General Information of Drug Therapeutic Target (DTT) (ID: TTNE7KG)

DTT Name Adenosine A2b receptor (ADORA2B)
Synonyms Adenosine receptor A2b; A2b Adenosine receptor
Gene Name ADORA2B
DTT Type
Successful target
[1]
Related Disease
Herpes simplex infection [ICD-11: 1F00]
Supraventricular tachyarrhythmia [ICD-11: BC81]
BioChemical Class
GPCR rhodopsin
UniProt ID
AA2BR_HUMAN
TTD ID
T86679
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT
RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS
YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV
GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT
FHKIISRYLLCQADVKSGNGQAGVQPALGVGL
Function The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Receptor for adenosine.
KEGG Pathway
Rap1 signaling pathway (hsa04015 )
Calcium signaling pathway (hsa04020 )
Neuroactive ligand-receptor interaction (hsa04080 )
Vascular smooth muscle contraction (hsa04270 )
Alcoholism (hsa05034 )
Reactome Pathway
G alpha (s) signalling events (R-HSA-418555 )
Surfactant metabolism (R-HSA-5683826 )
Adenosine P1 receptors (R-HSA-417973 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Adenosine DMM2NSK Paroxysmal supraventricular tachycardia BC81.Z Approved [1]
Vidarabine DM0N85H Herpes simplex virus infection 1F00 Approved [1]
------------------------------------------------------------------------------------
7 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [2]
YT-146 DM3YVKQ Hypertension BA00-BA04 Phase 2 [3]
AB928 DMDOXMN Metastatic colorectal cancer 2B91 Phase 1/2 [4]
CVT-6883 DMY84TW Asthma CA23 Phase 1 [5]
KF-17837 DMQ6DLZ Parkinson disease 8A00.0 Phase 1 [6]
PBF-1129 DMOPGXM Non-small-cell lung cancer 2C25.Y Phase 1 [4]
Xanthine DMFBOQ7 Apnea MD11.0 Phase 1 [7]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 Clinical Trial Drug(s)
3 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-1913539 DMXEU14 Alzheimer disease 8A20 Discontinued in Phase 3 [8]
Methylthioadenosine DMC8J6F Multiple sclerosis 8A40 Terminated [11]
ZM-241385 DMWQ38G N. A. N. A. Terminated [12]
------------------------------------------------------------------------------------
2 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 60-6583 DMTEJV1 Myocardial ischemia BA6Z Preclinical [9]
LAS-101057 DMFBMXD Asthma CA23 Preclinical [10]
------------------------------------------------------------------------------------
132 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl DM4FSTL Discovery agent N.A. Investigative [13]
(E)-8-(3-chlorostyryl)-caffeine DMQT15Z Discovery agent N.A. Investigative [14]
(R,S)-PHPNECA DMQO71C Discovery agent N.A. Investigative [15]
(S)-PIA DM04BHI Discovery agent N.A. Investigative [16]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione DMEV8G2 Discovery agent N.A. Investigative [17]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione DMKYE16 Discovery agent N.A. Investigative [17]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione DMUL2B3 Discovery agent N.A. Investigative [17]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione DMMRV21 Discovery agent N.A. Investigative [18]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione DMSNK98 Discovery agent N.A. Investigative [19]
1-METHYLXANTHINE DM2WQ1E Discovery agent N.A. Investigative [17]
1-Propyl-3,7-dihydro-purine-2,6-dione DML5J94 Discovery agent N.A. Investigative [18]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl DMME09C Discovery agent N.A. Investigative [13]
2'-Me-tecadenoson DMY2GXT Discovery agent N.A. Investigative [20]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine DMMESIU Discovery agent N.A. Investigative [21]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine DMY3C78 Discovery agent N.A. Investigative [22]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol DMRBX1D Discovery agent N.A. Investigative [23]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile DMVN0EC Discovery agent N.A. Investigative [24]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile DMP4NHD Discovery agent N.A. Investigative [24]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile DMUYTXS Discovery agent N.A. Investigative [24]
