Target General Infomation
Target ID
T92072
Former ID
TTDS00186
Target Name
Adenosine A1 receptor
Gene Name
ADORA1
Synonyms
A(1) adenosine receptor; ADORA1
Target Type
Successful
Disease Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48]
Autoimmune diabetes [ICD10: E08-E13]
Atrial fibrillation; Cardiac arrhythmias [ICD9:272, 427.31, 427; ICD10: E78, I48, I47-I49]
Allergy [ICD9: 995.3; ICD10: T78.4]
Acute and chronic heart failure [ICD9: 428; ICD10: I50]
Cardiac disease [ICD10: I00-I99]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Fatigue; Orthostatic hypotension [ICD9: 458.0, 780.7; ICD10: I95.1, R53]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Heart failure [ICD9: 428; ICD10: I50]
Hypertension [ICD9: 401; ICD10: I10-I16]
Hypertriglyceridemia [ICD9: 272.1, 427; ICD10: E78.1, E78.2, E78.3, I47-I49]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Multiple scierosis [ICD9: 340; ICD10: G35]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Parkinson's disease [ICD9: 332; ICD10: G20]
Renal failure [ICD9: 584, 585; ICD10: N17, N18, N19]
Sepsis [ICD9: 995.91; ICD10: A40, A41]
Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T92072
UniProt ID
Sequence
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD
Drugs and Mode of Action
Drug(s) Caffeine Drug Info Approved Fatigue; Orthostatic hypotension [536949], [540664]
Rolofylline Drug Info Phase 3 Heart failure [537064], [540972]
Tonapofylline Drug Info Phase 2/3 Discovery agent [522369], [540973]
AMP-579 Drug Info Phase 2 Hyperlipidaemia [544253]
Apaxifylline Drug Info Phase 2 Cognitive disorders [544358]
BAY 1067197 Drug Info Phase 2 Heart failure [549353]
BG-9928 Drug Info Phase 2 Acute and chronic heart failure [536372]
Capadenoson Drug Info Phase 2 Atrial fibrillation [522175]
DTI-0009 (oral) Drug Info Phase 2 Atrial fibrillation [521520]
SELODENOSON Drug Info Phase 2 Cardiac arrhythmias [521520]
SLV320 Drug Info Phase 2 Heart failure [537065], [540245]
INO-8875 Drug Info Phase 1/2 Glaucoma [523044]
GS 9667 Drug Info Phase 1 Hypertriglyceridemia [540961], [547637]
KF-17837 Drug Info Phase 1 Parkinson's disease [546031]
SCH-442416 Drug Info Phase 1 Discovery agent [522117], [540246]
CVT-124 Drug Info Discontinued in Phase 3 Autoimmune diabetes [547364]
N-0861 Drug Info Discontinued in Phase 3 Cardiac disease [545445]
Tecadenoson Drug Info Discontinued in Phase 3 Atrial fibrillation; Cardiac arrhythmias [540960], [546828]
BRL-61063 Drug Info Discontinued in Phase 2 Allergy [545780]
FK-352 Drug Info Discontinued in Phase 2 Hypertension [545925]
FK-453 Drug Info Discontinued in Phase 2 Renal failure [540974], [544923]
FK-838 Drug Info Discontinued in Phase 2 Hypertension [545873]
GW-493838 Drug Info Discontinued in Phase 2 Neuropathic pain [536374]
GR-79236 Drug Info Discontinued in Phase 1 Diabetes [540251], [544895]
SDZ-WAG-994 Drug Info Discontinued in Phase 1 Hypertension [545500]
ARISTEROMYCIN Drug Info Terminated Discovery agent [546315]
METHYLTHIOADENOSINE Drug Info Terminated Multiple scierosis [544778]
METRIFUDIL Drug Info Terminated Discovery agent [467595], [546171]
ZM-241385 Drug Info Terminated Discovery agent [540649], [546100]
Inhibitor (1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine Drug Info [529774]
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl Drug Info [530590]
(2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine Drug Info [529774]
(9-Methyl-9H-purin-6-yl)-phenyl-amine Drug Info [529774]
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-Diethyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info [533446]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione Drug Info [533429]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Drug Info [533429]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info [526958]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info [533339]
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]
2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info [530035]
2,6,8-triphenyl-9H-purine Drug Info [528192]
2,6-bis(4-tolyl)-9H-purine Drug Info [528192]
2,6-dimethyl-8-ethyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-9H-purine Drug Info [528192]
2,6-Diphenyl-pyrimidin-4-ylamine Drug Info [529299]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info [528673]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [529313]
2-(2''-indolylethyloxy)adenosine Drug Info [528748]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine Drug Info [529255]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-indolylethyloxy)adenosine Drug Info [528748]
2-(3''-pyrrolylethyloxy)adenosine Drug Info [528748]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [527933]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info [528192]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info [527933]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info [528684]
2-(4-methoxyphenyl)-6-phenyl-9H-purine Drug Info [528192]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [529313]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info [528684]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Drug Info [530966]
2-(6-Cyclopentylamino-purin-9-yl)-ethanol Drug Info [529774]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info [528684]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile Drug Info [529602]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile Drug Info [529602]
