Target Information

Target General Information

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Target ID

T86679 (Former ID: TTDS00188)

Target Name

Adenosine A2b receptor (ADORA2B)

Synonyms

Adenosine receptor A2b; A2b Adenosine receptor

Gene Name

ADORA2B

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Herpes simplex infection [ICD-11: 1F00]

Supraventricular tachyarrhythmia [ICD-11: BC81]

Function

The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Receptor for adenosine.

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BioChemical Class

GPCR rhodopsin

UniProt ID

AA2BR_HUMAN

Sequence

MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT
RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS
YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV
GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT
FHKIISRYLLCQADVKSGNGQAGVQPALGVGL

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

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Approved Drug(s)

[+] 2 Approved Drugs

Adenosine

Drug Info

Approved

Paroxysmal supraventricular tachycardia

[2], [3]

Vidarabine

Drug Info

Approved

Herpes simplex virus infection

[4], [5]

Clinical Trial Drug(s)

[+] 7 Clinical Trial Drugs

Tonapofylline

Drug Info

Phase 2

Acute and chronic heart failure

[6]

YT-146

Drug Info

Phase 2

Hypertension

[7]

AB928

Drug Info

Phase 1/2

Metastatic colorectal cancer

[8]

CVT-6883

Drug Info

Phase 1

Asthma

[9], [10]

KF-17837

Drug Info

Phase 1

Parkinson disease

[11]

PBF-1129

Drug Info

Phase 1

Non-small-cell lung cancer

[12]

Xanthine

Drug Info

Phase 1

Apnea

[13], [14]

Discontinued Drug(s)

[+] 2 Discontinued Drugs

PF-1913539

Drug Info

Discontinued in Phase 3

Alzheimer disease

[15]

METHYLTHIOADENOSINE

Drug Info

Terminated

Multiple sclerosis

[19]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

BAY 60-6583

Drug Info

Preclinical

Myocardial ischemia

[16]

LAS-101057

Drug Info

Preclinical

Asthma

[17], [18]

Mode of Action

[+] 4 Modes of Action

Modulator

[+] 3 Modulator drugs

Adenosine

Drug Info

[1]

Vidarabine

Drug Info

[1]

CVT-6883

Drug Info

[10]

Inhibitor

[+] 70 Inhibitor drugs

Tonapofylline

Drug Info

[20]

KF-17837

Drug Info

[22]

METHYLTHIOADENOSINE

Drug Info

[27]

ZM-241385

Drug Info

[28]

(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl

Drug Info

[29]

1,3-Diallyl-3,7-dihydro-purine-2,6-dione

Drug Info

[33]

1,3-Diethyl-3,7-dihydro-purine-2,6-dione

Drug Info

[33]

1,3-Dipropyl-3,7-dihydro-purine-2,6-dione

Drug Info

[33]

1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione

Drug Info

[34]

1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[35]

1-METHYLXANTHINE

Drug Info

[33]

1-Propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[34]

1H-Imidazo[4,5-c]quinolin-4-ylamine HCl

Drug Info

[29]

2'-Me-tecadenoson

Drug Info

[36]

2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine

Drug Info

[37]

2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine

Drug Info

[38]

2-(6-amino-8-bromo-9H-purin-9-yl)ethanol

Drug Info

[39]

2-Amino-4,6-di-furan-2-yl-nicotinonitrile

Drug Info

[40]

2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile

Drug Info

[40]

2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile

Drug Info

[40]

2-chloro-2'-C-methyl-tecadenoson

Drug Info

[36]

2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[29]

2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[42]

2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[29]

3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione

Drug Info

[34]

3-noradamantyl-1,3-dipropylxanthine

Drug Info

[44]

8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine

Drug Info

[46]

8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine

Drug Info

[47]

8-Bromo-9-(2-butyl)-9H-adenine

Drug Info

[47]

8-Bromo-9-(2-hydroxypropyl)-9H-adenine

Drug Info

[47]

8-Bromo-9-(3-hydroxypropyl)-9H-adenine

Drug Info

[47]

8-Bromo-9-(sec-butyl)-9H-adenine

Drug Info

[47]

