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Adenosine receptor A2b
An adenosine receptor A2b that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29275]
Synonyms
Research
Bioassay Publications (126)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 9 (7.14) | 18.7374 |
1990's | 12 (9.52) | 18.2507 |
2000's | 43 (34.13) | 29.6817 |
2010's | 47 (37.30) | 24.3611 |
2020's | 15 (11.90) | 2.80 |
Compounds (104)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
9-ethyladenine | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
1,3-diethyl-8-phenylxanthine | Homo sapiens (human) | Ki | 0.0620 | 1 | 1 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | IC50 | 0.0234 | 2 | 2 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 0.5857 | 18 | 18 |
1,3-dipropyl-8-(4-sulfophenyl)xanthine | Homo sapiens (human) | Ki | 2.7300 | 5 | 5 |
enprofylline | Homo sapiens (human) | Ki | 35.1271 | 7 | 7 |
5-(n,n-hexamethylene)amiloride | Homo sapiens (human) | IC50 | 0.2700 | 1 | 1 |
7-(2-chloroethyl)theophylline | Homo sapiens (human) | Ki | 1.3900 | 1 | 1 |
etofylline | Homo sapiens (human) | Ki | 17.3000 | 2 | 2 |
8-(4-sulfophenyl)theophylline | Homo sapiens (human) | Ki | 2.8980 | 5 | 5 |
8-cyclopentyl-1,3-dimethylxanthine | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
8-phenyltheophylline | Homo sapiens (human) | IC50 | 0.3125 | 2 | 2 |
8-phenyltheophylline | Homo sapiens (human) | Ki | 1.0825 | 4 | 4 |
theophylline | Homo sapiens (human) | Ki | 10.1426 | 19 | 19 |
caffeine | Homo sapiens (human) | Ki | 26.7211 | 19 | 19 |
cgs 15943 | Homo sapiens (human) | IC50 | 0.6304 | 2 | 2 |
cgs 15943 | Homo sapiens (human) | Ki | 0.0262 | 6 | 6 |
denbufylline | Homo sapiens (human) | Ki | 31.5000 | 1 | 1 |
pentoxifylline | Homo sapiens (human) | Ki | 5.1800 | 1 | 1 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 28.2491 | 5 | 5 |
2-chloroadenosine | Homo sapiens (human) | Ki | 23.4500 | 2 | 2 |
9-benzyladenine | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
rolofylline | Homo sapiens (human) | Ki | 0.2666 | 5 | 5 |
aristeromycin | Homo sapiens (human) | Ki | 47.3000 | 1 | 1 |
metrifudil | Homo sapiens (human) | Ki | 0.2835 | 1 | 3 |
acefylline | Homo sapiens (human) | Ki | 27.6000 | 1 | 1 |
9-methyladenine | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
3-methylxanthine | Homo sapiens (human) | Ki | 240.0000 | 1 | 1 |
7-methyladenine | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
9-(2,3-dihydroxypropyl)adenine, (s)-isomer | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
1-methylxanthine | Homo sapiens (human) | Ki | 1.9000 | 1 | 1 |
8-bromoadenine | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | Ki | 1.7000 | 1 | 1 |
3,7-dimethyl-1-propargylxanthine | Homo sapiens (human) | Ki | 4.1300 | 3 | 3 |
bw a1433u | Homo sapiens (human) | Ki | 0.3200 | 2 | 2 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 6.5200 | 2 | 2 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | Ki | 10.2210 | 2 | 2 |
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.1908 | 5 | 5 |
1-propylxanthine | Homo sapiens (human) | Ki | 0.3600 | 1 | 1 |
1,3-dipropyl-8-phenylxanthine | Homo sapiens (human) | Ki | 0.8896 | 5 | 5 |
8-(dicyclopropylmethyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.4300 | 1 | 1 |
kfm 19 | Homo sapiens (human) | Ki | 2.1060 | 2 | 2 |
2-(1-octynyl)adenosine | Homo sapiens (human) | Ki | 0.0399 | 1 | 1 |
1-isoamyl-3-isobutylxanthine | Homo sapiens (human) | Ki | 6.3700 | 2 | 2 |
tecadenoson | Homo sapiens (human) | Ki | 0.2270 | 1 | 1 |
1,3-dipropyl-7-methylxanthine | Homo sapiens (human) | Ki | 4.0500 | 2 | 2 |
bw a522 | Homo sapiens (human) | Ki | 0.7000 | 1 | 1 |
2-hexynyladenosine-5'-n-ethylcarboxamide | Homo sapiens (human) | Ki | 0.0057 | 1 | 1 |
1,3-dipropylxanthine | Homo sapiens (human) | Ki | 4.4017 | 6 | 6 |
zm 241385 | Homo sapiens (human) | IC50 | 0.0646 | 3 | 3 |
zm 241385 | Homo sapiens (human) | Ki | 0.0511 | 12 | 12 |
sch 58261 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 0 |
sch 58261 | Homo sapiens (human) | Ki | 4.4951 | 5 | 5 |
l 734005 | Homo sapiens (human) | IC50 | 1.0400 | 1 | 1 |
8-cyclohexylcaffeine | Homo sapiens (human) | Ki | 1.4301 | 3 | 3 |
5'-methylthioadenosine | Homo sapiens (human) | Ki | 11.0500 | 2 | 2 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 0.7926 | 10 | 12 |
roflumilast | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
wr-142,490 | Homo sapiens (human) | Ki | 7.0720 | 1 | 1 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | Ki | 7.8810 | 3 | 3 |
4-(2-furanyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxylic acid ethyl ester | Homo sapiens (human) | Ki | 0.6082 | 2 | 2 |
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
mrs 1523 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
mre 3008-f20 | Homo sapiens (human) | Ki | 2.0707 | 6 | 6 |
istradefylline | Homo sapiens (human) | Ki | 7.6571 | 7 | 7 |
osip 339391 | Homo sapiens (human) | Ki | 0.0005 | 5 | 5 |
psb 1115 | Homo sapiens (human) | Ki | 0.0932 | 7 | 7 |
8-(3-chlorostyryl)caffeine | Homo sapiens (human) | Ki | 4.6000 | 2 | 2 |
isoalloxazine | Homo sapiens (human) | Ki | 0.0038 | 1 | 1 |
ciproxifan | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
bw a1433 | Homo sapiens (human) | Ki | 0.0600 | 2 | 2 |
fk 453 | Homo sapiens (human) | IC50 | 0.9800 | 1 | 1 |
kf 17837 | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
mrs 1754 | Homo sapiens (human) | IC50 | 0.0320 | 1 | 0 |
mrs 1754 | Homo sapiens (human) | Ki | 0.0025 | 15 | 15 |
binodenoson | Homo sapiens (human) | Ki | 220.0000 | 2 | 2 |
st 1535 | Homo sapiens (human) | Ki | 0.3521 | 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 | 1.3500 | 4 | 4 |
sch 442416 | Homo sapiens (human) | Ki | 10.0000 | 3 | 3 |
cvt-6883 | Homo sapiens (human) | Ki | 0.0174 | 3 | 3 |
tozadenant | Homo sapiens (human) | Ki | 2.1333 | 3 | 3 |
psb 36 | Homo sapiens (human) | Ki | 0.1870 | 1 | 1 |
v 2006 | Homo sapiens (human) | Ki | 0.0630 | 2 | 2 |
psb603 | Homo sapiens (human) | IC50 | 0.0052 | 4 | 4 |
psb603 | Homo sapiens (human) | Ki | 0.0009 | 2 | 2 |
psb 11 | Homo sapiens (human) | Ki | 3.7000 | 1 | 1 |
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) | IC50 | 0.0380 | 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 | 0.0055 | 10 | 10 |
luf 5834 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
cgs 15943 | Homo sapiens (human) | Kd | 0.0100 | 1 | 1 |
6-phenyl-1,3,5-triazine-2,4-diamine | Homo sapiens (human) | Kd | 107.0000 | 1 | 1 |
2-chloroadenosine | Homo sapiens (human) | EC50 | 0.0251 | 1 | 1 |
adenosine | Homo sapiens (human) | EC50 | 18.9935 | 9 | 9 |
isoguanosine | Homo sapiens (human) | EC50 | 0.0794 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | EC50 | 1.3150 | 2 | 2 |
