Page last updated: 2024-08-07 16:22:28

Adenosine receptor A2b

An adenosine receptor A2b that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29275]

Synonyms

Research

Bioassay Publications (126)

TimeframeStudies on this Protein(%)All Drugs %
pre-19909 (7.14)18.7374
1990's12 (9.52)18.2507
2000's43 (34.13)29.6817
2010's47 (37.30)24.3611
2020's15 (11.90)2.80

Compounds (104)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
9-ethyladenineHomo sapiens (human)Ki30.000011
1,3-diethyl-8-phenylxanthineHomo sapiens (human)Ki0.062011
1,3-dipropyl-8-cyclopentylxanthineHomo sapiens (human)IC500.023422
1,3-dipropyl-8-cyclopentylxanthineHomo sapiens (human)Ki0.58571818
1,3-dipropyl-8-(4-sulfophenyl)xanthineHomo sapiens (human)Ki2.730055
enprofyllineHomo sapiens (human)Ki35.127177
5-(n,n-hexamethylene)amilorideHomo sapiens (human)IC500.270011
7-(2-chloroethyl)theophyllineHomo sapiens (human)Ki1.390011
etofyllineHomo sapiens (human)Ki17.300022
8-(4-sulfophenyl)theophyllineHomo sapiens (human)Ki2.898055
8-cyclopentyl-1,3-dimethylxanthineHomo sapiens (human)Ki0.140011
8-phenyltheophyllineHomo sapiens (human)IC500.312522
8-phenyltheophyllineHomo sapiens (human)Ki1.082544
theophyllineHomo sapiens (human)Ki10.14261919
caffeineHomo sapiens (human)Ki26.72111919
cgs 15943Homo sapiens (human)IC500.630422
cgs 15943Homo sapiens (human)Ki0.026266
denbufyllineHomo sapiens (human)Ki31.500011
pentoxifyllineHomo sapiens (human)Ki5.180011
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthineHomo sapiens (human)Ki28.249155
2-chloroadenosineHomo sapiens (human)Ki23.450022
9-benzyladenineHomo sapiens (human)Ki30.000011
rolofyllineHomo sapiens (human)Ki0.266655
aristeromycinHomo sapiens (human)Ki47.300011
metrifudilHomo sapiens (human)Ki0.283513
acefyllineHomo sapiens (human)Ki27.600011
9-methyladenineHomo sapiens (human)Ki30.000011
3-methylxanthineHomo sapiens (human)Ki240.000011
7-methyladenineHomo sapiens (human)Ki30.000011
9-(2,3-dihydroxypropyl)adenine, (s)-isomerHomo sapiens (human)Ki30.000011
1-methylxanthineHomo sapiens (human)Ki1.900011
8-bromoadenineHomo sapiens (human)Ki30.000011
phenylisopropyladenosineHomo sapiens (human)Ki1.700011
3,7-dimethyl-1-propargylxanthineHomo sapiens (human)Ki4.130033
bw a1433uHomo sapiens (human)Ki0.320022
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosineHomo sapiens (human)Ki6.520022
2-chloro-n(6)cyclopentyladenosineHomo sapiens (human)Ki10.221022
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthineHomo sapiens (human)Ki0.190855
1-propylxanthineHomo sapiens (human)Ki0.360011
1,3-dipropyl-8-phenylxanthineHomo sapiens (human)Ki0.889655
8-(dicyclopropylmethyl)-1,3-dipropylxanthineHomo sapiens (human)Ki0.430011
kfm 19Homo sapiens (human)Ki2.106022
2-(1-octynyl)adenosineHomo sapiens (human)Ki0.039911
1-isoamyl-3-isobutylxanthineHomo sapiens (human)Ki6.370022
tecadenosonHomo sapiens (human)Ki0.227011
1,3-dipropyl-7-methylxanthineHomo sapiens (human)Ki4.050022
bw a522Homo sapiens (human)Ki0.700011
2-hexynyladenosine-5'-n-ethylcarboxamideHomo sapiens (human)Ki0.005711
1,3-dipropylxanthineHomo sapiens (human)Ki4.401766
zm 241385Homo sapiens (human)IC500.064633
zm 241385Homo sapiens (human)Ki0.05111212
sch 58261Homo sapiens (human)IC502.000010
sch 58261Homo sapiens (human)Ki4.495155
l 734005Homo sapiens (human)IC501.040011
8-cyclohexylcaffeineHomo sapiens (human)Ki1.430133
5'-methylthioadenosineHomo sapiens (human)Ki11.050022
adenosine-5'-(n-ethylcarboxamide)Homo sapiens (human)Ki0.79261012
roflumilastHomo sapiens (human)IC501.000011
wr-142,490Homo sapiens (human)Ki7.072011
n(6)-cyclopentyladenosineHomo sapiens (human)Ki7.881033
4-(2-furanyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxylic acid ethyl esterHomo sapiens (human)Ki0.608222
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamideHomo sapiens (human)Ki10.000011
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosineHomo sapiens (human)Ki10.000022
mrs 1523Homo sapiens (human)Ki10.000011
mre 3008-f20Homo sapiens (human)Ki2.070766
istradefyllineHomo sapiens (human)Ki7.657177
osip 339391Homo sapiens (human)Ki0.000555
psb 1115Homo sapiens (human)Ki0.093277
8-(3-chlorostyryl)caffeineHomo sapiens (human)Ki4.600022
isoalloxazineHomo sapiens (human)Ki0.003811
ciproxifanHomo sapiens (human)Ki1.000011
bw a1433Homo sapiens (human)Ki0.060022
fk 453Homo sapiens (human)IC500.980011
kf 17837Homo sapiens (human)IC501.500011
mrs 1754Homo sapiens (human)IC500.032010
