Page last updated: 2024-08-07 16:25:23
Adenosine receptor A1
An adenosine receptor A1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30542]
Synonyms
Research
Bioassay Publications (214)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 1 (0.47) | 18.7374 |
1990's | 12 (5.61) | 18.2507 |
2000's | 100 (46.73) | 29.6817 |
2010's | 78 (36.45) | 24.3611 |
2020's | 23 (10.75) | 2.80 |
Compounds (117)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
9-ethyladenine | Homo sapiens (human) | Ki | 7.4000 | 1 | 1 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | IC50 | 0.0083 | 9 | 9 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 20,737.6376 | 46 | 48 |
enprofylline | Homo sapiens (human) | Ki | 43.0000 | 2 | 2 |
8-phenyltheophylline | Homo sapiens (human) | IC50 | 1.3400 | 1 | 1 |
theophylline | Homo sapiens (human) | IC50 | 17.1040 | 1 | 0 |
theophylline | Homo sapiens (human) | Ki | 6.6399 | 18 | 17 |
caffeine | Homo sapiens (human) | Ki | 35.4333 | 15 | 15 |
cgs 15943 | Homo sapiens (human) | Ki | 0.0044 | 2 | 2 |
clotrimazole | Homo sapiens (human) | IC50 | 13.4200 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 7.8300 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 16.9240 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 9.8720 | 1 | 0 |
nocodazole | Homo sapiens (human) | IC50 | 50.3300 | 1 | 0 |
nocodazole | Homo sapiens (human) | Ki | 29.4330 | 1 | 0 |
miconazole | Homo sapiens (human) | IC50 | 12.5190 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 7.3030 | 1 | 0 |
n 0840 | Homo sapiens (human) | Ki | 1.1330 | 2 | 2 |
nifedipine | Homo sapiens (human) | IC50 | 7.7010 | 1 | 0 |
nifedipine | Homo sapiens (human) | Ki | 4.4920 | 1 | 0 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 3.6486 | 8 | 8 |
triiodothyronine | Homo sapiens (human) | IC50 | 0.4109 | 1 | 0 |
triiodothyronine | Homo sapiens (human) | Ki | 0.2397 | 1 | 0 |
2-chloroadenosine | Homo sapiens (human) | Ki | 0.0075 | 3 | 3 |
azacitidine | Homo sapiens (human) | Ki | 2.8450 | 1 | 2 |
alpha-naphthoflavone | Homo sapiens (human) | IC50 | 1.1325 | 1 | 0 |
alpha-naphthoflavone | Homo sapiens (human) | Ki | 0.6606 | 1 | 0 |
9-benzyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
3-deazaadenosine | Homo sapiens (human) | Ki | 0.4610 | 1 | 1 |
ribavirin | Homo sapiens (human) | Ki | 7.4100 | 2 | 2 |
mefloquine | Homo sapiens (human) | Ki | 14.0440 | 1 | 1 |
lovastatin | Homo sapiens (human) | IC50 | 26.7200 | 1 | 0 |
lovastatin | Homo sapiens (human) | Ki | 15.5860 | 1 | 0 |
adenosine | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
adenosine | Homo sapiens (human) | Ki | 0.8128 | 1 | 1 |
rolofylline | Homo sapiens (human) | Ki | 0.0006 | 5 | 5 |
metrifudil | Homo sapiens (human) | Ki | 0.2224 | 2 | 4 |
9-methyladenine | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
7-methyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
9-(2,3-dihydroxypropyl)adenine, (s)-isomer | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
8-bromoadenine | Homo sapiens (human) | Ki | 33.0000 | 1 | 1 |
5-methylcytidine | Homo sapiens (human) | Ki | 8.0200 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | IC50 | 0.8300 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | Ki | 0.1647 | 3 | 3 |
5'-n-methylcarboxamideadenosine | Homo sapiens (human) | Ki | 0.0367 | 1 | 1 |
n-methyladenosine | Homo sapiens (human) | Ki | 6.0000 | 1 | 1 |
2'-o-methyladenosine | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 0.1908 | 15 | 15 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | IC50 | 0.0009 | 2 | 2 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | Ki | 0.0062 | 9 | 9 |
adenosine amine congener | Homo sapiens (human) | Ki | 0.0104 | 1 | 1 |
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.1750 | 1 | 1 |
7-bromoeudistomine d | Homo sapiens (human) | Ki | 7.3700 | 2 | 2 |
kfm 19 | Homo sapiens (human) | Ki | 0.0105 | 1 | 1 |
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine | Homo sapiens (human) | IC50 | 0.0112 | 3 | 3 |
tecadenoson | Homo sapiens (human) | IC50 | 0.0082 | 1 | 1 |
tecadenoson | Homo sapiens (human) | Ki | 0.0234 | 3 | 3 |
1-deazaadenosine | Homo sapiens (human) | Ki | 0.4373 | 1 | 3 |
sb 203580 | Homo sapiens (human) | IC50 | 2.9500 | 1 | 0 |
sb 203580 | Homo sapiens (human) | Ki | 1.7210 | 1 | 0 |
zm 241385 | Homo sapiens (human) | Ki | 16,022.9053 | 18 | 18 |
sch 58261 | Homo sapiens (human) | Ki | 0.4137 | 9 | 9 |
2-(4-morpholinoanilino)-6-cyclohexylaminopurine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
regadenoson | Homo sapiens (human) | Ki | 5,493.4100 | 3 | 3 |
mrs 1067 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
mrs 1220 | Homo sapiens (human) | IC50 | 0.0479 | 1 | 1 |
mrs 1220 | Homo sapiens (human) | Ki | 0.1112 | 3 | 3 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | IC50 | 0.0007 | 2 | 2 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 0.1571 | 34 | 38 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 2.8560 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 1.6660 | 1 | 0 |
