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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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ADORA1
adenosine A1 receptor
Chromosome 1 · 1q32.1
NCBI Gene: 134Ensembl: ENSG00000163485.19HGNC: HGNC:262UniProt: B7Z1L9
146PubMed Papers
20Diseases
22Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
response to purine-containing compoundplasma membraneprotein bindingG protein-coupled receptor signaling pathwayasthmamigraine disorderparoxysmal tachycardiaApnea
✦AI Summary

ADORA1 encodes the adenosine A1 receptor, a G protein-coupled receptor that mediates adenosine signaling through inhibition of adenylyl cyclase via GNAI2 1. This receptor functions across multiple physiological systems with distinct roles in health and disease. In the nervous system, ADORA1 plays critical roles in sleep homeostasis, where neuronal A1 receptors facilitate slow-wave activity during sleep through adenosine accumulation in a neuronal-glial circuit 2. However, ADORA1 upregulation is pathologically implicated in Alzheimer's disease, where tau pathology increases neuronal A1R expression via miR-133a-3p regulation, promoting astrocyte activation and neurodegeneration 3. A loss-of-function ADORA1 mutation (p.Gly279Ser) causes early-onset parkinsonism and cognitive dysfunction, likely through disrupted interaction with dopamine D1 receptors 4. In cancer immunology, ADORA1 deletion suppresses melanoma cell growth but paradoxically promotes immune evasion by upregulating PD-L1 via ATF3, which can be overcome with PD-1 checkpoint inhibition 5. ADORA1 also mediates stress-induced anxiety through purine metabolic dysfunction in CD4+ T cells, where CD4-derived xanthine activates oligodendrocytes via A1 receptors 6. Additionally, ADORA1 expression is significantly elevated in epicardial adipose tissue and associates with cardiac physiology and coronary artery disease pathophysiology 7.

Sources cited
1
ADORA1 is a receptor for adenosine that inhibits adenylyl cyclase through G proteins like GNAI2
PMID: 29925945
2
ADORA1 facilitates slow-wave activity during sleep through neuronal-glial adenosine homeostasis
PMID: 28633050
3
Tau pathology upregulates neuronal ADORA1 expression via miR-133a-3p, promoting astrocyte activation and neurodegeneration in Alzheimer's disease
PMID: 37083538
4
ADORA1 mutation p.Gly279Ser causes early-onset parkinsonism and cognitive dysfunction through disrupted dopamine D1 receptor interaction
PMID: 27134041
5
ADORA1 deletion suppresses melanoma growth but promotes PD-L1-mediated immune evasion through ATF3 upregulation
PMID: 32183950
6
CD4+ T cell-derived xanthine acts on oligodendrocytes via ADORA1 to mediate stress-induced anxiety-like behavior
PMID: 31675497
7
ADORA1 expression is significantly elevated in epicardial adipose tissue compared to subcutaneous fat and may contribute to cardiac pathophysiology
PMID: 28081581
Disease Associationsⓘ20
asthmaOpen Targets
0.72Strong
migraine disorderOpen Targets
0.61Moderate
paroxysmal tachycardiaOpen Targets
0.59Moderate
ApneaOpen Targets
0.57Moderate
PainOpen Targets
0.57Moderate
chronic obstructive pulmonary diseaseOpen Targets
0.57Moderate
Wolff-Parkinson-White SyndromeOpen Targets
0.56Moderate
Airway obstructionOpen Targets
0.55Moderate
hepatic veno-occlusive diseaseOpen Targets
0.54Moderate
HeadacheOpen Targets
0.53Moderate
chronic bronchitisOpen Targets