mrs 1754Homo sapiens (human)Ki0.00251515
binodenosonHomo sapiens (human)Ki220.000022
st 1535Homo sapiens (human)Ki0.352122
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-amineHomo sapiens (human)Ki1.350044
sch 442416Homo sapiens (human)Ki10.000033
cvt-6883Homo sapiens (human)Ki0.017433
tozadenantHomo sapiens (human)Ki2.133333
psb 36Homo sapiens (human)Ki0.187011
v 2006Homo sapiens (human)Ki0.063022
psb603Homo sapiens (human)IC500.005244
psb603Homo sapiens (human)Ki0.000922
psb 11Homo sapiens (human)Ki3.700011
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)-acetamideHomo sapiens (human)IC500.038022
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)-acetamideHomo sapiens (human)Ki0.00551010
luf 5834Homo sapiens (human)Ki0.001011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
1,3-dipropyl-8-cyclopentylxanthineHomo sapiens (human)EC501.000011
cgs 15943Homo sapiens (human)Kd0.010011
6-phenyl-1,3,5-triazine-2,4-diamineHomo sapiens (human)Kd107.000011
2-chloroadenosineHomo sapiens (human)EC500.025111
adenosineHomo sapiens (human)EC5018.993599
isoguanosineHomo sapiens (human)EC500.079411
phenylisopropyladenosineHomo sapiens (human)EC501.315022
5'-n-methylcarboxamideadenosineHomo sapiens (human)EC5023.350022
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosineHomo sapiens (human)EC5011.000011
2-chloro-n(6)cyclopentyladenosineHomo sapiens (human)EC5072.443611
salvinorin aHomo sapiens (human)EC500.003812
2-(1-octynyl)adenosineHomo sapiens (human)EC500.681011
1-deazaadenosineHomo sapiens (human)EC5018.000011
2-hexynyladenosine-5'-n-ethylcarboxamideHomo sapiens (human)EC500.105011
regadenosonHomo sapiens (human)EC5010.000011
adenosine-5'-(n-ethylcarboxamide)Homo sapiens (human)EC501.47372526
1-deaza-2-chloro-n(6)-cyclopentyladenosineHomo sapiens (human)EC5028.000011
n(6)-cyclopentyladenosineHomo sapiens (human)EC501.131622
adenosine-5'-(N-propyl)carboxamideHomo sapiens (human)EC5029.000011
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosineHomo sapiens (human)EC501,150.595166
mrs 1754Homo sapiens (human)EC5033.815922
cv 1808Homo sapiens (human)EC500.018211
binodenosonHomo sapiens (human)EC5050.000122
2-(2-(4-chlorophenyl)ethoxy)adenosineHomo sapiens (human)EC5010.000011
n(6)-(2,2-diphenylethyl)adenosineHomo sapiens (human)EC500.485011
cgs 24012Homo sapiens (human)EC500.000411
n-cyclopropyl adenosine-5'-carboxamideHomo sapiens (human)EC502.780022
mrs 3558Homo sapiens (human)EC5010.000011
bay 60-6583Homo sapiens (human)EC500.031011
v 2006Homo sapiens (human)Kd0.031611
psb603Homo sapiens (human)Kd0.000522
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)-acetamideHomo sapiens (human)Kd0.001611
luf 5834Homo sapiens (human)EC500.012011
luf 5834Homo sapiens (human)Kd3.070011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
1,3-diethyl-8-phenylxanthineHomo sapiens (human)Kb0.210011
8-phenyltheophyllineHomo sapiens (human)Affinity constant0.200011
8-phenyltheophyllineHomo sapiens (human)Kb1.900011
theophyllineHomo sapiens (human)Affinity constant10.000011
caffeineHomo sapiens (human)Affinity constant30.000011
1-methyl-3-isobutylxanthineHomo sapiens (human)Affinity constant5.000011
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthineHomo sapiens (human)Kb0.025011
2-chloroadenosineHomo sapiens (human)Affinity constant5.000011
adenosineHomo sapiens (human)Affinity constant15.000022
n(6)-benzyladenosineHomo sapiens (human)Affinity constant80.000011
phenylisopropyladenosineHomo sapiens (human)Affinity constant30.000011
n(6)-phenyladenosineHomo sapiens (human)Affinity constant50.000011
n-methyladenosineHomo sapiens (human)Affinity constant80.000011
bw a1433uHomo sapiens (human)Kb0.110011
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthineHomo sapiens (human)Kb2.400011
1,3-dipropyl-8-phenylxanthineHomo sapiens (human)Kb1.200022
1,3-dipropylxanthineHomo sapiens (human)Kb2.700011
zm 241385Homo sapiens (human)Activity0.028011
zm 241385Homo sapiens (human)INH0.028011
5'-methylthioadenosineHomo sapiens (human)Affinity constant10.000011
adenosine-5'-(n-ethylcarboxamide)Homo sapiens (human)Affinity constant2.000011
n-(1-methyl-2-phenylethyl)adenosine, (s)-isomerHomo sapiens (human)Affinity constant100.000011
n(6)-cyclohexyladenosineHomo sapiens (human)Affinity constant30.000011
sch 442416Homo sapiens (human)INH10.000011
cvt-6883Homo sapiens (human)Kb0.006011
v 2006Homo sapiens (human)KA0.031011

