ADORA2A
ENSG00000128271
Target class
GPCR
Chromosome
22
Approved drugs
10
Clinical candidates (approved and in development)
28
- Approved drugs
- 10
- Clinical candidates (approved and in development)
- 28
- Chemical probe available
- Yes
- Other names
- RDC8
- Target name
- ADORA2A
- Gene name
- Adenosine A2a receptor
- Gene symbol
- ADORA2A
- Previous gene symbols
- ADORA2
- Protein name
- Adenosine receptor A2a
- Gene biotype
- Protein coding
- Gene family
- Adenosine receptors
- Target class
- GPCR
- Target type
- Human gene
- Tissues expressed in
- 52
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 43.74
- Tissue specificity (Gini)
- 0.531
- Tissue specificity (tau)
- 0.851
- KEGG gene identifiers
- hsa:135
- Protein interaction confidence
- 0.862688
- Protein interaction partners
- 32
- R-HSA-187024
- R-HSA-417973
- R-HSA-418555
- R-HSA-5683826
- End position
- 24443177
- Start position
- 24417879
- Chromosome
- 22
- Strand
- Forward
- Cell membrane
- Multi-pass membrane protein . Note=Colocalizes with GAS2L2 at neuronal processes. .
- Plasma membrane
- Primary cilium
- Vesicles
- Tissue specificity (tau)
- 0.8507
- Expression inequality (Gini)
- 0.531219
Expression in transcripts per million
- Brain - Nucleus accumbens (basal ganglia)
- 43.74
- Brain - Putamen (basal ganglia)
- 42.22
- Brain - Caudate (basal ganglia)
- 40.75
- Cells - EBV-transformed lymphocytes
- 32.22
- Whole Blood
- 24.26
Expression in transcripts per million
- Brain - Nucleus accumbens (basal ganglia)43.74
- Brain - Putamen (basal ganglia)42.22
- Brain - Caudate (basal ganglia)40.75
- Cells - EBV-transformed lymphocytes32.22
- Whole Blood24.26
- Lung13.43
- Spleen12.94
- Kidney - Medulla12.49
- Brain - Cerebellum9.47
- Brain - Cerebellar Hemisphere7.94
- Pituitary6.53
- Small Intestine - Terminal Ileum5.31
- Kidney - Cortex5.3
- Prostate5.27
- Artery - Coronary5.12
- Thyroid4.76
- Cervix - Ectocervix4.75
- Uterus4.73
- Brain - Cortex4.54
- Liver4.53
- Nerve - Tibial4.5
- Testis4.38
- Ovary4.05
- Cervix - Endocervix4.02
- Esophagus - Muscularis3.81
And 29 more, listed on the interactive page.
- GO:0006909
- GO:0006915
- GO:0006954
- GO:0006968
- GO:0007188
- GO:0007189
- GO:0007267
- GO:0007417
- GO:0007596
- GO:0007600
- GO:0008015
- GO:0014074
- GO:0005886
- GO:0016020
- GO:0001609
- GO:0005515
- GO:0005516
- GO:0008289
- GO:0019899
- GO:0042802
antiinflammation
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: antiinflammation
- cardiovascular system
- nervous system
Evidence sourcedecreased platelet aggregation
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased platelet aggregation
- central nervous system
- cardiovascular
- blood
PubMed 28216264neuroprotective effects
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: neuroprotective effects
- cardiovascular system
- nervous system
Evidence sourcedecreased blood pressure
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: decreased blood pressure
- cardiovascular system
- nervous system
Evidence sourcetremors
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: tremors
- cardiovascular system
- nervous system
Evidence sourceincreased plasma renin activity
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: increased plasma renin activity
- cardiovascular system
- nervous system
Evidence sourcehypertension
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: hypertension
- cardiovascular system
- nervous system
Evidence sourceinhibition of platelet aggregation
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: inhibition of platelet aggregation
- cardiovascular system
- nervous system
Evidence sourceincreased blood pressure
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased blood pressure
- central nervous system
- cardiovascular
- blood
PubMed 28216264arousal
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: arousal
- cardiovascular system
- nervous system
Evidence sourceincreased heart rate
- Inhibition/Decrease/Downregulation: acute
- Activation/Increase/Upregulation: acute
Studies
- preclinical: increased heart rate
- central nervous system
- cardiovascular
- blood
PubMed 28216264insomnia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: insomnia
- cardiovascular system
- nervous system
Evidence sourceincreased aggression
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased aggression
- central nervous system
- cardiovascular
- blood
