Therapeutic Targets Database
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TTD Target ID: TTDS00188

Target Information
NameAdenosine A2b receptor    
Type of targetSuccessful target    
SynonymsA2b Adenosine receptor    
Adenosine receptor A2b    
DiseaseAsthma
[ICD9: 493   ICD10: J45]
[1][2]
Drug(s)Enprofylline paradoxApprovedAsthma[3][1]
XanthinePre-clinicalApnea[1]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP29275
FunctionReceptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.    
SequenceMLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT FHKIISRYLLCQADVKSGNGQAGVQPALGVGL
Related US Patent6,387,913
6,545,002
6,579,868
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine,   HCl[4]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione[5]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione[5]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione[5]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione[6]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione[7]
1-METHYLXANTHINE[5]
1-Propyl-3,7-dihydro-purine-2,6-dione[6]
1H-Imidazo[4,5-c]quinolin-4-ylamine,   HCl[4]
2'-Me-tecadenoson[8]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine[9]
2,6-diphenyl-8- (1-ethylpropyl)-1-deazapurine[10]
2- (6-amino-8-bromo-9H-purin-9-yl)ethanol[11]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile[12]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile[12]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile[12]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine[4]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine[4]
2-chloro-2'-C-methyl-tecadenoson[8]
2-chloro-N6-cyclopentyladenosine[8]
2-ethyl-4- (thiazol-2-yl)thieno[3,2-d]pyrimidine[13]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione[14]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione[6]
3-noradamantyl-1,3-dipropylxanthine[15]
8- (3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine[16]
8-Bromo-9- (2,3-dihydroxypropyl)-9H-adenine[17]
8-Bromo-9- (2-butyl)-9H-adenine[17]
8-Bromo-9- (2-hydroxypropyl)-9H-adenine[17]
8-Bromo-9- (3-hydroxypropyl)-9H-adenine[17]
8-Bromo-9- (sec-butyl)-9H-adenine[17]
8-Bromo-9-cyclobutyl-9H-adenine[17]
8-Bromo-9-cyclopentyl-9H-adenine[17]
8-Bromo-9-ethyl-9H-adenine[17]
8-Bromo-9-isopropyl-9H-adenine[17]
8-Bromo-9-methyl-9H-adenine[17]
8-Bromo-9-propyl-9H-adenine[17]
8-PHENYL THEOPHYLLINE[16]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione[7]
8-bromo-9-isobutyl-9H-purin-6-amine[11]
9- (sec-Butyl)-9H-adenine[17]
9-Allyl-8-bromo-9H-adenine[17]
9-Cyclobutyl-9H-adenine[17]
9-Isopropyl-9H-adenine[17]
9-Propyl-9H-adenine[17]
ALLOXAZINE[18]
BETA-HYDROXYETHYL THEOPHYLLINE,   Etofylline[11]
CGS-15943[19]
CVT-6694[11]
CVT-6883[19]
CVT-7124[11]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate[20]
FK-453[16]
GNF-PF-2224[21]
GNF-PF-2700[11]
GW-328267[22]
ISOGUANOSINE[23]
KF-17837[24]
LUF-5816[10]
LUF-5978[10]
LUF-5980[10]
LUF-5981[10]
METHYLTHIOADENOSINE[25]
N- (2-[26]
N6- ([9]
N6-CYCLOPENTYLADENOSINE[27]
NECA[27]
OSIP-339391[11]
PD-115199[28]
PSB-0788[19]
PSB-09120[19]
PSB-1115[19]
PSB-601[11]
SB-298[19]
SLV-320[20]
ST-1535[18]
Tonapofylline[20]
ZM-241385[29]
AntagonistEnprofylline paradox[3][1]
Xanthine[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6. To Reference
Ref 2Adenosine A2B receptors: a novel therapeutic target in asthma? Trends Pharmacol Sci. 1998 Apr;19(4):148-53. To Reference
Ref 3The Quintiles Prize Lecture 2004. The identification of the adenosine A2B receptor as a novel therapeutic target in asthma. Br J Pharmacol. 2005 Aug;145(8):1009-15. To Reference
Ref 4J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. To Reference
Ref 5J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. To Reference
Ref 6J Med Chem. 2002 May 23;45(11):2131-8.Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. To Reference
Ref 7J 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 8Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species. To Reference
Ref 9J Med Chem. 2009 Apr 23;52(8):2393-406.N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. To Reference
Ref 10J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. To Reference
Ref 11Eur 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 12J 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 13Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3. Epub 2008 Mar 30.Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. To Reference
Ref 14J Med Chem. 1982 Mar;25(3):197-207.Adenosine receptors: targets for future drugs. To Reference
Ref 15J Med Chem. 2006 Nov 30;49(24):7119-31.Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. To Reference
Ref 16J Med Chem. 2001 Jan 18;44(2):170-9.2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor. To Reference
Ref 17Bioorg 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 18J 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 19J 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 20Bioorg 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 21Bioorg. Med. Chem. Lett. 6(17):2059-2062 (1996) To Reference
Ref 22J Med Chem. 2004 Jul 29;47(16):4041-53.Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor. To Reference
Ref 23Bioorg. Med. Chem. Lett. 1(9):481-486 (1991) To Reference
Ref 24J 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 25J 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 26Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700. Epub 2010 Jan 20.Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. To Reference
Ref 27J 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 28J 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 29Bioorg Med Chem. 2010 Mar 15;18(6):2081-8. Epub 2010 Feb 15.Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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