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 80,109,132
Mouse 7 326 1 E4 Adora1 adenosine A1 receptor 88,141
Rat 7 326 13q13 Adora1 adenosine A1 receptor 87
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
GenitoUrinary Development Molecular Anatomy Project
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:  44
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 71,112
pKd 9.2 (Kd 6.31x10-10 M) [71,112]
5-Cl-5-deoxy-(±)-ENBA Hs Full agonist 9.3 pKi 31
pKi 9.3 (Ki 5.1x10-10 M) [31]
N(6)-cyclohexyladenosine Rn Agonist 9.1 pKi 20
pKi 9.1 (Ki 8.5x10-10 M) [20]
(R)-PIA Rn Agonist 8.9 pKi 20
pKi 8.9 (Ki 1.2x10-9 M) [20]
CCPA Rn Agonist 8.9 pKi 79
pKi 8.9 (Ki 1.3x10-9 M) [79]
(R,S)-PHPNECA Hs Full agonist 8.6 pKi 139
pKi 8.6 [139]
TCPA Hs Agonist 8.6 pKi 7
pKi 8.6 (Ki 2.8x10-9 M) [7]
GR79236 Rn Agonist 8.5 pKi 57
pKi 8.5 (Ki 3.1x10-9 M) [57]
NECA Rn Agonist 8.3 pKi 83
pKi 8.3 (Ki 5.1x10-9 M) [83]
tecadenoson Pig Agonist 8.2 pKi 57,97
pKi 8.2 (Ki 6.5x10-9 M) [57,97]
2-chloroadenosine Rn Agonist 8.2 pKi 20
pKi 8.2 (Ki 6.7x10-9 M) [20]
cyclopentyladenosine Hs Full agonist 6.5 – 9.4 pKi 18,21,36,48,57-58,112
pKi 6.5 – 9.4 [18,21,36,48,57-58,112]
CCPA Hs Full agonist 7.7 – 8.1 pKi 57,101
pKi 7.7 – 8.1 [57,101]
MRS3558 Mm Agonist 7.8 pKi 79
pKi 7.8 (Ki 1.58x10-8 M) [79]
LUF5831 Hs Partial agonist 7.7 pKi 48
pKi 7.7 [48]
(R)-PIA Hs Full agonist 6.4 – 8.7 pKi 36,58,71,112,131
pKi 6.4 – 8.7 [36,58,71,112,131]
Cl-IB-MECA Mm Agonist 7.5 pKi 79
pKi 7.5 (Ki 3.5x10-8 M) [79]
piclidenoson Hs Agonist 7.3 pKi 57
pKi 7.3 (Ki 5.1x10-8 M) [57]
GS9667 Hs Agonist 7.3 pKi 29
pKi 7.3 (Ki 5.5x10-8 M) [29]
2-hexynyl-NECA Hs Full agonist 7.2 pKi 139
pKi 7.2 [139]
adenosine Rn Agonist 7.1 pKi 144
pKi 7.1 (Ki 7.3x10-8 M) [144]
apadenoson Hs Agonist 7.1 pKi 57
pKi 7.1 (Ki 7.7x10-8 M) [57]
adenosine Hs Agonist ~7.0 pKi 144
pKi ~7.0 (Ki ~1x10-7 M) [144]
MRS3558 Rn Agonist 7.0 pKi 79
pKi 7.0 (Ki 1.05x10-7 M) [79]
NECA Hs Full agonist 5.3 – 8.2 pKi 36,58,112,131,144
pKi 5.3 – 8.2 [36,58,112,131,144]
Cl-IB-MECA Hs Agonist 6.7 pKi 57
pKi 6.7 (Ki 2.2x10-7 M) [57]
MRS3558 Hs Agonist 6.6 pKi 57
pKi 6.6 (Ki 2.6x10-7 M) [57]
Cl-IB-MECA Rn Agonist 6.6 pKi 79
pKi 6.6 (Ki 2.8x10-7 M) [79]
HEMADO Hs Agonist 6.5 pKi 72,139
pKi 6.5 (Ki 3.3x10-7 M) [72,139]
PENECA Hs Full agonist 6.2 pKi 139
pKi 6.2 [139]
CGS 21680 Hs Full agonist 5.8 – 6.4 pKi 36,57
pKi 5.8 – 6.4 [36,57]
CGS 21680 Rn Agonist 5.7 pKi 79
pKi 5.7 (Ki 1.8x10-6 M) [79]
2-chloroadenosine Hs Full agonist 5.2 – 5.6 pKi 58,112
pKi 5.2 – 5.6 [58,112]
(S)-PIA Hs Full agonist 4.6 – 6.0 pKi 58,131
pKi 4.6 – 6.0 [58,131]
CP608,039 Hs Agonist 5.1 pKi 57
pKi 5.1 (Ki 7.3x10-6 M) [57]
BAY 60-6583 Hs Agonist <5.0 pKi 75
pKi <5.0 (Ki >1x10-5 M) [75]
regadenoson Hs Agonist <5.0 pKi 57
pKi <5.0 (Ki >1x10-5 M) [57]
MRS5151 Mm Agonist 5.0 pKi 91
pKi 5.0 (Ki 1.05x10-5 M) [91]
MRS5151 Hs Agonist 4.8 pKi 91
pKi 4.8 (Ki 1.49x10-5 M) [91]
binodenoson Hs Agonist 4.3 pKi 57
pKi 4.3 (Ki 4.8x10-5 M) [57]
View species-specific agonist tables
Agonist Comments
The role for adenosine as endogenous ligand for the A1 receptor is described in [32] and [33].

