Target Information

Target General Infomation
Target ID
T86679
Former ID
TTDS00188
Target Name
Adenosine A2b receptor
Gene Name
ADORA2B
Synonyms
A2b Adenosine receptor; Adenosine receptor A2b; ADORA2B
Target Type
Successful
Disease Asthma [ICD10: J45]
Apnea [ICD9: 786.03; ICD10: R06.81]
Herpes simplex virus infection [ICD9: 54; ICD10: B00]
Hypertension [ICD9: 401; ICD10: I10-I16]
Multiple scierosis [ICD9: 340; ICD10: G35]
Non-insulin dependent diabetes [ICD10: E11.9]
Parkinson's disease [ICD9: 332; ICD10: G20]
Paroxysmal supraventricular tachycardia [ICD9: 427, 427.0, 427.1, 427.89, 785.0; ICD10: I47-I49, I47.1, I47.2, R00.0]
Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T86679
UniProt ID
P29275
Sequence
MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT
RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS
YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV
GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT
FHKIISRYLLCQADVKSGNGQAGVQPALGVGL
Structure
1MMH; 1UPE; 2YDO; 2YDV; 3EML; 3PWH; 3QAK; 3REY; 3RFM; 3UZA; 3UZC; 3VG9; 3VGA; 4EIY
Drugs and Mode of Action
Drug(s) Adenosine Drug Info Approved Paroxysmal supraventricular tachycardia [536838], [539879]
Vidarabine Drug Info Approved Herpes simplex virus infection [468037], [538596]
Tonapofylline Drug Info Phase 2/3 Discovery agent [522369], [540973]
YT-146 Drug Info Phase 2 Hypertension [544864]
CVT-6883 Drug Info Phase 1 Asthma [532020], [540984]
KF-17837 Drug Info Phase 1 Parkinson's disease [546031]
Xanthine Drug Info Phase 1 Apnea [467794], [527315]
LAS-101057 Drug Info Preclinical Asthma [540986], [548701]
METHYLTHIOADENOSINE Drug Info Terminated Multiple scierosis [544778]
ZM-241385 Drug Info Terminated Discovery agent [540649], [546100]
Inhibitor (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl Drug Info [530590]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione Drug Info [533429]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione Drug Info [533429]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Drug Info [533429]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info [526958]
1-METHYLXANTHINE Drug Info [533429]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl Drug Info [530590]
2'-Me-tecadenoson Drug Info [529098]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info [530035]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info [528673]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Drug Info [530966]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile Drug Info [529602]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Drug Info [529602]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile Drug Info [529602]
2-chloro-2'-C-methyl-tecadenoson Drug Info [529098]
2-chloro-N6-cyclopentyladenosine Drug Info [529098]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info [530590]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info [530590]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info [533542]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
3-noradamantyl-1,3-dipropylxanthine Drug Info [528544]
8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine Drug Info [525962]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine Drug Info [530014]
8-Bromo-9-(2-butyl)-9H-adenine Drug Info [530014]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine Drug Info [530014]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info [530014]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info [530014]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info [530014]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info [530014]
8-Bromo-9-ethyl-9H-adenine Drug Info [530014]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info [530966]
8-Bromo-9-isopropyl-9H-adenine Drug Info [530014]
8-Bromo-9-methyl-9H-adenine Drug Info [530014]
8-Bromo-9-propyl-9H-adenine Drug Info [530014]
8-PHENYL THEOPHYLLINE Drug Info [525962]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Drug Info [526958]
