Therapeutic Targets Database
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TTD Target ID: TTDS00186

Target Information
NameAdenosine A1 receptor    
Type of targetSuccessful target    
SynonymsA(1) adenosine receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Asthma
[ICD9: 493   ICD10: J45]
[2]
Cardiac arrhythmias
[ICD9: 427   ICD10: I47-I49]
[2][3]
Chronic ileitis
[ICD9: 555-558   ICD10: K50-K52]
[4]
Inflammation[2]
Inflammatory bowel disease
[ICD9: 555, 556   ICD10: K50, K51]
[4]
Insulin resistance (obesity-related)[5][3]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[5]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[1]
Renal failure
[ICD9: 584, 585   ICD10: N17, N18, N19]
[2]
Drug(s)CaffeineApprovedFatigue and orthostatic hypotension[6][7]
MK-7418Phase III completedHeart Failure, Congestive[8][9]
RolofyllinePhase III completedHeart failure[10]
TecadenosonPhase IIIAtrial Fibrillation[11][2]
SLV320Phase IIHeart failure[12]
BAY 1067197Phase IHeart Failure
CVT-124Discontinued in Phase IIAtrial fibrillation; Congestive Heart Failure[11][2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP30542
FunctionReceptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.    
SequenceMPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL KIWNDHFRCQPAPPIDEDLPEERPDD
Related US Patent6,495,687
6,576,620
6,586,413
6,605,600
6,605,601
6,638,914
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1-METHYLXANTHINE[13]
2'-Me-tecadenoson[14]
2,6-diphenyl-9H-purine[15]
2-phenylpropoxyadenosine[16]
2-tolyl-6-phenyl-9H-purine[15]
9-Ethyl-9H-adenine[17]
9-Propyl-9H-adenine[17]
A-987306[18]
ARISTEROMYCIN[19]
Anthoptilide C[20]
BRL-61063[21]
CGS-15943[22]
CGS-21680[23]
CIRSIMARIN[24]
CVT-6883[25]
CYPROTERONE ACETATE[26]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate[27]
FK-453[27]
FK-838[27]
FR-166124[28]
GNF-PF-2224[29]
GNF-PF-2700[30]
GW-328267[31]
ISOGUANOSINE[32]
ISTRADEFYLLINE[33]
KF-17837[34]
L-249313[34]
LUF-5417[27]
LUF-5433[27]
LUF-5735[35]
LUF-5737[35]
LUF-5764[35]
LUF-5767[35]
LUF-5816[36]
LUF-5853[37]
LUF-5956[15]
LUF-5957[15]
LUF-5962[15]
LUF-5978[36]
LUF-5980[36]
LUF-5981[36]
LUF-6258[38]
METHYLTHIOADENOSINE[26]
METRIFUDIL[39]
NECA[40]
OSIP-339391[30]
PD-115199[41]
PD-81723[42]
PSB-0788[25]
PSB-1115[25]
PSB-1115[43]
PSB-601[25]
SB-298[25]
SCH-442416[44]
SCH-58261[45]
SCH-63390[22]
SLV-320[27]
ST-1535[46]
Tonapofylline[27]
VCP-28[47]
VUF-8507[48]
ZM-241385[49]
hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide[35]
kuanoniamine D[50]
p-IODOAMPHETAMINE[51]
AgonistCVT-2759[2]
Tecadenoson[11][2]
AntagonistCVT-124[11][2]
Caffeine[6][7]
MK-7418[8][9]
PD-116,948[52][53][54]
Rolofylline[10]
SLV320[12]
MultitargetCaffeine[6][7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2Adenosine receptors and cardiovascular disease: the adenosine-1 receptor (A1) and A1 selective ligands. Cardiovasc Toxicol. 2003;3(1):71-88. To Reference
Ref 3Pharmacology and therapeutic applications of A1 adenosine receptor ligands. Curr Top Med Chem. 2003;3(4):369-85. To Reference
Ref 4Rabbit chronic ileitis leads to up-regulation of adenosine A1/A3 gene products, oxidative stress, and immune modulation. Biochem Pharmacol. 2003 May 1;65(9):1529-38. To Reference
Ref 5Overexpression of the A1 adenosine receptor in adipose tissue protects mice from obesity-related insulin resistance. Diabetes Obes Metab. 2001 Oct;3(5):360-6. To Reference
Ref 6Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72. To Reference
Ref 7Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51. To Reference
Ref 8Merck. Product Development Pipeline. July 15 2009. To Reference
Ref 9Merck. Report of Merck. March 2008. To Reference
Ref 10Association between the PDE4D gene and ischemic stroke in Han Chinese population. Clin Sci (Lond). 2009 Feb 5. [Epub ahead of print] To Reference
Ref 11CV Therapeutics. Company report from CV Therapeutics, Inc. CV Therapeutics. 2009 To Reference
Ref 12Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64. To Reference