roflumilast | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
wr-142,490 | Homo sapiens (human) | Ki | 0.2513 | 3 | 3 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | IC50 | 0.0027 | 1 | 1 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | Ki | 0.0069 | 11 | 11 |
tamoxifen | Homo sapiens (human) | IC50 | 23.7670 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 13.8640 | 1 | 0 |
5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxy-2-oxolanecarboxamide | Homo sapiens (human) | Ki | 0.0140 | 1 | 1 |
fk 838 | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 0.4861 | 23 | 25 |
adenosine-5'-(N-propyl)carboxamide | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | Ki | 1.3899 | 9 | 9 |
mrs 1523 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
genistein | Homo sapiens (human) | IC50 | 19.9040 | 1 | 0 |
genistein | Homo sapiens (human) | Ki | 11.6110 | 1 | 0 |
naloxone | Homo sapiens (human) | Ki | 50.0000 | 1 | 1 |
mre 3008-f20 | Homo sapiens (human) | Ki | 1.1731 | 8 | 8 |
istradefylline | Homo sapiens (human) | Ki | 1.9050 | 13 | 13 |
osip 339391 | Homo sapiens (human) | Ki | 0.1747 | 3 | 3 |
psb 1115 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
8-(3-chlorostyryl)caffeine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
isoalloxazine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
7-chloro-4-hydroxy-2-phenyl-1,8-naphthyridine | Homo sapiens (human) | Ki | 0.3234 | 3 | 3 |
ciproxifan | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
bw a1433 | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
fk 453 | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
kf 17837 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
gw 1929 | Homo sapiens (human) | IC50 | 14.9660 | 1 | 0 |
gw 1929 | Homo sapiens (human) | Ki | 8.7300 | 1 | 0 |
mrs 1754 | Homo sapiens (human) | Ki | 0.3817 | 9 | 9 |
binodenoson | Homo sapiens (human) | Ki | 32.0563 | 3 | 3 |
atl 146e | Homo sapiens (human) | Ki | 0.0770 | 1 | 1 |
rwj 68354 | Homo sapiens (human) | IC50 | 0.8870 | 1 | 0 |
rwj 68354 | Homo sapiens (human) | Ki | 0.5180 | 1 | 0 |
st 1535 | Homo sapiens (human) | Ki | 0.0807 | 4 | 4 |
n-((1s,trans)-2-hydroxycyclopentyl)adenosine | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
2-(2-(4-chlorophenyl)ethoxy)adenosine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
bay-68-4986 | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 2 | 2 |
2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine | Homo sapiens (human) | Ki | 0.8433 | 5 | 6 |
vuf 8504 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
n(6)-(2,2-diphenylethyl)adenosine | Homo sapiens (human) | Ki | 0.0500 | 3 | 3 |
n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 0.0019 | 2 | 2 |
sch 442416 | Homo sapiens (human) | Ki | 0.5567 | 4 | 4 |
mrs 3558 | Homo sapiens (human) | Ki | 0.2600 | 5 | 5 |
cvt-6883 | Homo sapiens (human) | Ki | 4.6267 | 3 | 3 |
ino-8875 | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
tozadenant | Homo sapiens (human) | Ki | 1.9533 | 6 | 6 |
psb 36 | Homo sapiens (human) | Ki | 0.0007 | 2 | 2 |
lj 529 | Homo sapiens (human) | Ki | 0.1930 | 8 | 8 |
a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
v 2006 | Homo sapiens (human) | Ki | 0.0680 | 2 | 2 |
psb603 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
sildenafil | Homo sapiens (human) | IC50 | 1.4930 | 1 | 0 |
sildenafil | Homo sapiens (human) | Ki | 0.8710 | 1 | 0 |
psb 11 | Homo sapiens (human) | Ki | 1.6400 | 2 | 2 |
n-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-1-methyl-1h-pyrazol-3-yloxy)-acetamide | Homo sapiens (human) | Ki | 0.2069 | 7 | 7 |
luf 5834 | Homo sapiens (human) | Ki | 0.0026 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | EC50 | 0.4674 | 2 | 2 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Kd | 0.0031 | 3 | 2 |
theophylline | Homo sapiens (human) | Kd | 12.0000 | 1 | 1 |
caffeine | Homo sapiens (human) | Kd | 45.0000 | 1 | 1 |
cgs 15943 | Homo sapiens (human) | Kd | 0.0754 | 1 | 0 |
1-methyl-3-isobutylxanthine | Homo sapiens (human) | Kd | 5.9000 | 1 | 1 |
tinoridine | Homo sapiens (human) | EC50 | 10.3000 | 1 | 1 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Kd | 0.0147 | 1 | 0 |
adenosine monophosphate | Homo sapiens (human) | EC50 | 0.5000 | 1 | 1 |
6-phenyl-1,3,5-triazine-2,4-diamine | Homo sapiens (human) | Kd | 2.2100 | 1 | 1 |
adenosine | Homo sapiens (human) | EC50 | 0.6588 | 8 | 8 |
adenosine | Homo sapiens (human) | Kd | 0.2951 | 1 | 1 |
rolofylline | Homo sapiens (human) | Kd | 0.0114 | 1 | 0 |
phenylisopropyladenosine | Homo sapiens (human) | EC50 | 1.2000 | 1 | 1 |
2'-o-methyladenosine | Homo sapiens (human) | EC50 | 3.0000 | 1 | 1 |
pd 81723 | Homo sapiens (human) | EC50 | 8.1730 | 5 | 6 |
pd 81723 | Homo sapiens (human) | Kd | 0.0012 | 3 | 3 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | EC50 | 0.0727 | 3 | 3 |
8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine | Homo sapiens (human) | Kd | 0.0005 | 3 | 4 |