2-Amino-4,6-diphenyl-nicotinonitrile Drug Info [529602]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile Drug Info [529299]
2-Amino-4,6-diphenyl-pyrimidine Drug Info [529299]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Drug Info [529602]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile Drug Info [529602]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile Drug Info [529602]
2-amino-6-phenyl-4-p-tolylnicotinonitrile Drug Info [528434]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile Drug Info [529602]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide Drug Info [529421]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Drug Info [528559]
2-chloro-2'-C-methyl-tecadenoson Drug Info [529098]
2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-chloro-N6-cyclopentyladenosine Drug Info [529098]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info [530590]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethynyl-N6-methoxyadenosine Drug Info [528684]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info [528969]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info [528969]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info [528969]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info [528969]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info [530590]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info [528969]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info [528969]
2-phenylpropoxyadenosine Drug Info [528748]
2-tolyl-6-phenyl-9H-purine Drug Info [528192]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info [528684]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info [528684]
3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Drug Info [529313]
3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol Drug Info [527683]
3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol Drug Info [527683]
3-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info [533542]
3-noradamantyl-1,3-dipropylxanthine Drug Info [528544]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine Drug Info [528434]
4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine Drug Info [529858]
4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info [529421]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info [529419]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile Drug Info [529299]
4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine Drug Info [525857]
4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Drug Info [526099]
4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info [529305]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Drug Info [528673]
6-(furan-2-yl)-9H-purin-2-amine Drug Info [529858]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Drug Info [528748]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info [528748]
7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline Drug Info [530768]
7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol Drug Info [527090]
7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol Drug Info [527090]
7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol Drug Info [527090]
7-Methyl-2-propyl-[1,8]naphthyridin-4-ol Drug Info [527090]
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-(but-3-enyl)-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-cyclohexyl-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-phenylethyl-9H-adenine Drug Info [530014]
8-Bromo-9-propyl-9H-adenine Drug Info [530014]
8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine Drug Info [528192]
8-PHENYL THEOPHYLLINE Drug Info [530590]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Drug Info [533940]
8-Phenyl-3,7-dihydro-purine-2,6-dione Drug Info [533940]
8-propyl-2,6-diphenyl-9H-purine Drug Info [528192]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info [529421]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info [529421]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info [529421]
9-Allyl-8-bromo-9H-adenine Drug Info [530014]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine Drug Info [529421]
9-Benzyl-8-bromo-9H-adenine Drug Info [530014]
9-Cyclobutyl-9H-adenine Drug Info [530014]
9-Cyclopentyl-9H-adenine Drug Info [529774]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info [526104]
9-Ethyl-9H-adenine Drug Info [530014]
9-Isopropyl-9H-adenine Drug Info [530014]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine Drug Info [527823]
9-Methyl-9H-adenine Drug Info [527040]
9-Phenyl-9H-purin-6-ylamine Drug Info [529774]
9-Propyl-9H-adenine Drug Info [530014]
A-987306 Drug Info [529789]
Anthoptilide C Drug Info [525744]
ARISTEROMYCIN Drug Info [525783]
BRL-61063 Drug Info [533908]
CIRSIMARIN Drug Info [534416]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info [527647]
Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine Drug Info [529774]
Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine Drug Info [529774]
Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine Drug Info [529774]
Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine Drug Info [529774]
Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine Drug Info [529774]
Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine Drug Info [529774]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info [530752]
