Target Information
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 | Acute and chronic heart failure [ICD9: 428; ICD10: I50] | ||||
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] | |||||
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] | |||||
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78] | |||||
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] | |||||
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 521520 | ClinicalTrials.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 522117 | ClinicalTrials.gov (NCT00531193) Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
Ref 522175 | ClinicalTrials.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 522369 | ClinicalTrials.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 523044 | ClinicalTrials.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 536372 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | ||||
Ref 537064 | Association between the PDE4D gene and ischemic stroke in Han Chinese population. Clin Sci (Lond). 2009 Feb 5. | ||||
Ref 537065 | Role 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 544253 | Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May; 1808(5): 1290-1308. | ||||
Ref 544358 | Xanthines as Adenosine Receptor Antagonists. Handb Exp Pharmacol. 2011; (200): 10.1007/978-3-642-13443-2_6. | ||||
Ref 544778 | 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 544895 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001436) | ||||
Ref 544923 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001559) | ||||
Ref 545445 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003285) | ||||
Ref 545500 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003507) | ||||
Ref 545780 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004678) | ||||
Ref 545873 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005145) | ||||
Ref 545925 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005374) | ||||
Ref 546031 | 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 546100 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006356) | ||||
Ref 546171 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006749) | ||||
Ref 546315 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007402) | ||||
Ref 546828 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010504) | ||||
Ref 547364 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015498) | ||||
Ref 525562 | Bioorg 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 525578 | J Med Chem. 1999 Sep 9;42(18):3463-77.N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. | ||||
Ref 525731 | 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 525744 | J Nat Prod. 2000 Mar;63(3):318-21.Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali. | ||||
Ref 525783 | J Med Chem. 2000 Jun 1;43(11):2196-203.Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. | ||||
Ref 525784 | J Med Chem. 2000 Jun 1;43(11):2227-38.Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. | ||||
Ref 525857 | J 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 525917 | J 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 525962 | J 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 526099 | Bioorg 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 526104 | Bioorg 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 526188 | 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 526332 | J 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 526356 | 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 526375 | 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 526448 | 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 526502 | 2-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 526590 | N6-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 526609 | Effect 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 526824 | J 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 526852 | Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66. Epub 2003 Oct 16. | ||||
Ref 526958 | J 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 526981 | 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 527040 | J 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 527090 | J 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 527141 | N-0861 selectively antagonizes adenosine A1 receptors in vivo. Eur J Pharmacol. 1992 May 27;216(1):9-16. | ||||
Ref 527148 | Adenosine 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 527203 | Pharmacological 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 527331 | J 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 527647 | J 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 527683 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors. | ||||
Ref 527717 | J 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 527796 | Pharmacological 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 527823 | J 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 527933 | J 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 527956 | Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006 Mar;69(5):877-83. | ||||
Ref 527992 | Allosteric 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 528192 | J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. | ||||
Ref 528434 | Bioorg 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 528544 | J 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 528559 | J 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 528673 | J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. | ||||
Ref 528684 | J 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 528748 | J 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 528950 | Protein 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 528969 | J 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 529098 | Bioorg 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 529183 | Eur 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 529255 | J 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 529299 | Bioorg 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 529305 | Bioorg 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 529313 | J 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 529418 | Bioorg 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 529419 | Bioorg 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 529421 | Bioorg 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 529435 | 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 529602 | J 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 529655 | J 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 529774 | J Med Chem. 1991 Sep;34(9):2877-82.N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor. | ||||
Ref 529789 | J 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 529810 | A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10. | ||||
Ref 529858 | J 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 530014 | Bioorg 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 530035 | J 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 530243 | J 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 530372 | J 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 530590 | J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. | ||||
Ref 530672 | Eur 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 530694 | Bioorg 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 530752 | Bioorg 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 530768 | Bioorg 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 530808 | J Med Chem. 2010 Apr 22;53(8):3028-37.Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. | ||||
Ref 530849 | Bioorg 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 530966 | Eur 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 531079 | J 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 531316 | Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308. | ||||
Ref 531357 | International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev. 2011 Mar;63(1):1-34. | ||||
Ref 532076 | INO-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 532240 | Reduction 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 533339 | J 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 533429 | J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. | ||||
Ref 533446 | J Med Chem. 1988 Apr;31(4):745-51.125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors. | ||||
Ref 533449 | J Med Chem. 1988 Jun;31(6):1179-83.Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. | ||||
Ref 533744 | Species 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 533841 | The 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 533908 | J Med Chem. 1994 Feb 18;37(4):476-85.Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. | ||||
Ref 533940 | J 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 533981 | A 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 534039 | Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100. | ||||
Ref 534056 | Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem. 1993 May 14;36(10):1333-42. | ||||
Ref 534124 | Characterization 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 534145 | J Med Chem. 1996 Jun 7;39(12):2293-301.Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. | ||||
Ref 534416 | J Nat Prod. 1997 Jun;60(6):638-41.Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. | ||||
Ref 534553 | 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 534583 | J Nat Prod. 1998 Feb;61(2):301-5.Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. | ||||
Ref 534646 | J 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 534717 | J Med Chem. 1998 Oct 8;41(21):3987-93.A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. | ||||
Ref 534757 | Thermodynamics 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 534823 | Identification of the adenine binding site of the human A1 adenosine receptor. J Biol Chem. 1999 Feb 5;274(6):3617-21. | ||||
Ref 535393 | Minoxidil-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 535721 | Adenosine receptors and cardiovascular disease: the adenosine-1 receptor (A1) and A1 selective ligands. Cardiovasc Toxicol. 2003;3(1):71-88. | ||||
Ref 535951 | Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72. | ||||
Ref 536302 | Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51. | ||||
Ref 537064 | Association between the PDE4D gene and ischemic stroke in Han Chinese population. Clin Sci (Lond). 2009 Feb 5. | ||||
Ref 537065 | Role 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 537069 | Influence 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 537747 | Potent 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 545800 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779) | ||||
Ref 551229 | High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.