Tecadenoson (CV-510) is a selective A1 agonist with potential therapeutic use in controlling paroxysmal supraventricular tachycardia [105].
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 18,30,71,103,112,131
pKd 8.4 – 9.2 (Kd 1.2x10-9 – 6x10-10 M) [18,30,71,103,112,131]
xanthine amine congener Hs Antagonist 7.5 pKd 31
pKd 7.5 [31]
PSB36 Rn Antagonist 9.9 pKi 1
pKi 9.9 (Ki 1.24x10-10 M) [1]
DPCPX Rn Antagonist 9.0 – 9.7 pKi 68,73,140
pKi 9.0 – 9.7 (Ki 1x10-9 – 1.8x10-10 M) [68,73,140]
CPFPX Rn Antagonist 9.2 pKi 51
pKi 9.2 (Ki 6.3x10-10 M) [51]
LUF5981 Hs Antagonist 9.1 pKi 14
pKi 9.1 (Ki 9x10-10 M) [14]
derenofylline Hs Antagonist 9.0 pKi 62
pKi 9.0 (Ki 1x10-9 M) [62]
FR194921 Hs Antagonist 8.9 pKi 86
pKi 8.9 [86]
CPFPX Hs Antagonist 8.9 pKi 51
pKi 8.9 (Ki 1.26x10-9 M) [51]
tonapofylline Rn Antagonist 8.9 pKi 67
pKi 8.9 (Ki 1.3x10-9 M) [67]
rolofylline Rn Antagonist 7.9 – 9.7 pKi 107
pKi 7.9 – 9.7 (Ki 1.26x10-8 – 1.9x10-10 M) [107]
WRC-0571 Hs Antagonist 8.8 pKi 89
pKi 8.8 [89]
rolofylline Hs Antagonist 8.1 – 9.1 pKi 67,107
pKi 8.1 – 9.1 (Ki 8x10-9 – 7.2x10-10 M) [67,107]
derenofylline Rn Antagonist 8.6 pKi 62
pKi 8.6 (Ki 2.51x10-9 M) [62]
CGS 15943 Hs Antagonist 8.5 pKi 103
pKi 8.5 (Ki 3.5x10-9 M) [103]
DPCPX Hs Antagonist 7.4 – 9.2 pKi 21,54,101,112,140
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.3x10-10 M) [21,54,101,112,140]
CGS 15943 Rn Antagonist 8.2 pKi 82
pKi 8.2 (Ki 6.4x10-9 M) [82]
tonapofylline Hs Antagonist 8.1 pKi 67
pKi 8.1 (Ki 7.4x10-9 M) [67]
MRS1754 Rn Antagonist 7.8 pKi 69
pKi 7.8 (Ki 1.68x10-8 M) [69]
8-cyclopentyltheophylline Hs Antagonist 7.5 – 8.0 pKi 18
pKi 7.5 – 8.0 [18]
FK-453 Hs Antagonist 7.7 pKi 57
pKi 7.7 (Ki 1.8x10-8 M) [57]
xanthine amine congener Hs Antagonist 7.6 pKi 58
pKi 7.6 [58]
DU172 Hs Antagonist 7.4 pKi 44
pKi 7.4 [44]
vipadenant Hs Antagonist 7.2 pKi 41
pKi 7.2 (Ki 6.8x10-8 M) [41]
ST-1535 Hs Antagonist 7.1 pKi 94
pKi 7.1 (Ki 7.18x10-8 M) [94]
MRE 2029F20 Hs Antagonist 6.7 pKi 6,135
pKi 6.7 [6,135]
istradefylline Rn Antagonist 6.6 pKi 34
pKi 6.6 (Ki 2.3x10-7 M) [34]
AS70 Hs Antagonist 6.6 pKi 135
pKi 6.6 [135]
AS100 Hs Antagonist 6.5 pKi 135
pKi 6.5 [135]
ATL802 Hs Antagonist 6.4 pKi 69
pKi 6.4 (Ki 3.69x10-7 M) [69]
MRS1754 Hs Antagonist 6.4 pKi 69
pKi 6.4 (Ki 4.03x10-7 M) [69]
PSB-11 Rn Antagonist 6.4 pKi 104
pKi 6.4 (Ki 4.4x10-7 M) [104]
ZM-241385 Hs Antagonist 6.1 – 6.6 pKi 57,103
pKi 6.1 – 6.6 [57,103]
MRS928 Rn Antagonist 6.3 pKi 66
pKi 6.3 [66]
L-97-1 Hs Antagonist 6.2 pKi 101