5'-n-methylcarboxamideadenosine | Homo sapiens (human) | EC50 | 23.3500 | 2 | 2 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | EC50 | 72.4436 | 1 | 1 |
salvinorin a | Homo sapiens (human) | EC50 | 0.0038 | 1 | 2 |
2-(1-octynyl)adenosine | Homo sapiens (human) | EC50 | 0.6810 | 1 | 1 |
1-deazaadenosine | Homo sapiens (human) | EC50 | 18.0000 | 1 | 1 |
2-hexynyladenosine-5'-n-ethylcarboxamide | Homo sapiens (human) | EC50 | 0.1050 | 1 | 1 |
regadenoson | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | EC50 | 1.4737 | 25 | 26 |
1-deaza-2-chloro-n(6)-cyclopentyladenosine | Homo sapiens (human) | EC50 | 28.0000 | 1 | 1 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | EC50 | 1.1316 | 2 | 2 |
adenosine-5'-(N-propyl)carboxamide | Homo sapiens (human) | EC50 | 29.0000 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | EC50 | 1,150.5951 | 6 | 6 |
mrs 1754 | Homo sapiens (human) | EC50 | 33.8159 | 2 | 2 |
cv 1808 | Homo sapiens (human) | EC50 | 0.0182 | 1 | 1 |
binodenoson | Homo sapiens (human) | EC50 | 50.0001 | 2 | 2 |
2-(2-(4-chlorophenyl)ethoxy)adenosine | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
n(6)-(2,2-diphenylethyl)adenosine | Homo sapiens (human) | EC50 | 0.4850 | 1 | 1 |
cgs 24012 | Homo sapiens (human) | EC50 | 0.0004 | 1 | 1 |
n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | EC50 | 2.7800 | 2 | 2 |
mrs 3558 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
bay 60-6583 | Homo sapiens (human) | EC50 | 0.0310 | 1 | 1 |
v 2006 | Homo sapiens (human) | Kd | 0.0316 | 1 | 1 |
psb603 | Homo sapiens (human) | Kd | 0.0005 | 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) | Kd | 0.0016 | 1 | 1 |
luf 5834 | Homo sapiens (human) | EC50 | 0.0120 | 1 | 1 |
luf 5834 | Homo sapiens (human) | Kd | 3.0700 | 1 | 1 |
Drugs with Other Measurements
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
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
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
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
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
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
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
Development of spin-labeled probes for adenosine receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
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
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
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
Molecular modeling and molecular dynamics simulation of the human A2B adenosine receptor. The study of the possible binding modes of the A2B receptor antagonists.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
AEuropean journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
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
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
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
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
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
AEuropean journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
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
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
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
Molecular modeling and molecular dynamics simulation of the human A2B adenosine receptor. The study of the possible binding modes of the A2B receptor antagonists.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:10, 1988
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
[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
Novel non-xanthine antagonist of the AEuropean journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
[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
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
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
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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
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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 (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
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
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
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.Journal of medicinal chemistry, , Volume: 28, Issue:9, 1985
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
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.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
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
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
2-aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
[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
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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
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:6, 1988
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
[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
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
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
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
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
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 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
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.Journal of medicinal chemistry, , Volume: 28, Issue:9, 1985
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:10, 1988
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
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, , 11-12, Volume: 63, Issue:21, 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
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
5,7-Disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazines as pharmacological tools to explore the antagonist selectivity profiles toward adenosine receptors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
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
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
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 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
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
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
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
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
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
[no title available],
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.Journal of medicinal chemistry, , Feb-07, Volume: 35, Issue:3, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Examining the Role of the Linker in Bitopic Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Biological Evaluation of 5'-(ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