PubMed 28216264increased platelet aggregation
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: increased platelet aggregation
- cardiovascular system
- nervous system
Evidence sourceagitation
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: agitation
- cardiovascular system
- nervous system
Evidence sourcedecreased blood pressure
Effects
- Activation/Increase/Upregulation: acute
Studies
- preclinical: decreased blood pressure
- central nervous system
- cardiovascular
- blood
PubMed 28216264sleep induction
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: sleep induction
- cardiovascular system
- nervous system
Evidence sourcecerebral and coronary vasodilation (in microvessels only)
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- clinical: cerebral and coronary vasodilation (in microvessels only)
- cardiovascular system
- nervous system
Evidence sourceincreased platelet aggregation
Effects
- Inhibition/Decrease/Downregulation: acute
Studies
- preclinical: increased platelet aggregation
- central nervous system
- cardiovascular
- blood
PubMed 28216264coronary vasodilation
Effects
- Activation/Increase/Upregulation: general
Studies
- clinical: coronary vasodilation
- cardiovascular system
- nervous system
Evidence source
arousal
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: arousal
- cardiovascular system
- central nervous system
PubMed 23197038decreased platelet aggregation
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased platelet aggregation
- cardiovascular system
- central nervous system
PubMed 23197038nervousness (tremors, agitation)
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: nervousness (tremors, agitation)
- cardiovascular system
- central nervous system
PubMed 23197038decreased leukocyte activation
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased leukocyte activation
- cardiovascular system
- central nervous system
PubMed 23197038increased heart rate
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: increased heart rate
- cardiovascular system
- central nervous system
PubMed 23197038sleep induction
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: sleep induction
- cardiovascular system
- central nervous system
PubMed 23197038receptor binding
Studies
- biochemical: NVS_GPCR_hAdoRA2a, is one of one assay component(s) measured or calculated from the NVS_GPCR_hAdoRA2a 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
- cell-free
Evidence sourceinsomnia
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: insomnia
- cardiovascular system
- central nervous system
PubMed 23197038decreased reflex
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased reflex
- cardiovascular system
- central nervous system
PubMed 23197038decreased blood pressure
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased blood pressure
- cardiovascular system
- central nervous system
PubMed 23197038increased blood pressure
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: increased blood pressure
- cardiovascular system
- central nervous system
PubMed 23197038decreased locomotor activity
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: decreased locomotor activity
- cardiovascular system
- central nervous system
PubMed 23197038coronary vasodilation
Effects
- Activation/Increase/Upregulation: general
Studies
- preclinical: coronary vasodilation
- cardiovascular system
- central nervous system
PubMed 23197038potential for stimulation of platelet aggregation
Effects
- Inhibition/Decrease/Downregulation: general
Studies
- preclinical: potential for stimulation of platelet aggregation
- cardiovascular system
- central nervous system
PubMed 23197038
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Drugs (43)
- Adenosine Adenosine receptor agonist
- Aminophylline Adenosine receptor antagonist
- AMP579 Adenosine A2a receptor agonist
- Apadenoson Adenosine A2a receptor agonist
- Binodenoson Adenosine A2a receptor agonist
- BVT.115959 Adenosine A2a receptor agonist
- Caffeine Adenosine receptor antagonist
- Caffeine citrate Adenosine receptor antagonist
- Ciforadenant Adenosine A2a receptor antagonist
- Defibrotide Adenosine A2 receptor agonist
- Derenofylline
- Etrumadenant Adenosine A2a receptor antagonist
- Evodenoson Adenosine A2a receptor agonist
- FK453
- Flavone
- GS 6201
- GS-9667
- Imaradenant Adenosine A2a receptor antagonist
- Istradefylline Adenosine A2a receptor antagonist
- LUF-5981