pKi 6.2 [101]
MRS1041 Rn Antagonist 6.2 pKi 66
pKi 6.2 [66]
SCH 58261 Hs Antagonist 6.1 – 6.3 pKi 57,103,131
pKi 6.1 – 6.3 [57,103,131]
AS99 Hs Antagonist 6.1 pKi 135
pKi 6.1 [135]
galangin Rn Antagonist 6.1 pKi 66
pKi 6.1 [66]
PSB-10 Rn Antagonist 6.1 pKi 99
pKi 6.1 (Ki 8.05x10-7 M) [99]
istradefylline Hs Antagonist 6.1 pKi 34
pKi 6.1 (Ki 8.41x10-7 M) [34]
MSX-2 Rn Antagonist 6.1 pKi 117
pKi 6.1 (Ki 9x10-7 M) [117]
MRS1042 Rn Antagonist 6.0 pKi 66
pKi 6.0 [66]
preladenant Hs Antagonist <6.0 pKi 96
pKi <6.0 (Ki >1x10-6 M) [96]
MRE 3008F20 Hs Antagonist 5.9 – 6.0 pKi 57,135-136
pKi 5.9 – 6.0 [57,135-136]
SCH442416 Hs Antagonist 5.9 pKi 57
pKi 5.9 (Ki 1.11x10-6 M) [57]
PSB-11 Hs Antagonist 5.8 pKi 104
pKi 5.8 (Ki 1.64x10-6 M) [104]
PSB-10 Hs Antagonist 5.8 pKi 104
pKi 5.8 (Ki 1.7x10-6 M) [104]
KF26777 Hs Antagonist 5.7 pKi 113
pKi 5.7 (Ki 1.8x10-6 M) [113]
CVT-6883 Hs Antagonist 5.7 pKi 28
pKi 5.7 (Ki 1.94x10-6 M) [28]
MRS1093 Rn Antagonist 5.7 pKi 66
pKi 5.7 [66]
PSB1115 Rn Antagonist 5.7 pKi 98
pKi 5.7 (Ki 2.2x10-6 M) [98]
MRS1132 Rn Antagonist 5.6 pKi 66
pKi 5.6 [66]
MSX-2 Hs Antagonist 5.6 pKi 117
pKi 5.6 (Ki 2.5x10-6 M) [117]
LAS38096 Hs Antagonist 5.6 pKi 27,137
pKi 5.6 (Ki 2.821x10-6 M) [27,137]
flavone Rn Antagonist 5.5 pKi 66
pKi 5.5 [66]
isobutylmethylxanthine Hs Antagonist 5.1 pKi 58
pKi 5.1 [58]
sakuranetin Rn Antagonist 5.1 pKi 66
pKi 5.1 [66]
theophylline Hs Antagonist 4.9 – 5.2 pKi 30,58,71,135
pKi 4.9 – 5.2 [30,58,71,135]
ATL802 Mm Antagonist 5.0 pKi 69
pKi 5.0 (Ki 9.583x10-6 M) [69]
MRS1191 Hs Antagonist <5.0 pKi 79
pKi <5.0 (Ki >1x10-5 M) [79]
MRS1523 Hs Antagonist <5.0 pKi 79
pKi <5.0 (Ki >1x10-5 M) [79]
VUF5574 Rn Antagonist >5.0 pKi 134
pKi >5.0 (Ki <1x10-5 M) [134]
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 47
pKi <5.0 (Ki >1x10-5 M) [47]
theophylline Rn Antagonist 4.8 – 5.1 pKi 55,98
pKi 4.8 – 5.1 (Ki 1.4x10-5 – 8.74x10-6 M) [55,98]
morin Rn Antagonist 4.9 pKi 66
pKi 4.9 [66]
MRS1523 Rn Antagonist 4.8 pKi 79
pKi 4.8 (Ki 1.56x10-5 M) [79]
caffeine Hs Antagonist 4.3 – 5.0 pKi 1,23,55
pKi 4.3 – 5.0 (Ki 4.49x10-5 – 1.07x10-5 M) [1,23,55]
MRS923 Rn Antagonist 4.6 pKi 66
pKi 4.6 [66]
CSC Rn Antagonist 4.6 pKi 56
pKi 4.6 (Ki 2.8x10-5 M) [56]
MRS1065 Rn Antagonist 4.5 pKi 66
pKi 4.5 [66]
MRS1086 Rn Antagonist 4.5 pKi 66
pKi 4.5 [66]
flavanone Rn Antagonist 4.5 pKi 66
pKi 4.5 [66]
MRS1066 Rn Antagonist 4.4 pKi 66
pKi 4.4 [66]
MRS1084 Rn Antagonist 4.4 pKi 66
pKi 4.4 [66]
MRS1191 Rn Antagonist 4.4 pKi 79
