Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00187

Target Information
NameAdenosine A2a receptor    
Type of targetSuccessful target    
SynonymsA(2A) adenosine receptor    
A2a Adenosine receptor    
Adenosine receptor A2a    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Brain injury[1]
Depression
[ICD9: 311   ICD10: F32]
[2]
Dyskinesia
[ICD9: 333.8   ICD10: G24.9]
[3]
Inflammation[4]
Ischemia reperfusion injuries
[ICD9: 459.89   ICD10: I99.8]
[5]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[6]
Neuropsychiatric disorders[7]
Oxygen-induced retinopathy
[ICD9: 362.0-362.2   ICD10: H35-H35.2]
[8]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[1]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[3][9][7]
Renal diseases
[ICD9: 580-599   ICD10: N00-N39]
[10]
Drug(s)CaffeineApprovedFatigue and orthostatic hypotension[11][12]
RegadenosonApprovedPharmacological stress agent for radionuclide imaging
KW-3902Phase III completedAcute and chronic heart failure[13]
KW-6002Phase IIIParkinson's Disease[9][6][2][14]
MRE-0094Phase II completedDiabetic foot ulcers[15]
SCH 420814Phase II completedParkinsoní»s disease[16]
ATL-146ePhase IIGastric diseases[5]
BG-9928Phase IIAcute and chronic heart failure[13]
BIIB014Phase IIParkinsoní»s disease[16]
DexefaroxanDiscontinued in Phase IISchizophrenia[17]
GW-493838Discontinued in Phase IINeuropathic pain[18]
T-62Terminated in Phase INeuropathic pain[18]
Adenosine A(2A) receptor antagonistPreclinicalParkinsoní»s Disease[19]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP29274
PDB Structure1MMH; 1UPE; 2YDO; 2YDV; 3EML; 3PWH; 3QAK; 3REY; 3RFM; 3UZA; 3UZC; 3VG9; 3VGA; 4EIY.    
FunctionReceptor for adenosine, and the activity of this receptor is mediated by G proteins which activate adenylyl cyclase.    
SequenceMPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAI PFAITISTGFCAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTR AKGIIAICWVLSFAIGLTPMLGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYF NFFACVLVPLLLMLGVYLRIFLAARRQLKQMESQPLPGERARSTLQKEVHAAKSLAIIVG LFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTNSVVNPFIYAYRIREFRQTFR KIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGSAPHPERRPNG YALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS
Related US Patent6,440,948
6,448,235
6,555,545
6,579,868
6,583,156
6,586,413
6,608,085
6,630,475
6,642,210
6,653,315
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (S)-DHPA[20]
1-METHYLXANTHINE[21]
2,6-diphenyl-9H-purine[22]
2-phenylpropoxyadenosine[23]
7-Isopropyl-7H-adenine[20]
7-Propyl-7H-adenine[20]
8-Br-adenine[20]
9-Butyl-9H-adenine[20]
9-Ethyl-9H-adenine[20]
9-Isopropyl-9H-adenine[20]
9-Propyl-9H-adenine[20]
ALLOXAZINE[24]
ARISTEROMYCIN[25]
CGS-15943[26]
CGS-15943[27]
CGS-21680[28]
CVT-6883[29]
FK-453[30]
FK-838[30]
FR-166124[31]
GALANGIN[32]
GNF-PF-2224[33]
GNF-PF-2700[34]
GW-328267[35]
ISOGUANOSINE[36]
ISTRADEFYLLINE[37]
KF-17837[38]
LUF-5417[30]
LUF-5433[30]
LUF-5437[27]
LUF-5767[39]
LUF-5956[22]
LUF-5957[22]
LUF-5962[22]
LUF-5978[40]
LUF-5980[40]
LUF-5981[40]
METHYLTHIOADENOSINE[41]
METRIFUDIL[42]
NECA[43]
OSIP-339391[34]
PD-115199[44]
PSB-0788[29]
PSB-09120[29]
PSB-1115[45]
PSB-601[29]
SB-298[29]
SCH-412348[46]
SCH-442416[47]
SCH-58261[48]
SCH-63390[49]
SLV-320[30]
ST-1535[50]
Tonapofylline[30]
ZM-241385[51]
kuanoniamine D[52]
AgonistATL-146e[5]
CGS 21680[53]
Dexefaroxan[17]
GW-493838[18]
MRE-0094[15]
AntagonistAdenosine A (2A) receptor antagonist[19]
BG-9928[13]
BIIB014[16]
Caffeine[11][12]
KW-3902[13]
KW-6002[9][6][2][14]
SCH 420814[16]
SCH58261[6][2]
T-62[18]
MultitargetCaffeine[11][12]
Dexefaroxan[17]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Blockade of adenosine A2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats. Neuroreport. 1998 Dec 1;9(17):3955-9. To Reference
Ref 2Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. Br J Pharmacol. 2001 Sep;134(1):68-77. To Reference
Ref 3Adenosine A2A receptors in neuroadaptation to repeated dopaminergic stimulation: implications for the treatment of dyskinesias in Parkinson's disease. Neurology. 2003 Dec 9;61(11 Suppl 6):S74-81. To Reference
Ref 4Adenosine A(2A) receptor stimulation reduces inflammation and neointimal growth in a murine carotid ligation model. Arterioscler Thromb Vasc Biol. 2001 May;21(5):791-6. To Reference
Ref 5Selective A(2A) adenosine receptor activation reduces skin pressure ulcer formation and inflammation. Am J Physiol Heart Circ Physiol. 2001 Jul;281(1):H67-74. To Reference
Ref 6Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4. To Reference
Ref 7Characterization of genomic organization of the adenosine A2A receptor gene by molecular and bioinformatics analyses. Brain Res. 2004 Mar 12;1000(1-2):156-73. To Reference