Ref 13J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. To Reference
Ref 14Bioorg 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 15J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. To Reference
Ref 16J Med Chem. 2007 Apr 19;50(8):1810-27. Epub 2007 Mar 23.Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine 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. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 19J Med Chem. 2000 Jun 1;43(11):2196-203.Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. To Reference
Ref 20J Nat Prod. 2000 Mar;63(3):318-21.Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali. To Reference
Ref 21J Med Chem. 1994 Feb 18;37(4):476-85.Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. To Reference
Ref 22J Med Chem. 1998 Jun 4;41(12):2126-33.Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists. To Reference
Ref 23J Med Chem. 1999 Apr 22;42(8):1384-92.5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. To Reference
Ref 24J Nat Prod. 1997 Jun;60(6):638-41.Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. To Reference
Ref 25J 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 26J 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 27Bioorg 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 28Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. To Reference
Ref 29Eur J Med Chem. 2010 May;45(5):1739-45. Epub 2010 Jan 14.Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine receptor ligands. To Reference
Ref 30Eur 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 31J 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 32Bioorg. Med. Chem. Lett. 1(9):481-486 (1991) To Reference
Ref 33Bioorg Med Chem. 2007 Jul 15;15(14):5003-17. Epub 2007 Apr 19.N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors. To Reference
Ref 34J 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 35J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. To Reference
Ref 36J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. To Reference
Ref 37Bioorg Med Chem. 2008 Mar 15;16(6):2741-52. Epub 2008 Jan 12.A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. To Reference
Ref 38J Med Chem. 2010 Apr 22;53(8):3028-37.Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. To Reference
Ref 39J Med Chem. 1999 Sep 9;42(18):3463-77.N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. To Reference
Ref 40J 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 41J 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 42J Med Chem. 2008 Sep 25;51(18):5875-9. Epub 2008 Aug 26.Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor. To Reference
Ref 43J 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 44J Med Chem. 2000 Nov 16;43(23):4359-62.Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography. To Reference
Ref 45J Med Chem. 2004 Dec 2;47(25):6218-29.Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists. To Reference
Ref 46J 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 47Bioorg Med Chem. 2010 May 1;18(9):3078-87. Epub 2010 Mar 27.Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. To Reference
Ref 48J Med Chem. 2000 Jun 1;43(11):2227-38.Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. To Reference
Ref 49J Med Chem. 2009 Dec 10;52(23):7640-52.2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition. To Reference
Ref 50J Nat Prod. 1998 Feb;61(2):301-5.Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. To Reference
Ref 51J Med Chem. 1992 Oct 30;35(22):4143-9.Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists. To Reference
Ref 52Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001 Dec;117(6):1594-600. To Reference
Ref 53Influence of the antagonist of adenosine A1 receptors, 8-cyclopentyl-1 ,3-dipropylxanthine, upon the anticonvulsant activity of antiepileptic drugs in mice. Przegl Lek. 2008;65(11):759-63. To Reference
Ref 54Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. Mol Pharmacol. 1987 Mar;31(3):247-52. To Reference



 

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