pKi 4.4 (Ki 4.01x10-5 M) [79]
caffeine Rn Antagonist 4.4 – 4.4 pKi 19,46
pKi 4.4 – 4.4 (Ki 4.4x10-5 – 4.1x10-5 M) [19,46]
MRS1062 Rn Antagonist 4.3 pKi 66
pKi 4.3 [66]
View species-specific antagonist tables
Antagonist Comments
Reference [23] does not use a transfected cell system but measures binding to the human hippocampus.

Istradefylline pKi values are derived from unpublished data (Müller et al.).
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
VPC171 Hs Positive - - 5,53
[5,53]
PD81723 Hs Positive - - 12
[12]
Allosteric Modulator Comments
In vitro, VPC171 enhances A1R agonist ((R)-PIA)-induced ERK1/2 phosphorylation with a 2.4-fold positive cooperativity, and enhances [35S]GTPγS binding with a 6.9-fold positive cooperativity under the same conditions [53].
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  16,58
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family
Gq/G11 family
Adenylate cyclase stimulation
Phospholipase C stimulation
References:  16
Tissue Distribution
Brain > heart, kidney, lung.
Species:  Human
Technique:  Northern blotting.
References:  115
Spermatozoa.
Species:  Human
Technique:  immunocytochemistry.
References:  92
Adopicytes.
Species:  Human
Technique:  Northern blotting.
References:  13
Jejunum, ileum, colon.
Species:  Human
Technique:  RT-PCR.
References:  15
Brain (cerebral cortex, hippocampus), spinal cord and trigeminal ganglia.
Species:  Human
Technique:  Immunohistochemistry.
References:  119
Kidney: medullary tubular structures.
Species:  Mouse
Technique:  RNAse protection and RT-PCR.
References:  138
Jejunum.
Species:  Mouse
Technique:  RT-PCR.
References:  39
Brain: cerebral cortex.
Species:  Mouse
Technique:  Autoradiography.
References:  81
Brain: cortex, cerebellum, hippocampus > olfactory bulb, mesencephalon, striatum.
Species:  Rat
Technique:  Northern blotting.
References:  87
Kidney: medullary tubular structures.
Species:  Rat
Technique:  RNAse protection and RT-PCR.
References:  138
CNS: spinal cord lumbar dorsal horn.
Species:  Rat
Technique:  Immunohistochemistry.
References:  124
Testes: Sertoli cells >> spermatogonia, spermatocytes.
Species:  Rat
Technique:  in situ hybridisation.
References:  111
Spermatozoa.
Species:  Rat
Technique:  immunocytochemistry.
References:  92
Spleen, stomach, heart, testis.
Species:  Rat
Technique:  Northern blotting.
References:  87
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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