ADORA1
ENSG00000163485
Target class
GPCR
Chromosome
1
Approved drugs
7
Clinical candidates (approved and in development)
24
- Approved drugs
- 7
- Clinical candidates (approved and in development)
- 24
- Chemical probe available
- Yes
- Other names
- RDC7
- Target name
- ADORA1
- Gene name
- Adenosine A1 receptor
- Gene symbol
- ADORA1
- Protein name
- Adenosine receptor A1
- Gene biotype
- Protein coding
- Gene family
- Adenosine receptors
- Target class
- GPCR
- Target type
- Human gene
- Tissues expressed in
- 32
- Protein localisation evidence grade
- Supported
- Highest tissue expression
- 43.18
- Tissue specificity (Gini)
- 0.671
- Tissue specificity (tau)
- 0.798
- KEGG gene identifiers
- hsa:134
- Protein interaction confidence
- 0.819833
- Protein interaction partners
- 18
- R-HSA-417973
- R-HSA-418594
- End position
- 203167407
- Start position
- 203090654
- Chromosome
- 1
- Strand
- Forward
- Cell membrane
- Multi-pass membrane protein.
- Plasma membrane
Publication evidence
- PubMed 27134041
- Tissue specificity (tau)
- 0.79843
- Expression inequality (Gini)
- 0.671196
Expression in transcripts per million
- Brain - Spinal cord (cervical c-1)
- 43.18
- Brain - Frontal Cortex (BA9)
- 39.61
- Brain - Cortex
- 36.67
- Testis
- 35.52
- Brain - Substantia nigra
- 31
Expression in transcripts per million
- Brain - Spinal cord (cervical c-1)43.18
- Brain - Frontal Cortex (BA9)39.61
- Brain - Cortex36.67
- Testis35.52
- Brain - Substantia nigra31
- Brain - Putamen (basal ganglia)30.76
- Brain - Caudate (basal ganglia)29.27
- Brain - Amygdala27.56
- Brain - Nucleus accumbens (basal ganglia)27.1
- Brain - Hippocampus27.05
- Brain - Cerebellum26.78
- Brain - Anterior cingulate cortex (BA24)26.62
- Brain - Cerebellar Hemisphere26.56
- Brain - Hypothalamus20.82
- Heart - Atrial Appendage7.72
- Spleen6.47
- Pancreas6.43
- Kidney - Cortex5.71
- Skin - Sun Exposed (Lower leg)4.73
- Breast - Mammary Tissue3.76
- Minor Salivary Gland3.56
- Heart - Left Ventricle3.55
- Thyroid3.21
- Adipose - Visceral (Omentum)3.16
- Skin - Not Sun Exposed (Suprapubic)2.84
And 29 more, listed on the interactive page.
- GO:0006909
- GO:0006954
- GO:0007165
- GO:0007267
- GO:0007399
- GO:0014074
- GO:0097190
Cellular components
- GO:0005886
Molecular functions
- GO:0005515
bronchoconstriction
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: bronchoconstriction
- cardiovascular system
- nervous system
- renal
Evidence sourceinduction of sleep
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: induction of sleep
- cardiovascular system
- nervous system
- renal
Evidence sourcenatriuresis
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: natriuresis
- cardiovascular system
- nervous system
- renal
Evidence sourcedeath
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: death
- nervous system
- renal
- cardiovascular
PubMed 28216264heart failure
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: heart failure
- nervous system
- renal
- cardiovascular
PubMed 28216264diuresis
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: diuresis
- cardiovascular system
- nervous system
- renal
Evidence sourceatrioventricular block
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: atrioventricular block
- nervous system
- renal
- cardiovascular
PubMed 28216264convulsions
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: convulsions
- nervous system
- renal
- cardiovascular
PubMed 28216264increased urinary sodium excretion
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased urinary sodium excretion
- nervous system
- renal
- cardiovascular
PubMed 28216264bradycardia
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: bradycardia
- cardiovascular system
- nervous system
- renal
Evidence sourcedecreased pain
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased pain
- nervous system
- renal
- cardiovascular
PubMed 28216264cardioprotection
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: cardioprotection
- cardiovascular system
- nervous system
- renal
Evidence sourcedecreased blood pressure
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased blood pressure
- nervous system
- renal
- cardiovascular
PubMed 28216264decreased heart rate
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased heart rate
- nervous system
- renal
- cardiovascular
PubMed 28216264cardiac arrhythmia
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: cardiac arrhythmia
- nervous system
- renal
- cardiovascular
PubMed 28216264vasoconstriction
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: vasoconstriction
- cardiovascular system
- nervous system
- renal
Evidence sourceincreased urine excretion
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased urine excretion
- nervous system
- renal
- cardiovascular
PubMed 28216264vasodilation
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: vasodilation
- cardiovascular system
- nervous system
- renal
Evidence source
receptor binding
Studies
- biochemical: NVS_GPCR_hAdoRA1, is one of one assay component(s) measured or calculated from the NVS_GPCR_hAdoRA1 assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Filter-based radiodetection technology.