2-chloro-2'-C-methyl-tecadenoson DMD3ZNP Discovery agent N.A. Investigative [20]
2-chloroadenosine DMYPQEW Discovery agent N.A. Investigative [25]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine DM6CZAN Discovery agent N.A. Investigative [13]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine DMWCGE8 Discovery agent N.A. Investigative [26]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine DMDC6XP Discovery agent N.A. Investigative [13]
3-isobutyl-8-pyrrolidinoxanthine DM9GM1H Discovery agent N.A. Investigative [27]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione DMKYPUW Discovery agent N.A. Investigative [18]
3-noradamantyl-1,3-dipropylxanthine DMFHYAE Discovery agent N.A. Investigative [28]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one DM8642Z Discovery agent N.A. Investigative [29]
8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine DMLQPVH Discovery agent N.A. Investigative [30]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine DMMQ79W Discovery agent N.A. Investigative [31]
8-Bromo-9-(2-butyl)-9H-adenine DM5DCPF Discovery agent N.A. Investigative [31]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine DMKW2PE Discovery agent N.A. Investigative [31]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine DMA258T Discovery agent N.A. Investigative [31]
8-Bromo-9-(sec-butyl)-9H-adenine DMSQPFM Discovery agent N.A. Investigative [31]
8-Bromo-9-cyclobutyl-9H-adenine DMUTV76 Discovery agent N.A. Investigative [31]
8-Bromo-9-cyclopentyl-9H-adenine DMCK0O1 Discovery agent N.A. Investigative [31]
8-Bromo-9-ethyl-9H-adenine DM4YAD6 Discovery agent N.A. Investigative [31]
8-bromo-9-isobutyl-9H-purin-6-amine DMZF3UN Discovery agent N.A. Investigative [23]
8-Bromo-9-isopropyl-9H-adenine DMIN9HC Discovery agent N.A. Investigative [31]
8-Bromo-9-methyl-9H-adenine DM1DS3B Discovery agent N.A. Investigative [31]
8-Bromo-9-propyl-9H-adenine DMRIPU5 Discovery agent N.A. Investigative [31]
8-PHENYL THEOPHYLLINE DMFGUCY Discovery agent N.A. Investigative [30]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione DMHQGOC Discovery agent N.A. Investigative [19]
9-(sec-Butyl)-9H-adenine DMFKVPA Discovery agent N.A. Investigative [31]
9-Allyl-8-bromo-9H-adenine DM8VZIY Discovery agent N.A. Investigative [31]
9-Cyclobutyl-9H-adenine DM04QWX Discovery agent N.A. Investigative [31]
9-Isopropyl-9H-adenine DMBQLAI Discovery agent N.A. Investigative [31]
9-Propyl-9H-adenine DMQTEPY Discovery agent N.A. Investigative [31]
AB-MECA DMQPHFU Discovery agent N.A. Investigative [32]
AB-NECA DME8G7F Discovery agent N.A. Investigative [16]
Alloxazine DM7U2BE Discovery agent N.A. Investigative [33]
APNEA DMW45GK Discovery agent N.A. Investigative [8]
AS100 DMXZ8S9 Discovery agent N.A. Investigative [34]
AS16 DMP0A17 Discovery agent N.A. Investigative [34]
AS70 DM9CIJP Discovery agent N.A. Investigative [34]
AS74 DMZPHKG Discovery agent N.A. Investigative [34]
AS94 DM7WJ6F Discovery agent N.A. Investigative [34]
AS95 DMN3E9Q Discovery agent N.A. Investigative [34]
AS96 DML6I8J Discovery agent N.A. Investigative [34]
AS99 DMZ7FJN Discovery agent N.A. Investigative [34]
ATL-801 DMAZ0EQ Non-insulin dependent diabetes 5A11 Investigative [14]
ATL-844 DM6V9SC Asthma CA23 Investigative [14], [35]
ATL802 DMYMCQA Discovery agent N.A. Investigative [36]
BETA-HYDROXYETHYL THEOPHYLLINE DMGP9MN Discovery agent N.A. Investigative [23]
CGS 21680 DMZ0TGY Discovery agent N.A. Investigative [37]
CGS 24012 DMRU8G7 Discovery agent N.A. Investigative [38]
CPFPX DMFE5GX Discovery agent N.A. Investigative [39]
CV-1674 DM9AL7W Discovery agent N.A. Investigative [8]
CV-1808 DM07VRS Discovery agent N.A. Investigative [40]
CVT-6694 DMYC1DW Discovery agent N.A. Investigative [23]
CVT-7124 DM53VA8 Discovery agent N.A. Investigative [23]
DEPX DM4JM50 Discovery agent N.A. Investigative [16]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate DMK4T5Y Discovery agent N.A. Investigative [2]
Flavone DMEQH6J Discovery agent N.A. Investigative [29]