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
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
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
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
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
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
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
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
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
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
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
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:6, 1988
N6-substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors.Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
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
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:6, 1988
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.ACS medicinal chemistry letters, , Nov-14, Volume: 4, Issue:11, 2013
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
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
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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
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
[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
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
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Trifluorinated Pyrimidine-Based AJournal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
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
Development of subtype-selective covalent ligands for the adenosine ARSC medicinal chemistry, , Jul-20, Volume: 13, Issue:7, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
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
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Novel non-xanthine antagonist of the AEuropean journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
AEuropean journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
In search for new chemical entities as adenosine receptor ligands: development of agents based on benzo-γ-pyrone skeleton.European journal of medicinal chemistry, , Volume: 54, 2012
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
[no title available],
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
2-(N'-alkylidenehydrazino)adenosines: potent and selective coronary vasodilators.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
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
[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
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
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
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
[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
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
Development of Covalent, Clickable Probes for Adenosine AJournal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
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
AEuropean journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
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
Molecular modeling and molecular dynamics simulation of the human A2B adenosine receptor. The study of the possible binding modes of the A2B receptor antagonists.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
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
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 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 3 target(s):
Target | Category | Definition |
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] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal 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, http://www.iuphar-db.org, Wikipedia:GPCR] |
Located In
This protein is located in 4 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] |
Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
presynapse | cellular component | The part of a synapse that is part of the presynaptic cell. [GOC:dos] |
glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 1 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] |
Involved In
This protein is involved in 15 target(s):
Target | Category | Definition |
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] |
positive regulation of chronic inflammatory response to non-antigenic stimulus | biological process | Any process that activates or increases the frequency, rate, or extent of a chronic inflammatory response to a non-antigenic stimulus. [GOC:add] |
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] |
activation of adenylate cyclase activity | biological process | Any process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai] |
positive regulation of vascular endothelial growth factor production | biological process | Any process that increases or activates the frequency, rate, or extent of production of vascular endothelial growth factor. [GOC:BHF, GOC:rl] |
positive regulation of cGMP-mediated signaling | biological process | Any process that increases the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, GOC:dph, GOC:tb] |
cGMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic GMP (cGMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |
positive regulation of chemokine production | biological process | Any process that activates or increases the frequency, rate, or extent of chemokine production. [GOC:mah] |
positive regulation of interleukin-6 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-6 production. [GOC:mah] |
mast cell degranulation | biological process | The regulated exocytosis of secretory granules containing preformed mediators such as histamine, serotonin, and neutral proteases by a mast cell. [ISBN:0781735149] |
positive regulation of mast cell degranulation | biological process | Any process that activates or increases the frequency, rate or extent of mast cell degranulation. [ISBN:0781735149] |
relaxation of vascular associated smooth muscle | biological process | A negative regulation of smooth muscle contraction resulting in relaxation of vascular smooth muscle. The relaxation is mediated by a decrease in the phosphorylation state of myosin light chain. This can be achieved by removal of calcium from the cytoplasm to the sarcoplasmic reticulum lumen through the action of Ca2+ ATPases leading to a decrease myosin light chain kinase activity, and through calcium-independent pathways leading to a increase in myosin light chain phosphatase activity. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:dph, GOC:rph, GOC:TermGenie, PMID:15867178, PMID:19996365, PMID:27389411] |
presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
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] |