8-Bromo-9-cyclobutyl-9H-adenine

Drug Info

[47]

8-Bromo-9-cyclopentyl-9H-adenine

Drug Info

[47]

8-Bromo-9-ethyl-9H-adenine

Drug Info

[47]

8-bromo-9-isobutyl-9H-purin-6-amine

Drug Info

[39]

8-Bromo-9-isopropyl-9H-adenine

Drug Info

[47]

8-Bromo-9-methyl-9H-adenine

Drug Info

[47]

8-Bromo-9-propyl-9H-adenine

Drug Info

[47]

8-PHENYL THEOPHYLLINE

Drug Info

[46]

8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[35]

9-(sec-Butyl)-9H-adenine

Drug Info

[47]

9-Allyl-8-bromo-9H-adenine

Drug Info

[47]

9-Cyclobutyl-9H-adenine

Drug Info

[47]

9-Isopropyl-9H-adenine

Drug Info

[47]

9-Propyl-9H-adenine

Drug Info

[47]

Alloxazine

Drug Info

[49]

BETA-HYDROXYETHYL THEOPHYLLINE

Drug Info

[39]

CVT-6694

Drug Info

[39]

CVT-7124

Drug Info

[39]

Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate

Drug Info

[20]

GNF-PF-2224

Drug Info

[57]

GNF-PF-2700

Drug Info

[39]

isobutylmethylxanthine

Drug Info

[58]

Isoguanosine

Drug Info

[59]

LUF-5816

Drug Info

[38]

LUF-5978

Drug Info

[38]

LUF-5980

Drug Info

[38]

LUF-5981

Drug Info

[38]

N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide

Drug Info

[64]

N6-((+/-)-endo-norborn-2-yl)adenosine

Drug Info

[37]

N6-CYCLOPENTYLADENOSINE

Drug Info

[65]

PD-115199

Drug Info

[66]

PSB-0788

Drug Info

[67]

PSB-09120

Drug Info

[67]

PSB-1115

Drug Info

[67]

PSB-601

Drug Info

[39]

SB-298

Drug Info

[67]

ST-1535

Drug Info

[49]

[3H]CCPA

Drug Info

[36]

Agonist

[+] 19 Agonist drugs

YT-146

Drug Info

[21]

BAY 60-6583

Drug Info

[25]

(R,S)-PHPNECA

Drug Info

[31]

(S)-PIA

Drug Info

[32]

2-chloroadenosine

Drug Info

[41]

AB-MECA

Drug Info

[48]

AB-NECA

Drug Info

[32]

APNEA

Drug Info

[24]

CGS 21680

Drug Info

[53]

CGS 24012

Drug Info

[54]

CV-1674

Drug Info

[24]

CV-1808

Drug Info

[56]

MRS5151

Drug Info

[63]

N(6)-cyclohexyladenosine

Drug Info

[41]

PENECA

Drug Info

[31]

R-N6-(phenylisopropyl)adenosine

Drug Info

[41]

TCPA

Drug Info

[70]

[3H]HEMADO

Drug Info

[75]

[3H]NECA

Drug Info

[48], [65]

Antagonist

[+] 54 Antagonist drugs

AB928

Drug Info

[12]

PBF-1129

Drug Info

[12]

Xanthine

Drug Info

[23]

PF-1913539

Drug Info

[24]

LAS-101057

Drug Info

[26]

(E)-8-(3-chlorostyryl)-caffeine

Drug Info

[30]

3-isobutyl-8-pyrrolidinoxanthine

Drug Info

[43]

4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one

Drug Info

[45]

AS100

Drug Info

[50]

AS16

Drug Info

[50]

AS70

Drug Info

[50]

AS74

Drug Info

[50]

AS94

Drug Info

[50]

AS95

Drug Info

[50]

AS96

Drug Info

[50]

AS99

Drug Info

[50]

ATL-801

Drug Info

[30]

ATL-844

Drug Info

[30], [51]

ATL802

Drug Info

[52]

CPFPX

Drug Info

[55]

DEPX

Drug Info

[32]

flavone

Drug Info

[45]

I-ABOPX

Drug Info

[32]

KF 17837S

Drug Info

[56]