9-(sec-Butyl)-9H-adenine Drug Info [530014]
9-Allyl-8-bromo-9H-adenine Drug Info [530014]
9-Cyclobutyl-9H-adenine Drug Info [530014]
9-Isopropyl-9H-adenine Drug Info [530014]
9-Propyl-9H-adenine Drug Info [530014]
ALLOXAZINE Drug Info [527823]
BETA-HYDROXYETHYL THEOPHYLLINE Drug Info [530966]
CVT-6694 Drug Info [530966]
CVT-7124 Drug Info [530966]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info [530752]
GNF-PF-2224 Drug Info [551303]
GNF-PF-2700 Drug Info [530966]
ISOGUANOSINE Drug Info [551229]
KF-17837 Drug Info [533955]
LUF-5816 Drug Info [528673]
LUF-5978 Drug Info [528673]
LUF-5980 Drug Info [528673]
LUF-5981 Drug Info [528673]
METHYLTHIOADENOSINE Drug Info [527040]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info [530694]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info [530035]
N6-CYCLOPENTYLADENOSINE Drug Info [533449]
NECA Drug Info [533449]
OSIP-339391 Drug Info [530966]
PD-115199 Drug Info [527717]
PSB-0788 Drug Info [530243]
PSB-09120 Drug Info [530243]
PSB-1115 Drug Info [530243]
PSB-601 Drug Info [530966]
SB-298 Drug Info [530243]
ST-1535 Drug Info [527823]
Tonapofylline Drug Info [530752]
ZM-241385 Drug Info [530768]
Agonist (R)-PIA Drug Info [533531]
(R,S)-PHPNECA Drug Info [526375]
(S)-PIA Drug Info [525595]
2-chloroadenosine Drug Info [533531]
AB-MECA Drug Info [534553]
AB-NECA Drug Info [525595]
APNEA Drug Info [534821]
BAY 60-6583 Drug Info [528730]
CGS 24012 Drug Info [533734]
CV-1674 Drug Info [534821]
CV-1808 Drug Info [534396]
HEMADO Drug Info [528546]
MRS5151 Drug Info [529435]
N(6)-cyclohexyladenosine Drug Info [533531]
PENECA Drug Info [526375]
TCPA Drug Info [534519]
YT-146 Drug Info [533910]
[3H]CGS 21680 Drug Info [533253]
[3H]NECA Drug Info [534553]
Antagonist 3-isobutyl-8-pyrrolidinoxanthine Drug Info [526188]
Adenosine A2b antagonists Drug Info [543534]
AS100 Drug Info [527796]
AS16 Drug Info [527796]
AS70 Drug Info [527796]
AS74 Drug Info [527796]
AS94 Drug Info [527796]
AS95 Drug Info [527796]
AS96 Drug Info [527796]
AS99 Drug Info [527796]
ATL-801 Drug Info [543534]
ATL-844 Drug Info [543534]
ATL802 Drug Info [525731]
CPFPX Drug Info [526448]
CSC Drug Info [543534]
DEPX Drug Info [525595]
flavone Drug Info [534145]
I-ABOPX Drug Info [525595]
KF 17837S Drug Info [534396]
KF26777 Drug Info [526356]
LAS-101057 Drug Info [532805]
MRE 2029F20 Drug Info [526981]
MRE 3008F20 Drug Info [528068]
MRS1041 Drug Info [534145]
MRS1042 Drug Info [534145]
MRS1065 Drug Info [534145]
MRS1066 Drug Info [534145]
MRS1084 Drug Info [534145]
MRS1086 Drug Info [534145]
MRS1088 Drug Info [534145]
MRS1093 Drug Info [534145]
MRS1132 Drug Info [534145]
MRS1191 Drug Info [543534]
MRS1523 Drug Info [543534]
MRS1706 Drug Info [525731]
MRS923 Drug Info [534145]
MRS928 Drug Info [534145]
PSB-10 Drug Info [526390]
PSB-11 Drug Info [526390]
PSB36 Drug Info [528011]
PSB603 Drug Info [530243]
sakuranetin Drug Info [534145]
visnagin Drug Info [534145]
VUF5574 Drug Info [534717]
Xanthine Drug Info [535254]
xanthine amine congener Drug Info [525667]
XCC Drug Info [526013]
[125I]ABOPX Drug Info [525595]
[125I]ZM-241385 Drug Info [534233]
[3H]DPCPX Drug Info [527107]
[3H]MRS1754 Drug Info [526013]
[3H]OSIP339391 Drug Info [527107]
[3H]PSB603 Drug Info [530243]
[3H]SCH 58261 Drug Info [534821]
[3H]XAC Drug Info [533734]
[3H]ZM 241385 Drug Info [525667]
Modulator Adenosine Drug Info [556264]
CVT-6883 Drug Info [532020]
Vidarabine Drug Info [556264]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Rap1 signaling pathway
Calcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
Alcoholism
NetPath Pathway TGF_beta_Receptor Signaling Pathway
TCR Signaling Pathway
Pathway Interaction Database C-MYB transcription factor network
PathWhiz Pathway Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Reactome Adenosine P1 receptors
G alpha (s) signalling events
Surfactant metabolism
WikiPathways Nucleotide GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 467794(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4557).