GNF-PF-2224 DM26UKN Discovery agent N.A. Investigative [41]
GNF-PF-2700 DMC56YJ Discovery agent N.A. Investigative [23]
I-ABOPX DM5X0JS Discovery agent N.A. Investigative [16]
isobutylmethylxanthine DM46F5X Discovery agent N.A. Investigative [42]
Isoguanosine DMAFLCJ Discovery agent N.A. Investigative [43]
KF 17837S DM7W9MT Discovery agent N.A. Investigative [40]
KF26777 DMPBDW0 Discovery agent N.A. Investigative [44]
LUF-5816 DMQZDMH Discovery agent N.A. Investigative [22]
LUF-5978 DMCTM3L Discovery agent N.A. Investigative [22]
LUF-5980 DMGOIF5 Discovery agent N.A. Investigative [22]
LUF-5981 DMHO3XL Discovery agent N.A. Investigative [22]
MRE 2029F20 DMUK1PA Discovery agent N.A. Investigative [45]
MRE 3008F20 DM72US0 Discovery agent N.A. Investigative [46]
MRS1041 DMBXKYR Discovery agent N.A. Investigative [29]
MRS1042 DMVT865 Discovery agent N.A. Investigative [29]
MRS1065 DMYAHU3 Discovery agent N.A. Investigative [29]
MRS1084 DMKELWG Discovery agent N.A. Investigative [29]
MRS1086 DM1K5E2 Discovery agent N.A. Investigative [29]
MRS1088 DMSKWL7 Discovery agent N.A. Investigative [29]
MRS1093 DM801AO Discovery agent N.A. Investigative [29]
MRS1132 DMY4C0G Discovery agent N.A. Investigative [29]
MRS1191 DM9WX3C Discovery agent N.A. Investigative [14]
MRS1523 DM4AONZ Discovery agent N.A. Investigative [14]
MRS1706 DM5I7PL Discovery agent N.A. Investigative [36]
MRS5151 DM1GUTC Discovery agent N.A. Investigative [47]
MRS923 DMMN42V Discovery agent N.A. Investigative [29]
MRS928 DMKJ9WM Discovery agent N.A. Investigative [29]
N(6)-cyclohexyladenosine DMHINE0 Discovery agent N.A. Investigative [25]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide DMLTROU Discovery agent N.A. Investigative [48]
N6-((+/-)-endo-norborn-2-yl)adenosine DM30KXV Discovery agent N.A. Investigative [21]
N6-cyclopentyladenosine DMD6AJO Discovery agent N.A. Investigative [49]
PD-115199 DMQ4LRZ Discovery agent N.A. Investigative [50]
PENECA DMIDSJ9 Discovery agent N.A. Investigative [15]
PSB-0788 DM0FKV9 Discovery agent N.A. Investigative [51]
PSB-09120 DMAFHLX Discovery agent N.A. Investigative [51]
PSB-10 DMXDWO7 Discovery agent N.A. Investigative [52]
PSB-11 DMGK2PC Discovery agent N.A. Investigative [52]
PSB-1115 DMOH2VC Discovery agent N.A. Investigative [51]
PSB-601 DMBIK7D Discovery agent N.A. Investigative [23]
PSB36 DMBGM1E Discovery agent N.A. Investigative [53]
PSB603 DM6QERS Discovery agent N.A. Investigative [51]
R-N6-(phenylisopropyl)adenosine DM2N3BA Discovery agent N.A. Investigative [25]
sakuranetin DMUAQYZ Discovery agent N.A. Investigative [29]
SB-298 DMU2J3K Discovery agent N.A. Investigative [51]
ST-1535 DMUTC9Z Discovery agent N.A. Investigative [33]
TCPA DMTF4VI Discovery agent N.A. Investigative [54]
visnagin DMCSHE8 Discovery agent N.A. Investigative [29]
VUF5574 DMUA751 Discovery agent N.A. Investigative [55]
xanthine amine congener DMGYVFD Discovery agent N.A. Investigative [56], [38]
XCC DM8PADV Discovery agent N.A. Investigative [35]
[125I]ABOPX DMZBNK9 Discovery agent N.A. Investigative [16]
[125I]ZM-241385 DME53D6 Discovery agent N.A. Investigative [57]
[3H]CCPA DMHDGB3 Discovery agent N.A. Investigative [20]
[3H]DPCPX DM9GY7O Discovery agent N.A. Investigative [58]
[3H]HEMADO DMEO6AH Discovery agent N.A. Investigative [59]
[3H]NECA DMAO9SH Discovery agent N.A. Investigative [32], [49]
[3H]OSIP339391 DM4BY5J Discovery agent N.A. Investigative [58], [23]
[3H]ZM 241385 DMKU4YQ Discovery agent N.A. Investigative [56]
------------------------------------------------------------------------------------
⏷ Show the Full List of 132 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Apnea CA23 Hyperplastic tonsil 8.57E-02 -0.76 -0.62
Asthma CA23 Nasal and bronchial airway 7.89E-02 0.09 0.11
Parkinson's disease 8A00.0 Substantia nigra tissue 7.34E-01 -0.01 -0.06
------------------------------------------------------------------------------------

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
2 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
3 Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 GS-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.