zm 241385 | Homo sapiens (human) | Kd | 0.0615 | 3 | 3 |
mrs 1220 | Homo sapiens (human) | EC50 | 0.0479 | 1 | 1 |
mrs 1220 | Homo sapiens (human) | Kd | 0.0158 | 1 | 1 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | EC50 | 0.0740 | 17 | 17 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Kd | 0.8143 | 7 | 7 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | EC50 | 0.0052 | 2 | 2 |
sch-202676 | Homo sapiens (human) | EC50 | 2.8000 | 1 | 1 |
5-amino-3-(4-methoxyphenyl)-4-oxo-1-thieno[3,4-d]pyridazinecarboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 4.3000 | 1 | 1 |
5-amino-3-(4-methoxyphenyl)-4-oxo-1-thieno[3,4-d]pyridazinecarboxylic acid ethyl ester | Homo sapiens (human) | Kd | 0.1995 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | EC50 | 215.7980 | 3 | 3 |
mrs 1754 | Homo sapiens (human) | EC50 | 67.6083 | 1 | 1 |
5-amino-4-oxo-3-phenyl-1-thieno[3,4-d]pyridazinecarboxylic acid | Homo sapiens (human) | EC50 | 9.8000 | 1 | 1 |
n-((1s,trans)-2-hydroxycyclopentyl)adenosine | Homo sapiens (human) | EC50 | 0.0059 | 1 | 1 |
bay-68-4986 | Homo sapiens (human) | EC50 | 0.0006 | 2 | 2 |
psb 36 | Homo sapiens (human) | Kd | 0.0006 | 1 | 0 |
v 2006 | Homo sapiens (human) | Kd | 0.1000 | 1 | 1 |
luf 5834 | Homo sapiens (human) | Kd | 0.0046 | 1 | 1 |
Drugs with Other Measurements
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
[no title available]ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine AJournal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
Identification of new potent AEuropean journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent AJournal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
[no title available]Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine AChemical biology & drug design, , Volume: 88, Issue:5, 2016
Further studies on pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective human A1 adenosine receptor antagonists.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis of a series of 8-(substituted-phenyl)xanthines and a study on the effects of substitution pattern of phenyl substituents on affinity for adenosine A(1) and A(2A) receptors.European journal of medicinal chemistry, , Volume: 44, Issue:5, 2009
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.Bioorganic & medicinal chemistry, , Apr-01, Volume: 17, Issue:7, 2009
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
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.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.Journal of medicinal chemistry, , Jan-11, Volume: 50, Issue:1, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
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.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
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.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 9, Issue:16, 1999
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.Journal of medicinal chemistry, , Volume: 33, Issue:7, 1990
[no title available],
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Structure-Based Optimization of Coumarin hAJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
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.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.Journal of natural products, , Volume: 63, Issue:3, 2000
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
[no title available],
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
[no title available]Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.Journal of natural products, , Volume: 63, Issue:3, 2000
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
[no title available],
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Exploring Non-orthosteric Interactions with a Series of Potent and Selective AACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
[no title available]MedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
[no title available],
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists.ACS chemical biology, , 10-21, Volume: 11, Issue:10, 2016
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 20, Issue:14, 2010
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
[no title available],
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.Journal of medicinal chemistry, , Apr-19, Volume: 50, Issue:8, 2007
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.Journal of natural products, , Volume: 69, Issue:3, 2006
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.Journal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards AEuropean journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Discovery of first-in-class multi-target adenosine AEuropean journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.Journal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
New irreversible adenosine A(1) antagonists based on FSCPX.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A(1)-adenosine receptor.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors.Journal of medicinal chemistry, , Aug-19, Volume: 37, Issue:17, 1994