0.46Moderate
atrial fibrillationOpen Targets
0.43Moderate
childhood onset asthmaOpen Targets
0.39Weak
attention deficit hyperactivity disorderOpen Targets
0.38Weak
cardiovascular diseaseOpen Targets
0.37Weak
Paroxysmal supraventricular tachycardiaOpen Targets
0.37Weak
drug dependenceOpen Targets
0.37Weak
CoughOpen Targets
0.37Weak
orthostatic hypotensionOpen Targets
0.37Weak
Recurrent thrombophlebitisOpen Targets
0.37Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets22
ADENOSINEApproved
Adenosine receptor agonist
Wolff-Parkinson-White Syndrome
AMINOPHYLLINEApproved
Adenosine receptor antagonist
asthma
AMP579Phase II
Adenosine A1 receptor agonist
familial hyperlipidemia
BAY1067197Phase II
Adenosine A1 receptor agonist
heart failure
CAFFEINEApproved
Adenosine receptor antagonist
migraine disorder
CAFFEINE CITRATEApproved
Adenosine receptor antagonist
Apnea
CAPADENOSONPhase II
Adenosine A1 receptor partial agonist
atrial fibrillation
DEFIBROTIDEApproved
Adenosine A2 receptor agonist
Recurrent thrombophlebitis
DERENOFYLLINEPhase II
Adenosine A1 receptor antagonist
heart failure
FK453Phase II
Adenosine A1 receptor antagonist
Renal insufficiency
GS-9667Phase I
Adenosine A1 receptor partial agonist
Hypertriglyceridemia
GW493838Phase II
Adenosine A1 receptor agonist
neuropathic pain
NAXIFYLLINEPhase III
Adenosine A1 receptor antagonist
OXTRIPHYLLINEApproved
Adenosine receptor antagonist
Cough
PBF-680Phase II
Adenosine A1 receptor antagonist
asthma
ROLOFYLLINEPhase III
Adenosine A1 receptor antagonist
heart failure
SELODENOSONPhase II
Adenosine A1 receptor agonist
Arrhythmia
T-62Phase II
Adenosine A1 receptor modulator
postherpetic neuralgia
TECADENOSONPhase III
Adenosine A1 receptor agonist
atrial fibrillation
THEOPHYLLINEApproved
Phosphodiesterase 4 inhibitor
asthma
TONAPOFYLLINEPhase II
Adenosine A1 receptor antagonist
TRABODENOSONPhase III
Adenosine A1 receptor agonist
ocular hypertension
Related Genes
GHRLProtein interaction93%GNAI2Protein interaction92%GNAI1Protein interaction92%GNAI3Protein interaction91%SLC29A1Protein interaction88%NPYProtein interaction85%
Tissue Expression6 tissues
Brain
100%
Heart
80%
Lung
4%
Liver
3%
Ovary
1%
Bone Marrow
0%
Gene Interaction Network
Click a node to explore
ADORA1GHRLGNAI2GNAI1GNAI3SLC29A1NPY
PROTEIN STRUCTURE
Preparing viewer…
PDB5UEN · 3.20 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.60Moderately Constrained
pLIⓘ
0.86Intermediate
Observed/Expected LoF0.30 [0.17–0.60]
RankingsWhere ADORA1 stands among ~20K protein-coding genes
  • #3,100of 20,598
    Most Researched146 · top quartile
  • #223of 1,025
    FDA-Approved Drug Targets7 · top quartile
  • #4,084of 17,882
    Most Constrained (LOEUF)0.60 · top quartile
Genes detectedADORA1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
ADORA1 Inhibition Promotes Tumor Immune Evasion by Regulating the ATF3-PD-L1 Axis.
PMID: 32183950
Cancer Cell · 2020
1.00
2
Stress-Induced Metabolic Disorder in Peripheral CD4
PMID: 31675497
Cell · 2019
0.90
3
Tau pathology epigenetically remodels the neuron-glial cross-talk in Alzheimer's disease.
PMID: 37083538
Sci Adv · 2023
0.80
4
The resurgence of the Adora2b receptor as an immunotherapeutic target in pancreatic cancer.
PMID: 37187740
Front Immunol · 2023
0.70
5
Differential Expression of Adenosine P1 Receptor ADORA1 and ADORA2A Associated with Glioma Development and Tumor-Associated Epilepsy.
PMID: 27038930
Neurochem Res · 2016
0.60