Ref 468037(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4806).
Ref 522369ClinicalTrials.gov (NCT00709865) Phase 2b Study to Assess the Safety and Tolerability of IV Tonapofylline in Subjects With Acute Decompensated Heart Failure (ADHF) and Renal Insufficiency. U.S. National Institutes of Health.
Ref 527315Febuxostat (TMX-67), a novel, non-purine, selective inhibitor of xanthine oxidase, is safe and decreases serum urate in healthy volunteers. Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1111-6.
Ref 532020GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95.
Ref 536838Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
Ref 538596FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050486.
Ref 539879(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2844).
Ref 540649(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 405).
Ref 540973(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5605).
Ref 540984(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5615).
Ref 540986(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5617).
Ref 544778Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987)
Ref 544864Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001363)
Ref 546031Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005980)
Ref 546100Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006356)
Ref 548701Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027811)
Ref 525595Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells. Mol Pharmacol. 1999 Oct;56(4):705-13.
Ref 525667Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors. Drug Des Discov. 1999 Nov;16(3):217-26.
Ref 525731Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem. 2000 Mar 23;43(6):1165-72.
Ref 525962J 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.
Ref 526013[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol. 2001 Mar 15;61(6):657-63.
Ref 526188Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2). Biochem Pharmacol. 2001 Nov 1;62(9):1163-73.
Ref 526332J 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.
Ref 526356KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist. Eur J Pharmacol. 2002 May 31;444(3):133-41.
Ref 526375N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. J Med Chem. 2002 Jul 18;45(15):3271-9.
Ref 526390Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. J Med Chem. 2002 Aug 1;45(16):3440-50.
Ref 526448Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J Med Chem. 2002 Nov 7;45(23):5150-6.
Ref 526958J 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 prodrugswith peroral bioavailability.
Ref 526981Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists. J Med Chem. 2004 Mar 11;47(6):1434-47.
Ref 527040J 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.
Ref 527107[3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors. Biochem Pharmacol. 2004 Jul 15;68(2):305-12.
Ref 527717J 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.
Ref 527796Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12. Epub 2005 Oct 10.
Ref 527823J 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.
Ref 528011Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists. Bioorg Med Chem. 2006 Jun 1;14(11):3654-61. Epub 2006 Feb 2.
Ref 528068Nat Rev Drug Discov. 2006 Mar;5(3):247-64.Adenosine receptors as therapeutic targets.
Ref 528544J Med Chem. 2006 Nov 30;49(24):7119-31.Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Ref 528546[3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8. Epub 2006 Oct 27.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 528730Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation. 2007 Mar 27;115(12):1581-90. Epub 2007 Mar 12.
Ref 529098Bioorg 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 selectivityfor A1 receptor from different species.
Ref 529419Bioorg 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.
Ref 529435Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.
Ref 529602J 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.
Ref 530014Bioorg 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.
Ref 530035J 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.
Ref 530243J 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.
Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 530694Bioorg 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.
Ref 530752Bioorg 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.
Ref 530768Bioorg 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.
Ref 530966Eur 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.
Ref 532020GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95.
Ref 532805Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. ACS Med Chem Lett. 2010 Dec 20;2(3):213-8.
Ref 533253[3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain. J Pharmacol Exp Ther. 1989 Dec;251(3):888-93.
Ref 533429J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
Ref 533449J Med Chem. 1988 Jun;31(6):1179-83.Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Ref 533531Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol. 1980 Jun;58(6):673-91.
Ref 533542J Med Chem. 1982 Mar;25(3):197-207.Adenosine receptors: targets for future drugs.
Ref 533734Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97.
Ref 533910Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10.
Ref 533955J 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.
Ref 534145J Med Chem. 1996 Jun 7;39(12):2293-301.Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Ref 534233125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor. Mol Pharmacol. 1995 Dec;48(6):970-4.
Ref 534396Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261. Br J Pharmacol. 1997 Jun;121(3):353-60.
Ref 534519Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. Br J Pharmacol. 1997 Nov;122(5):867-74.
Ref 534553Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.
Ref 534717J Med Chem. 1998 Oct 8;41(21):3987-93.A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Ref 534821Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors. Biochem Pharmacol. 1999 Jan 1;57(1):65-75.
Ref 535254Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6.
Ref 543534(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 20).
Ref 551229High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
Ref 551303Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist, Bioorg. Med. Chem. Lett. 6(17):2059-2062 (1996).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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