FR-166124 Drug Info [525562]
GNF-PF-2224 Drug Info [530672]
GNF-PF-2700 Drug Info [530966]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Drug Info [527331]
ISOGUANOSINE Drug Info [551229]
KF-17837 Drug Info [525962]
Kuanoniamine D Drug Info [534583]
L-249313 Drug Info [525962]
LUF-5417 Drug Info [530752]
LUF-5433 Drug Info [530752]
LUF-5735 Drug Info [527331]
LUF-5737 Drug Info [527331]
LUF-5764 Drug Info [527331]
LUF-5767 Drug Info [527331]
LUF-5816 Drug Info [528673]
LUF-5853 Drug Info [529299]
LUF-5956 Drug Info [528192]
LUF-5957 Drug Info [528192]
LUF-5962 Drug Info [528192]
LUF-5978 Drug Info [528673]
LUF-5980 Drug Info [528673]
LUF-5981 Drug Info [528673]
LUF-6258 Drug Info [530808]
METHYLTHIOADENOSINE Drug Info [527040]
METRIFUDIL Drug Info [525578]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine Drug Info [527647]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [527647]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [527647]
N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)acetamide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)benzamide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info [527331]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info [530694]
N-(4,5-diphenylpyrimidin-2-yl)acetamide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)benzamide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info [527331]
N-(4-Phenyl-thiazol-2-yl)-benzamide Drug Info [526099]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info [530752]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info [530035]
N6-CYCLOPENTYLADENOSINE Drug Info [529098]
N6-methoxy-2-phenylethynyladenosine Drug Info [528684]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Drug Info [528684]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info [528684]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine Drug Info [529183]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine Drug Info [529183]
NECA Drug Info [533449]
OSIP-339391 Drug Info [530966]
P-IODOAMPHETAMINE Drug Info [526824]
PD-115199 Drug Info [527717]
PD-81723 Drug Info [529655]
Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide Drug Info [527331]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol Drug Info [529418]
Phenyl-(9-phenyl-9H-purin-6-yl)-amine Drug Info [529774]
PSB-0788 Drug Info [530243]
PSB-1115 Drug Info [530243]
PSB-601 Drug Info [530243]
R-N6-(phenylisopropyl)adenosine Drug Info [528748]
SB-298 Drug Info [530243]
SCH-442416 Drug Info [525917]
SCH-63390 Drug Info [534646]
ST-1535 Drug Info [527823]
Tonapofylline Drug Info [530752]
VCP-28 Drug Info [530849]
VUF-8507 Drug Info [525784]
ZM-241385 Drug Info [530372]
Agonist (R)-PIA Drug Info [534553]
(R,S)-PHPNECA Drug Info [526375]
(S)-PIA Drug Info [533981]
2-chloroadenosine Drug Info [534823]
5-Cl-5-deoxy-(+/-)-ENBA Drug Info [530035]
BAY 60-6583 Drug Info [528950]
Capadenoson Drug Info [529810]
CP608,039 Drug Info [528068]
DTI-0009 (oral) Drug Info [531316], [531357]
GR-79236 Drug Info [526609]
GS 9667 Drug Info [532240]
HEMADO Drug Info [528546]
INO-8875 Drug Info [532076]
LUF5831 Drug Info [527992]
MRS5151 Drug Info [529435]
N(6)-cyclohexyladenosine Drug Info [534039]
PENECA Drug Info [526375]
SDZ-WAG-994 Drug Info [533841]
SELODENOSON Drug Info [531316], [531357], [551871]
TCPA Drug Info [526590]
Tecadenoson Drug Info [535721], [551534]
[3H]CCPA Drug Info [534553]
Antagonist 8-cyclopentyltheophylline Drug Info [534757]
Apaxifylline Drug Info [545800]
AS100 Drug Info [527796]
AS70 Drug Info [527796]
AS99 Drug Info [527796]
ATL802 Drug Info [525731]
Caffeine Drug Info [535951], [536302]
CPFPX Drug Info [526448]
CSC Drug Info [534056]
CVT-124 Drug Info [535721], [551534]
FK-352 Drug Info [527956]
flavone Drug Info [534145]
FR194921 Drug Info [527203]
isobutylmethylxanthine Drug Info [533744]
KF26777 Drug Info [526356]
MRE 2029F20 Drug Info [526981]
MRE 3008F20 Drug Info [528068]
MRS1041 Drug Info [534145]
MRS1042 Drug Info [534145]
MRS1062 Drug Info [534145]
MRS1065 Drug Info [534145]
MRS1066 Drug Info [534145]
MRS1084 Drug Info [534145]
MRS1086 Drug Info [534145]
MRS1093 Drug Info [534145]
MRS1132 Drug Info [534145]
MRS1191 Drug Info [543488]
MRS1523 Drug Info [543488]
MRS923 Drug Info [534145]
MRS928 Drug Info [534145]
N-0861 Drug Info [527141]
PD-116,948 Drug Info [535393], [537069], [537747]
PSB-10 Drug Info [526502]
PSB-11 Drug Info [526502]
PSB36 Drug Info [526852]
PSB603 Drug Info [530243]
Rolofylline Drug Info [537064]
sakuranetin Drug Info [534145]
SLV320 Drug Info [537065]
VUF5574 Drug Info [534717]
WRC-0571 Drug Info [534124]
xanthine amine congener Drug Info [533744]
[3H]DPCPX Drug Info [526188]
Modulator AMP-579 Drug Info [527148]
BAY 1067197 Drug Info [551527]
BG-9928 Drug Info
FK-453 Drug Info
FK-838 Drug Info
GW-493838 Drug Info [529810]
L-97-1 intravenous Drug Info [543488]
Paeoniflorin Drug Info [543488]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cGMP-PKG signaling pathway
cAMP signaling pathway
Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
Morphine addiction
NetPath Pathway TCR Signaling Pathway
RANKL Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Reactome Adenosine P1 receptors
G alpha (i) signalling events
WikiPathways Nucleotide GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 467595(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: 426).