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Structure-activity relationships of adenosines with heterocyclic N6-substituents.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 17, Issue:24, 2007
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Identification of new potent AEuropean journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent AJournal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Trifluorinated Pyrimidine-Based AJournal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Structure-activity relationship studies and pharmacological characterization of NEuropean journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent AJournal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
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.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Synthesis of a series of 8-(substituted-phenyl)xanthines and a study on the effects of substitution pattern of phenyl substituents on affinity for adenosine A(1) and A(2A) receptors.European journal of medicinal chemistry, , Volume: 44, Issue:5, 2009
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
[no title available],
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 18, Issue:7, 2010
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
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.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as AEuropean journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
[no title available]ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Examining the Role of the Linker in Bitopic Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
[no title available]ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine AJournal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
Discovery of first-in-class multi-target adenosine AEuropean journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
A Structure-Activity Relationship Study of Bitopic NJournal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the AJournal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.ACS medicinal chemistry letters, , Dec-08, Volume: 2, Issue:12, 2011
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.ACS medicinal chemistry letters, , Aug-11, Volume: 2, Issue:8, 2011
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.Journal of medicinal chemistry, , Apr-19, Volume: 50, Issue:8, 2007
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
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.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Structure activity relationship of 2-arylalkynyl-adenine derivatives as human AMedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards AEuropean journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as AEuropean journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.ACS medicinal chemistry letters, , Dec-08, Volume: 2, Issue:12, 2011
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.Bioorganic & medicinal chemistry letters, , Mar-17, Volume: 8, Issue:6, 1998
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.Bioorganic & medicinal chemistry letters, , Feb-07, Volume: 10, Issue:3, 2000
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 25, Issue:6, 2015
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
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.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.Journal of medicinal chemistry, , Jul-11, Volume: 56, Issue:13, 2013
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Structure activity relationship of 2-arylalkynyl-adenine derivatives as human AMedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Biological Evaluation of 5'-(ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
[no title available]MedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
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.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine AEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine AJournal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
A mild, efficient and alpha-selective glycosidation by using potassium dodecatungstocobaltate trihydrate as catalyst.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Enables
This protein enables 8 target(s):
Target | Category | Definition |
G protein-coupled receptor binding | molecular function | Binding to a G protein-coupled receptor. [GOC:ceb, GOC:dph] |
purine nucleoside binding | molecular function | Binding to a purine nucleoside, a compound consisting of a purine base linked either to ribose or deoxyribose. [GOC:hjd] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
heat shock protein binding | molecular function | Binding to a heat shock protein, a protein synthesized or activated in response to heat shock. [GOC:mah, GOC:vw] |
G-protein beta/gamma-subunit complex binding | molecular function | Binding to a complex of G-protein beta/gamma subunits. [GOC:nln, GOC:vw] |
heterotrimeric G-protein binding | molecular function | Binding to a heterotrimeric G-protein. [GOC:nln] |
protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
G protein-coupled adenosine receptor activity | molecular function | Combining with adenosine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:mah, PMID:9755289] |
Located In
This protein is located in 11 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
axolemma | cellular component | The portion of the plasma membrane surrounding an axon; it is a specialized trilaminar random mosaic of protein molecules floating within a fluid matrix of highly mobile phospholipid molecules, 7-8 nm in thickness. [http://www.medik.sk/clanky/bio_jun.htm, ISBN:0124325653] |
asymmetric synapse | cellular component | A type of synapse occurring between an axon and a dendritic spine or dendritic shaft. Asymmetric synapses, the most abundant synapse type in the central nervous system, involve axons that contain predominantly spherical vesicles and contain a thickened postsynaptic density. Most or all synapses of this type are excitatory. [GOC:dgh, GOC:ef] |
presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
terminal bouton | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal bouton is a specialized region of it. [GOC:dph, GOC:mc, GOC:nln, PMID:10218156, PMID:8409967] |
dendritic spine | cellular component | A small, membranous protrusion from a dendrite that forms a postsynaptic compartment, typically receiving input from a single presynapse. They function as partially isolated biochemical and an electrical compartments. Spine morphology is variable:they can be thin, stubby, mushroom, or branched, with a continuum of intermediate morphologies. They typically terminate in a bulb shape, linked to the dendritic shaft by a restriction. Spine remodeling is though to be involved in synaptic plasticity. [GOC:nln] |
calyx of Held | cellular component | The terminal specialization of a calyciferous axon which forms large synapses in the mammalian auditory central nervous system. [NIF_Subcellular:sao1684283879, PMID:11823805] |
postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
presynaptic active zone | cellular component | A specialized region of the plasma membrane and cell cortex of a presynaptic neuron; encompasses a region of the plasma membrane where synaptic vesicles dock and fuse, and a specialized cortical cytoskeletal matrix. [GOC:dh, GOC:dl, GOC:ef, GOC:jid, GOC:pr, PMID:3152289] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 51 target(s):
Target | Category | Definition |
temperature homeostasis | biological process | A homeostatic process in which an organism modulates its internal body temperature. [GOC:jl] |
response to hypoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
G protein-coupled adenosine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a receptor binding to extracellular adenosine and transmitting the signal to a heterotrimeric G-protein complex to initiate a change in cell activity. [GOC:dph] |
regulation of respiratory gaseous exchange by nervous system process | biological process | A process carried out by the nervous system that is required for the proper control of respiratory gaseous exchange. This process occurs in the respiratory center of the brain in vertebrates. [GOC:dph, GOC:tb, PMID:12458206] |
negative regulation of acute inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of an acute inflammatory response. [GOC:add] |
negative regulation of leukocyte migration | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of leukocyte migration. [GOC:add] |
positive regulation of peptide secretion | biological process | Any process that activates or increases the frequency, rate, or extent of peptide secretion. [GOC:add] |
positive regulation of systemic arterial blood pressure | biological process | The process that increases the force with which blood travels through the systemic arterial circulatory system. [GOC:mtg_cardio] |
negative regulation of systemic arterial blood pressure | biological process | The process that reduces the force with which blood travels through the systemic arterial circulatory system. [GOC:mtg_cardio] |
regulation of glomerular filtration | biological process | Any process that modulates the frequency, rate or extent of glomerular filtration. Glomerular filtration is the process in which blood is filtered by the glomerulus into the renal tubule. [GOC:mtg_cardio] |
protein targeting to membrane | biological process | The process of directing proteins towards a membrane, usually using signals contained within the protein. [GOC:curators] |
phagocytosis | biological process | A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732] |
inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
nervous system development | biological process | The process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh] |
negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
response to inorganic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an inorganic substance stimulus. [GOC:sm] |