Ref 8Retinal vascular development and oxygen-induced retinopathy: a role for adenosine. Prog Retin Eye Res. 2003 Jan;22(1):95-111. To Reference
Ref 9The treatment of Parkinson's disease--adenosine A2A receptor antagonists. Nippon Rinsho. 2002 Jan;60(1):112-6. To Reference
Ref 10A(2A) adenosine receptor: a novel therapeutic target in renal disease. Am J Physiol Renal Physiol. 2002 Jan;282(1):F10-8. To Reference
Ref 11Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72. To Reference
Ref 12Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51. To Reference
Ref 13Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. To Reference
Ref 14Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999 Nov;147(1):90-5. To Reference
Ref 15Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. To Reference
Ref 16Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54. To Reference
Ref 17The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 18Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 19Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. To Reference
Ref 20Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. To Reference
Ref 21J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. To Reference
Ref 22J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. To Reference
Ref 23J Med Chem. 2007 Apr 19;50(8):1810-27. Epub 2007 Mar 23.Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. To Reference
Ref 24J Med Chem. 2005 Nov 3;48(22):6887-96.2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. To Reference
Ref 25J Med Chem. 2000 Jun 1;43(11):2196-203.Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. To Reference
Ref 26Bioorg. Med. Chem. Lett. 4(21):2539-2544 (1994) To Reference
Ref 27J Med Chem. 2001 Mar 1;44(5):749-62.Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists. To Reference
Ref 28J Med Chem. 2002 Jan 17;45(2):420-9.2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor. To Reference
Ref 29J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. To Reference
Ref 30Bioorg Med Chem. 2010 Mar 15;18(6):2195-203. Epub 2010 Feb 4.2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. To Reference
Ref 31Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. To Reference
Ref 32J Med Chem. 1997 Aug 1;40(16):2588-95.Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. To Reference
Ref 33Eur J Med Chem. 2010 May;45(5):1739-45. Epub 2010 Jan 14.Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine receptor ligands. To Reference
Ref 34Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. To Reference
Ref 35Bioorg Med Chem Lett. 2010 Feb 1;20(3):1219-24. Epub 2009 Dec 1.Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. To Reference
Ref 36Bioorg. Med. Chem. Lett. 1(9):481-486 (1991) To Reference
Ref 37J Med Chem. 2008 Feb 14;51(3):400-6. Epub 2008 Jan 12.Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. To Reference
Ref 38J Med Chem. 1993 Nov 12;36(23):3731-3.Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. To Reference
Ref 39J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. To Reference
Ref 40J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. To Reference
Ref 41J Med Chem. 2004 Apr 22;47(9):2243-55.Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative. To Reference
Ref 42J Med Chem. 1999 Sep 9;42(18):3463-77.N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. To Reference
Ref 43J Med Chem. 1988 Jun;31(6):1179-83.Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. To Reference
Ref 44J Med Chem. 1992 Jun 12;35(12):2342-5.(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. To Reference
Ref 45J Med Chem. 2004 Feb 12;47(4):1031-43.Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability. To Reference
Ref 46Bioorg Med Chem Lett. 2007 Mar 1;17(5):1376-80. Epub 2006 Dec 3.Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. To Reference
Ref 47J Med Chem. 2000 Nov 16;43(23):4359-62.Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography. To Reference
Ref 48J Med Chem. 2004 Dec 2;47(25):6218-29.Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists. To Reference
Ref 49J Med Chem. 1998 Jun 4;41(12):2126-33.Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. To Reference
Ref 50J Med Chem. 2008 Aug 14;51(15):4449-55. Epub 2008 Jul 19.2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. To Reference
Ref 51J Med Chem. 2009 Dec 10;52(23):7640-52.2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition. To Reference
Ref 52J Nat Prod. 1998 Feb;61(2):301-5.Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. To Reference
Ref 53Effects of CGS 21680, a selective adenosine A2A receptor agonist, on allergic airways inflammation in the rat. Eur J Pharmacol. 2002 Mar 8;438(3):183-8. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543