Biological samples
- brain, tissue-based cell-free
Evidence source
Related records
Trials (419)
- "First-in-human" Study To Assess the Safety and Tolerability of PBF-680 in Male Healthy Volunteers
- "Pecos" B-adrenergic and PPAR-G Stimulation Upregulates Lipid Metabolism in Human Subcutaneous Fat
- A 1-year Multi-center, Prospective, Cohort Study in Patients With Chronic Obstructive Pulmonary Disease Treated With Long-acting Bronchodilator
- A Clinical Study to Test if an Investigational Treatment Called BNT314 When Used in Combination With Another Investigational Treatment Pumitamig (BNT327) and Chemotherapy, is Beneficial and Safe for Patients With Advanced Colorectal Cancer
- A Comparison of the Bioavailability of OZ439 When Delivered Directly to the Small Intestine, or Via the Oral Route
- A DDI Study to Assess the Effect of INC280 on the PK of Midazolam and Caffeine in Patients With cMET-dysregulated Advanced Solid Tumors
- A Dental Pain Study Comparing The Analgesic Efficacy Of Ibuprofen/Caffeine
- A Dose-Escalation Study Designed to Evaluate the Tolerability, Safety, Pharmacokinetics (PK), and Efficacy of Chronic Topical Ocular Application of INO-8875 in Adults With Ocular Hypertension or Primary Open-Angle Glaucoma
- A Drug Interaction Study of KW-6356 With Midazolam, Caffeine, or Rosuvastatin
- A Drug-Drug Interaction (DDI) Study of LY3437943 in Obese Participants
- A Drug-Drug Interaction Study of Abiraterone Acetate Plus Prednisone With Dextromethorphan and Theophylline in Patients With Metastatic Castration-Resistant Prostate Cancer
- A Phase I Dose Escalation Study of Erlotinib in Combination With Theophylline
- A Phase I Study of GFH312 in Healthy Chinese Subjects
- A Phase II Study to Evaluate the Additivity of Trabodenoson to Latanoprost in Adults With Ocular Hypertension or Primary Open-Angle Glaucoma
- A Pilot Study Into Health Pre and Post Treatment With Intravenous Aminophylline and Hydrocortisone in Severe Asthmatics
- A Pilot Study to Determine the Feasibility and Utility of Implementing of the Full Scale TOM Trial
- A Placebo-controlled Study to Investigate the Safety, and Pharmacokinetics of Oral GSK626616AC in Healthy Subjects
- A Possible Therapeutic Role for Adenosine During Inflammation
- A Randomized, Double-blind, Active Control, Parallel Group, Titration, Multicenter Study to Evaluate the Efficacy and Safety of Fimasartan
- A Research Study on How UBT251 Affects Levels of Midazolam, Caffeine and Warfarin in the Blood of Participants With Excess Body Weight
Drugs (26)
- Adenosine Adenosine receptor agonist
- Aminophylline Adenosine receptor antagonist
- AMP579 Adenosine A1 receptor agonist
- BAY1067197 Adenosine A1 receptor agonist
- Caffeine Adenosine receptor antagonist
- Caffeine citrate Adenosine receptor antagonist
- Capadenoson Adenosine A1 receptor partial agonist
- Defibrotide Adenosine A1 receptor agonist
- Derenofylline Adenosine A1 receptor antagonist
- FK453 Adenosine A1 receptor antagonist
- GS-9667 Adenosine A1 receptor partial agonist
- GW493838 Adenosine A1 receptor agonist
- Naxifylline Adenosine A1 receptor antagonist
- Oxtriphylline Adenosine receptor antagonist
- PBF-680 Adenosine A1 receptor antagonist
- Rolofylline Adenosine A1 receptor antagonist
- RPR749 Adenosine A1 receptor agonist
- Selodenoson Adenosine A1 receptor agonist
- T-62 Adenosine A1 receptor modulator
- Tecadenoson Adenosine A1 receptor agonist