negative regulation of glutamate secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of glutamate. [GOC:ef] |
response to purine-containing compound | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a purine-containing compound stimulus. [GOC:ef] |
lipid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of lipids, compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. [GOC:go_curators] |
negative regulation of synaptic transmission, GABAergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
positive regulation of nucleoside transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a nucleoside into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:mah] |
negative regulation of neurotrophin production | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of production of a neurotrophin. [GOC:mah] |
positive regulation of protein dephosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of removal of phosphate groups from a protein. [GOC:bf] |
vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
negative regulation of circadian sleep/wake cycle, non-REM sleep | biological process | Any process that stops, prevents or reduces the duration or quality of non-rapid eye movement (NREM) sleep. [GOC:jl] |
negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
positive regulation of potassium ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of potassium ions (K+) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
negative regulation of hormone secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of a hormone from a cell. [GOC:ai] |
cognition | biological process | The operation of the mind by which an organism becomes aware of objects of thought or perception; it includes the mental activities associated with thinking, learning, and memory. [ISBN:0721619908] |
leukocyte migration | biological process | The movement of a leukocyte within or between different tissues and organs of the body. [GOC:add, ISBN:0781735149, PMID:14680625, PMID:14708592, PMID:7507411, PMID:8600538] |
detection of temperature stimulus involved in sensory perception of pain | biological process | The series of events involved in the perception of pain in which a temperature stimulus is received and converted into a molecular signal. [GOC:ai, GOC:dos] |
negative regulation of lipid catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
positive regulation of lipid catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
regulation of sensory perception of pain | biological process | Any process that modulates the frequency, rate or extent of the sensory perception of pain, the series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. [GOC:ai] |
negative regulation of synaptic transmission, glutamatergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
fatty acid homeostasis | biological process | Any process involved in the maintenance of an internal steady state of fatty acid within an organism or cell. [GOC:BHF, GOC:rl] |
excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
long-term synaptic depression | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the decrease in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
mucus secretion | biological process | The regulated release of mucus by the mucosa. Mucus is a viscous slimy secretion consisting of mucins and various inorganic salts dissolved in water, with suspended epithelial cells and leukocytes. The mucosa, or mucous membrane, is the membrane covered with epithelium that lines the tubular organs of the body. Mucins are carbohydrate-rich glycoproteins that have a lubricating and protective function. [GOC:add, ISBN:068340007X, ISBN:0721662544] |
negative regulation of mucus secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of mucus from a cell or a tissue. [GOC:add] |
triglyceride homeostasis | biological process | Any process involved in the maintenance of an internal steady state of triglyceride within an organism or cell. [GOC:BHF, GOC:mah] |
regulation of cardiac muscle cell contraction | biological process | Any process that modulates the frequency, rate or extent of cardiac muscle cell contraction. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11] |
apoptotic signaling pathway | biological process | The series of molecular signals which triggers the apoptotic death of a cell. The pathway starts with reception of a signal, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis] |
regulation of presynaptic cytosolic calcium ion concentration | biological process | Any process that regulates the concentration of calcium in the presynaptic cytosol. [GOC:dos] |
negative regulation of long-term synaptic potentiation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of long-term synaptic potentiation. [GOC:BHF, GOC:TermGenie] |
negative regulation of long-term synaptic depression | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of long term synaptic depression. [GOC:BHF, GOC:TermGenie] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |