Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTNE7KG)

• DTT Name: Adenosine A2b receptor (ADORA2B) DTT Info
• UniProt ID: AA2BR_HUMAN
• Gene Name: ADORA2B

Molecule-Related Drug & Molecule List

2 Approved Drug(s) Transported by This DTP

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) Transported by This DTP

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]

3 Discontinued Drug(s) Transported by This DTP

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) Transported by This DTP

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) Transported by This DTP

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]

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.