki 6.8x10-8 M) [43]
ST-1535 Hs Antagonist 7.1 pKi 97
pKi 7.1 (Ki 7.18x10-8 M) [97]
MRE 2029F20 Hs Antagonist 6.7 pKi 6,139
pKi 6.7 [6,139]
istradefylline Rn Antagonist 6.6 pKi 36
pKi 6.6 (Ki 2.3x10-7 M) [36]
AS70 Hs Antagonist 6.6 pKi 139
pKi 6.6 [139]
AS100 Hs Antagonist 6.5 pKi 139
pKi 6.5 [139]
ATL802 Hs Antagonist 6.4 pKi 72
pKi 6.4 (Ki 3.69x10-7 M) [72]
MRS1754 Hs Antagonist 6.4 pKi 72
pKi 6.4 (Ki 4.03x10-7 M) [72]
PSB-11 Rn Antagonist 6.4 pKi 108
pKi 6.4 (Ki 4.4x10-7 M) [108]
ZM-241385 Hs Antagonist 6.1 – 6.6 pKi 60,107
pKi 6.1 – 6.6 [60,107]
MRS928 Rn Antagonist 6.3 pKi 69
pKi 6.3 [69]
L-97-1 Hs Antagonist 6.2 pKi 105
pKi 6.2 [105]
MRS1041 Rn Antagonist 6.2 pKi 69
pKi 6.2 [69]
SCH 58261 Hs Antagonist 6.1 – 6.3 pKi 60,107,135
pKi 6.1 – 6.3 [60,107,135]
AS99 Hs Antagonist 6.1 pKi 139
pKi 6.1 [139]
galangin Rn Antagonist 6.1 pKi 69
pKi 6.1 [69]
PSB-10 Rn Antagonist 6.1 pKi 102
pKi 6.1 (Ki 8.05x10-7 M) [102]
istradefylline Hs Antagonist 6.1 pKi 36
pKi 6.1 (Ki 8.41x10-7 M) [36]
MSX-2 Rn Antagonist 6.1 pKi 121
pKi 6.1 (Ki 9x10-7 M) [121]
MRS1042 Rn Antagonist 6.0 pKi 69
pKi 6.0 [69]
preladenant Hs Antagonist <6.0 pKi 99
pKi <6.0 (Ki >1x10-6 M) [99]
MRE 3008F20 Hs Antagonist 5.9 – 6.0 pKi 60,139-140
pKi 5.9 – 6.0 [60,139-140]
SCH442416 Hs Antagonist 5.9 pKi 60
pKi 5.9 (Ki 1.11x10-6 M) [60]
PSB-11 Hs Antagonist 5.8 pKi 108
pKi 5.8 (Ki 1.64x10-6 M) [108]
PSB-10 Hs Antagonist 5.8 pKi 108
pKi 5.8 (Ki 1.7x10-6 M) [108]
KF26777 Hs Antagonist 5.7 pKi 117
pKi 5.7 (Ki 1.8x10-6 M) [117]
CVT-6883 Hs Antagonist 5.7 pKi 30
pKi 5.7 (Ki 1.94x10-6 M) [30]
MRS1093 Rn Antagonist 5.7 pKi 69
pKi 5.7 [69]
PSB1115 Rn Antagonist 5.7 pKi 101
pKi 5.7 (Ki 2.2x10-6 M) [101]
MRS1132 Rn Antagonist 5.6 pKi 69
pKi 5.6 [69]
MSX-2 Hs Antagonist 5.6 pKi 121
pKi 5.6 (Ki 2.5x10-6 M) [121]
LAS38096 Hs Antagonist 5.6 pKi 29,141
pKi 5.6 (Ki 2.821x10-6 M) [29,141]
flavone Rn Antagonist 5.5 pKi 69
pKi 5.5 [69]
isobutylmethylxanthine Hs Antagonist 5.1 pKi 61
pKi 5.1 [61]
sakuranetin Rn Antagonist 5.1 pKi 69
pKi 5.1 [69]
theophylline Hs Antagonist 4.9 – 5.2 pKi 32,61,74,139
pKi 4.9 – 5.2 [32,61,74,139]
ATL802 Mm Antagonist 5.0 pKi 72
pKi 5.0 (Ki 9.583x10-6 M) [72]
MRS1191 Hs Antagonist <5.0 pKi 82
pKi <5.0 (Ki >1x10-5 M) [82]
MRS1523 Hs Antagonist <5.0 pKi 82
pKi <5.0 (Ki >1x10-5 M) [82]
VUF5574 Rn Antagonist >5.0 pKi 138
pKi >5.0 (Ki <1x10-5 M) [138]
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 50
pKi <5.0 (Ki >1x10-5 M) [50]
theophylline Rn Antagonist 4.8 – 5.1 pKi 58,101
pKi 4.8 – 5.1 (Ki 1.4x10-5 – 8.74x10-6 M) [58,101]
morin Rn Antagonist 4.9 pKi 69
pKi 4.9 [69]
MRS1523 Rn Antagonist 4.8 pKi 82
pKi 4.8 (Ki 1.56x10-5 M) [82]
caffeine Hs Antagonist 4.3 – 5.0 pKi 1,24,58
pKi 4.3 – 5.0 (Ki 4.49x10-5 – 1.07x10-5 M) [1,24,58]
MRS923 Rn Antagonist 4.6 pKi 69
pKi 4.6 [69]
CSC Rn Antagonist 4.6 pKi 59
pKi 4.6 (Ki 2.8x10-5 M) [59]
MRS1065 Rn Antagonist 4.5 pKi 69
pKi 4.5 [69]
MRS1086 Rn Antagonist 4.5 pKi 69
pKi 4.5 [69]
flavanone Rn Antagonist 4.5 pKi 69
pKi 4.5 [69]
MRS1066 Rn Antagonist 4.4 pKi 69
pKi 4.4 [69]
MRS1084 Rn Antagonist 4.4 pKi 69
pKi 4.4 [69]
MRS1191 Rn Antagonist 4.4 pKi 82
pKi 4.4 (Ki 4.01x10-5 M) [82]
caffeine Rn Antagonist 4.4 – 4.4 pKi 20,48
pKi 4.4 – 4.4 (Ki 4.4x10-5 – 4.1x10-5 M) [20,48]
MRS1062 Rn Antagonist 4.3 pKi 69
pKi 4.3 [69]
LUF5962