Ref 521520ClinicalTrials.gov (NCT00040001) Safety and Efficacy Study of an A1-Adenosine Receptor Agonist to Slow Heart Rate in Atrial Fibrillation. U.S. National Institutes of Health.
Ref 522117ClinicalTrials.gov (NCT00531193) Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers. U.S. National Institutes of Health.
Ref 522175ClinicalTrials.gov (NCT00568945) Study to Investigate the Effect of the A1 Agonist Capadenoson on Ventricular HR in Patients With Persistent or Permanent Atrial Fibrillation.. U.S. National Institutes of Health.
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 523044ClinicalTrials.gov (NCT01123785) A Dose-Escalation Study Designed to Evaluate the Tolerability, Safety, Pharmacokinetics (PK), and Efficacy of Chronic Topical Ocular Application of INO-8875 in AdultsWith Ocular Hypertension or Primary Open-Angle Glaucoma. U.S. National Institutes of Health.
Ref 536372Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536949Fatigue: an overview. Am Fam Physician. 2008 Nov 15;78(10):1173-9.
Ref 537064Association between the PDE4D gene and ischemic stroke in Han Chinese population. Clin Sci (Lond). 2009 Feb 5.
Ref 537065Role 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.
Ref 540245(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: 3281).
Ref 540246(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: 3283).
Ref 540251(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: 3288).
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 540664(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: 407).
Ref 540960(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: 5592).
Ref 540961(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: 5593).
Ref 540972(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: 5604).
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 540974(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: 5606).
Ref 544253Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May; 1808(5): 1290-1308.
Ref 544358Xanthines as Adenosine Receptor Antagonists. Handb Exp Pharmacol. 2011; (200): 10.1007/978-3-642-13443-2_6.
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 544895Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001436)
Ref 544923Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001559)
Ref 545445Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003285)
Ref 545500Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003507)
Ref 545780Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004678)
Ref 545873Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005145)
Ref 545925Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005374)
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 546171Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006749)
Ref 546315Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007402)
Ref 546828Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010504)
Ref 547364Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015498)
Ref 547637Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018030)
Ref 549353Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035637)
Ref 525562Bioorg 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.
Ref 525578J Med Chem. 1999 Sep 9;42(18):3463-77.N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects.
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 525744J Nat Prod. 2000 Mar;63(3):318-21.Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.
Ref 525783J Med Chem. 2000 Jun 1;43(11):2196-203.Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Ref 525784J Med Chem. 2000 Jun 1;43(11):2227-38.Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Ref 525857J Med Chem. 2000 Jul 27;43(15):2814-23.A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.
Ref 525917J 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.
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 526099Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Ref 526104Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
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 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 5265022-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56.
Ref 526590N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem. 2003 Apr 10;46(8):1492-503.
Ref 526609Effect of the adenosine A1 receptor agonist GR79236 on trigeminal nociception with blink reflex recordings in healthy human subjects. Cephalalgia. 2003 May;23(4):287-92.
Ref 526824J 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.
Ref 526852Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66. Epub 2003 Oct 16.
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 527090J Med Chem. 2004 Jun 3;47(12):3019-31.Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
Ref 527141N-0861 selectively antagonizes adenosine A1 receptors in vivo. Eur J Pharmacol. 1992 May 27;216(1):9-16.
Ref 527148Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53. Epub 2004 Jul 22.
Ref 527203Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52. Epub 2004 Sep 4.
Ref 527331J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Ref 527647J Med Chem. 2005 Jul 28;48(15):4910-8."Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Ref 527683Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors.
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 527933J Med Chem. 2005 Dec 29;48(26):8253-60.2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
Ref 527956Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006 Mar;69(5):877-83.
Ref 527992Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist. Br J Pharmacol. 2006 Mar;147(5):533-41.
Ref 528068Nat Rev Drug Discov. 2006 Mar;5(3):247-64.Adenosine receptors as therapeutic targets.
Ref 528192J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Ref 528434Bioorg Med Chem Lett. 2006 Dec 1;16(23):5993-7. Epub 2006 Sep 12.Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches.
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 528559J Med Chem. 2006 Dec 14;49(25):7373-83.2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 528684J Med Chem. 2007 Mar 22;50(6):1222-30. Epub 2007 Feb 20.N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
Ref 528748J 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.
Ref 528950Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71. Epub 2007 May 24.
Ref 528969J Med Chem. 2007 Aug 23;50(17):4061-74. Epub 2007 Aug 1.New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
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 529183Eur J Med Chem. 2008 Aug;43(8):1639-47. Epub 2007 Oct 24.N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.
Ref 529255J Med Chem. 2008 Feb 14;51(3):400-6. Epub 2008 Jan 12.Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Ref 529299Bioorg 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.
Ref 529305Bioorg Med Chem. 2008 Apr 1;16(7):3825-30. Epub 2008 Jan 30.Synthesis of eudistomin D analogues and its effects on adenosine receptors.
Ref 529313J Med Chem. 2008 Mar 27;51(6):1764-70. Epub 2008 Feb 13.Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Ref 529418Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9. Epub 2008 Mar 30.Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.
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 529421Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9. Epub 2008 Mar 30.Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidinesand 6-arylpurines.
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 529655J 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 enhancersof the A1 adenosine receptor.
Ref 529774J Med Chem. 1991 Sep;34(9):2877-82.N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.
Ref 529789J 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.
Ref 529810A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
Ref 529858J Med Chem. 2009 Jan 8;52(1):33-47.Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
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 530372J 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.
Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 530672Eur 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.
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 530808J Med Chem. 2010 Apr 22;53(8):3028-37.Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.
Ref 530849Bioorg 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.
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 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531316Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
Ref 531357International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev. 2011 Mar;63(1):1-34.
Ref 532076INO-8875, a highly selective A1 adenosine receptor agonist: evaluation of chronotropic, dromotropic, and hemodynamic effects in rats. J Pharmacol Exp Ther. 2013 Jan;344(1):59-67.
Ref 532240Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92.
Ref 533339J Med Chem. 1989 Jun;32(6):1231-7.Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
Ref 533429J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
Ref 533446J Med Chem. 1988 Apr;31(4):745-51.125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
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 533542J Med Chem. 1982 Mar;25(3):197-207.Adenosine receptors: targets for future drugs.
Ref 533744Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor. J Biol Chem. 1994 Dec 23;269(51):32077-84.
Ref 533841The cardiac effects of a novel A1-adenosine receptor agonist in guinea pig isolated heart. J Pharmacol Exp Ther. 1994 Dec;271(3):1371-82.
Ref 533908J Med Chem. 1994 Feb 18;37(4):476-85.Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Ref 533940J Med Chem. 1993 Oct 29;36(22):3341-9.Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Ref 533981A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem. 1994 Jan 28;269(4):2373-6.
Ref 534039Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.
Ref 534056Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem. 1993 May 14;36(10):1333-42.
Ref 534124Characterization of 8-(N-methylisopropyl)amino-N6-(5'-endohydroxy- endonorbornyl)-9-methyladenine (WRC-0571), a highly potent and selective, non-xanthine antagonist of A1 adenosine receptors. J Pharmacol Exp Ther. 1996 Feb;276(2):490-9.
Ref 534145J Med Chem. 1996 Jun 7;39(12):2293-301.Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Ref 534416J Nat Prod. 1997 Jun;60(6):638-41.Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.
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 534583J Nat Prod. 1998 Feb;61(2):301-5.Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp.
Ref 534646J 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.
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 534757Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochem Pharmacol. 1998 Dec 1;56(11):1437-45.
Ref 534823Identification of the adenine binding site of the human A1 adenosine receptor. J Biol Chem. 1999 Feb 5;274(6):3617-21.
Ref 535393Minoxidil-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.
Ref 535721Adenosine receptors and cardiovascular disease: the adenosine-1 receptor (A1) and A1 selective ligands. Cardiovasc Toxicol. 2003;3(1):71-88.
Ref 535951Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
Ref 536302Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51.
Ref 537064Association between the PDE4D gene and ischemic stroke in Han Chinese population. Clin Sci (Lond). 2009 Feb 5.
Ref 537065Role 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.
Ref 537069Influence 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.
Ref 537747Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. Mol Pharmacol. 1987 Mar;31(3):247-52.
Ref 543488(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: 18).
Ref 545800Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
Ref 551229High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
Ref 551527Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.
Ref 551534CV Therapeutics. Company report from CV Therapeutics, Inc. CV Therapeutics. 2009.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.