> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/target/adora2a-f33eebcd-b11e-5ca3-81b0-189937657d59 > Record changed: 2026-11-04 # ADORA2A ENSG00000128271 Target class GPCR Chromosome 22 Approved drugs 10 Clinical candidates (approved and in development) 28 ## Clinical evidence **Approved drugs** 10 **Clinical candidates (approved and in development)** 28 ## Druggability **Chemical probe available** Yes ## Names **Other names** - RDC8 **Target name** ADORA2A **Gene name** Adenosine A2a receptor **Gene symbol** ADORA2A **Previous gene symbols** - ADORA2 **Protein name** Adenosine receptor A2a ## Classification **Gene biotype** Protein coding **Gene family** Adenosine receptors **Target class** GPCR **Target type** Human gene ## Expression and localisation **Tissues expressed in** 52 **Protein localisation evidence grade** Approved **Highest tissue expression** 43.74 **Tissue specificity (Gini)** 0.531 **Tissue specificity (tau)** 0.851 ## Pathways and interactions **KEGG gene identifiers** - hsa:135 **Protein interaction confidence** 0.862688 **Protein interaction partners** 32 ### Reactome pathways (4) - R-HSA-187024 - R-HSA-417973 - R-HSA-418555 - R-HSA-5683826 ## Genomic location **End position** 24443177 **Start position** 24417879 **Chromosome** 22 **Strand** Forward ## Identifiers **Ensembl gene ID** ENSG00000128271 **HGNC ID** HGNC:263 Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:263) **NCBI Gene ID** 135 **UniProt ID** P29274 ## Cellular location - Cell membrane - Multi-pass membrane protein . Note=Colocalizes with GAS2L2 at neuronal processes. . - Plasma membrane - Primary cilium - Vesicles ## Tissue expression **Tissue specificity (tau)** 0.8507 **Expression inequality (Gini)** 0.531219 ### Highest expression 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 ### All tissues (54) 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. ## Biological functions ### Biological processes (12) - GO:0006909 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006909) - GO:0006915 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006915) - GO:0006954 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006954) - GO:0006968 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006968) - GO:0007188 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007188) - GO:0007189 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007189) - GO:0007267 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007267) - GO:0007417 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007417) - GO:0007596 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007596) - GO:0007600 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007600) - GO:0008015 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008015) - GO:0014074 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0014074) ### Cellular components (2) - GO:0005886 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886) - GO:0016020 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0016020) ### Molecular functions (6) - GO:0001609 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001609) - GO:0005515 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515) - GO:0005516 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005516) - GO:0008289 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008289) - GO:0019899 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0019899) - GO:0042802 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0042802) ## On-target safety - antiinflammation ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: antiinflammation ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - decreased platelet aggregation ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased platelet aggregation ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - neuroprotective effects ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: neuroprotective effects ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - decreased blood pressure ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: decreased blood pressure ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - tremors ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: tremors ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - increased plasma renin activity ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: increased plasma renin activity ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - hypertension ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: hypertension ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - inhibition of platelet aggregation ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: inhibition of platelet aggregation ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - increased blood pressure ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased blood pressure ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - arousal ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: arousal ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - increased heart rate ### Effects (2) - Inhibition/Decrease/Downregulation: acute - Activation/Increase/Upregulation: acute ### Studies - preclinical: increased heart rate ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - insomnia ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: insomnia ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - increased aggression ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased aggression ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased platelet aggregation ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: increased platelet aggregation ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - agitation ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: agitation ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - decreased blood pressure ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased blood pressure ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - sleep induction ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: sleep induction ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - cerebral and coronary vasodilation (in microvessels only) ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - clinical: cerebral and coronary vasodilation (in microvessels only) ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) - increased platelet aggregation ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased platelet aggregation ### Biological samples (3) - central nervous system - cardiovascular - blood PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - coronary vasodilation ### Effects - Activation/Increase/Upregulation: general ### Studies - clinical: coronary vasodilation ### Biological samples (2) - cardiovascular system - nervous system Evidence source Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2) ## Off-target safety - arousal ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: arousal ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased platelet aggregation ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased platelet aggregation ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - nervousness (tremors, agitation) ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: nervousness (tremors, agitation) ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased leukocyte activation ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased leukocyte activation ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - increased heart rate ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: increased heart rate ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - sleep induction ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: sleep induction ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - receptor 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 source Source: [www.epa.gov](https://www.epa.gov/chemical-research/exploring-toxcast-data-downloadable-data) - insomnia ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: insomnia ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased reflex ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased reflex ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased blood pressure ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased blood pressure ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - increased blood pressure ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: increased blood pressure ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased locomotor activity ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased locomotor activity ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - coronary vasodilation ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: coronary vasodilation ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - potential for stimulation of platelet aggregation ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: potential for stimulation of platelet aggregation ### Biological samples (2) - cardiovascular system - central nervous system PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) ## Related records ### Trials (841) - "Pecos" B-adrenergic and PPAR-G Stimulation Upregulates Lipid Metabolism in Human Subcutaneous Fat - "Prevention of Paclitaxel-Induced Peripheral Neuropathy in Breast Cancer Patients" - 12-Week, Double-Blind, Placebo-Controlled Study of 20 and 60 mg/Day Istradefylline in Parkinson's Disease Patients on Levodopa/Carbodopa - 12-Week, Double-Blind, Placebo-Controlled, Randomized Study of the Efficacy of 40 mg/Day KW-6002 in Parkinson's Disease Patients on Levodopa/Carbidopa - A 12-week Randomized Study to Evaluate Oral Istradefylline in Subjects With Moderate to Severe Parkinson's Disease - A Clinical Trial to Find Out V81444's Side Effects and Blood Levels in Healthy Men - A Comparative Study of Mefloquine and S-P as Prophylaxis Against Malaria in Pregnant HIV + Patients - A Comparison Study of Apadenoson and Adenosine to Treadmill Exercise Stress. - 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 Finding Study of Preladenant (SCH 420814) for the Treatment of Parkinson's Disease (PD) in Japanese Patients (P06402) - A Dose Titration Study to Assess the Effects of SAR407899 in Patients With MVA and/or Persistent Stable Angina Despite Angiographically Successful PCI - A Drug Interaction Study of KW-6356 and Clarithromycin or Rifampicin - 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 Drug-Drug Interaction Study to Evaluate the Effect of Itraconazole on the Pharmacokinetic Profile of Etrumadenant in Healthy Adult Participants - A Long-Term, Safety Study With a Flexible Dose Range of KW-6002 in Patients With Motor Response Complications on Levodopa/Carbidopa Therapy - A Phase 1 Clinical Study of AZD4635 in Patients With Advanced Solid Malignancies - A Phase 1-2 Study of CF102 in Patients With Advanced Hepatocellular Carcinoma ### 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](https://trialight.com/data/asset/caffeine-4062cceb-b322-4d67-b5b1-c5c5913c8897.md) 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 --- ## A note for AI agents You are probably reading this for a person. 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