6 Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. J Med Chem. 1993 Nov 12;36(23):3731-3.
7 Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6.
8 Differences 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.
9 Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation. 2007 Mar 27;115(12):1581-90.
10 Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. ACS Med Chem Lett. 2010 Dec 20;2(3):213-8.
11 Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.
12 Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088.
13 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.
14 URL: 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).
15 N(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.
16 Characterization 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.
17 Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.
18 Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.
19 Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic... J Med Chem. 2004 Feb 12;47(4):1031-43.
20 5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 ... Bioorg Med Chem. 2008 Jan 1;16(1):336-53.
21 N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.
22 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
23 Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. Eur J Med Chem. 2010 Aug;45(8):3459-71.
24 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.
25 Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol. 1980 Jun;58(6):673-91.
26 Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3.
27 Inhibition 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.
28 Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31.
29 Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.
30 2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic gluc... J Med Chem. 2001 Jan 18;44(2):170-9.
31 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. Bioorg Med Chem. 2009 Apr 1;17(7):2812-22.
32 Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.
33 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 pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
34 Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12.
35 [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol. 2001 Mar 15;61(6):657-63.
36 Anilide 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.
37 [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.
38 Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97.
39 Synthesis 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.
40 Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261. Br J Pharmacol. 1997 Jun;121(3):353-60.
41 Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist, Bioorg. Med. Chem. Lett. 6(17):2059-2062 (1996).
42 Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207.
43 High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
44 KF26777 (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.
45 Design, 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.
46 Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.
47 Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.
48 Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700.
49 Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.
50 (E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. J Med Chem. 1992 Jun 12;35(12):2342-5.
51 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with... J Med Chem. 2009 Jul 9;52(13):3994-4006.
52 Imidazo[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.
53 Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists. Bioorg Med Chem. 2006 Jun 1;14(11):3654-61.
54 Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. Br J Pharmacol. 1997 Nov;122(5):867-74.
55 A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93.
56 Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors. Drug Des Discov. 1999 Nov;16(3):217-26.
57 125I-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.
58 [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors. Biochem Pharmacol. 2004 Jul 15;68(2):305-12.
59 [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8.