Enables

This protein enables 3 target(s):

TargetCategoryDefinition
G protein-coupled adenosine receptor activitymolecular functionCombining 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 bindingmolecular functionBinding to a protein. [GOC:go_curators]
G protein-coupled receptor activitymolecular functionCombining 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):

TargetCategoryDefinition
plasma membranecellular componentThe 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 synapsecellular componentA synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689]
presynapsecellular componentThe part of a synapse that is part of the presynaptic cell. [GOC:dos]
glutamatergic synapsecellular componentA synapse that uses glutamate as a neurotransmitter. [GOC:dos]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe 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):

TargetCategoryDefinition
G protein-coupled adenosine receptor signaling pathwaybiological processThe 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 stimulusbiological processAny 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 pathwaybiological processThe 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 activitybiological processAny process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai]
positive regulation of vascular endothelial growth factor productionbiological processAny 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 signalingbiological processAny process that increases the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, GOC:dph, GOC:tb]
cGMP-mediated signalingbiological processAn 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 productionbiological processAny process that activates or increases the frequency, rate, or extent of chemokine production. [GOC:mah]
positive regulation of interleukin-6 productionbiological processAny process that activates or increases the frequency, rate, or extent of interleukin-6 production. [GOC:mah]
mast cell degranulationbiological processThe 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 degranulationbiological processAny process that activates or increases the frequency, rate or extent of mast cell degranulation. [ISBN:0781735149]
relaxation of vascular associated smooth musclebiological processA 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 transmissionbiological processAny process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos]
adenylate cyclase-activating G protein-coupled receptor signaling pathwaybiological processA 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]
vasodilationbiological processAn 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]