KF26777

Drug Info

[60]

MRE 2029F20

Drug Info

[61]

MRE 3008F20

Drug Info

[62]

MRS1041

Drug Info

[45]

MRS1042

Drug Info

[45]

MRS1065

Drug Info

[45]

MRS1084

Drug Info

[45]

MRS1086

Drug Info

[45]

MRS1088

Drug Info

[45]

MRS1093

Drug Info

[45]

MRS1132

Drug Info

[45]

MRS1191

Drug Info

[30]

MRS1523

Drug Info

[30]

MRS1706

Drug Info

[52]

MRS923

Drug Info

[45]

MRS928

Drug Info

[45]

PSB-10

Drug Info

[68]

PSB-11

Drug Info

[68]

PSB36

Drug Info

[69]

PSB603

Drug Info

[67]

sakuranetin

Drug Info

[45]

visnagin

Drug Info

[45]

VUF5574

Drug Info

[71]

xanthine amine congener

Drug Info

[54], [72]

XCC

Drug Info

[51]

[125I]ABOPX

Drug Info

[32]

[125I]ZM-241385

Drug Info

[73]

[3H]DPCPX

Drug Info

[74]

[3H]OSIP339391

Drug Info

[39], [74]

[3H]ZM 241385

Drug Info

[72]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-regulating microRNAs

Target-regulating microRNAs Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 5 KEGG Pathways

Rap1 signaling pathway

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Vascular smooth muscle contraction

Alcoholism

NetPath Pathway

[+] 2 NetPath Pathways

TGF_beta_Receptor Signaling Pathway

TCR Signaling Pathway

Pathwhiz Pathway

[+] 1 Pathwhiz Pathways

Intracellular Signalling Through Adenosine Receptor A2b and Adenosine

PID Pathway

[+] 1 PID Pathways

C-MYB transcription factor network

Reactome

[+] 3 Reactome Pathways

Adenosine P1 receptors

G alpha (s) signalling events

Surfactant metabolism

WikiPathways

[+] 4 WikiPathways

Nucleotide GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 2

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. (Ligand id: 2844).

REF 3

Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.

REF 4

REF 5

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050486.

REF 6

Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.

REF 7

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001363)

REF 8

ClinicalTrials.gov (NCT04660812) An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.

REF 9

REF 10

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.

REF 11

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005980)

REF 12

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 13

REF 14

Febuxostat (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 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021875)

REF 16

Circadian rhythm as a therapeutic target. Nat Rev Drug Discov. 2021 Apr;20(4):287-307.

REF 17

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027811)

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987)

REF 20

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.

REF 21

Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10.

REF 22

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.

REF 23

Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6.

REF 24

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.

REF 25

Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation. 2007 Mar 27;115(12):1581-90.

REF 26

Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. ACS Med Chem Lett. 2010 Dec 20;2(3):213-8.

REF 27

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.

REF 28

Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088.

REF 29

1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.

REF 30

REF 31

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.

REF 32

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.

REF 33

Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.

REF 34

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.

REF 35

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.

REF 36

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.

REF 37

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.

REF 38

2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.

REF 39

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.

REF 40

2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.

REF 41

Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol. 1980 Jun;58(6):673-91.

REF 42

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.

REF 43

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.

REF 44

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.

REF 45

Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.

REF 46

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.

REF 47

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.

REF 48

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.

REF 49

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.

REF 50

Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12.

REF 51

[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol. 2001 Mar 15;61(6):657-63.

REF 52

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.

REF 53

[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 54

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.

REF 55

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.

REF 56

Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261. Br J Pharmacol. 1997 Jun;121(3):353-60.

REF 57

Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist, Bioorg. Med. Chem. Lett. 6(17):2059-2062 (1996).

REF 58

Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207.

REF 59

High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).

REF 60

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.

REF 61

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.

REF 62

Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.

REF 63

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.

REF 64

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.

REF 65

Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.

REF 66

(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.

REF 67

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.

REF 68

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.

REF 69

Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists. Bioorg Med Chem. 2006 Jun 1;14(11):3654-61.

REF 70

Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. Br J Pharmacol. 1997 Nov;122(5):867-74.

REF 71

A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93.

REF 72

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.

REF 73

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