Page last updated: 2024-11-04

8-phenyltheophylline

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Description

8-phenyltheophylline: purinergic P1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1922
CHEMBL ID62350
SCHEMBL ID516432
MeSH IDM0091290

Synonyms (65)

Synonym
1,3-dimethyl-8-phenyl-3,7-dihydro-1h-purine-2,6-dione
STL293634
MLS000069624
smr000058251
8-phenyltheophylline
EU-0100917
1,3-dimethyl-8-phenylxanthine, crystalline
1h-purine-2,6-dione, 2,3,6,7-tetrahydro-1,3-dimethyl-8-phenyl-
theophylline, 8-phenyl-
nsc 14127
1h-purine-2,6-dione, 3,7-dihydro-1,3-dimethyl-8-phenyl-
nsc-14127
961-45-5
nsc14127
lopac-p-2278
NCGC00015807-01
PDSP2_000325
LOPAC0_000917
PDSP1_000322
OPREA1_390706
PDSP2_000320
PDSP1_000327
NCGC00094228-01
NCGC00094228-02
1,3-dimethyl-8-phenylxanthine
NCGC00015807-02
P 2278
NCGC00015807-04
CHEMBL62350 ,
8-phenyl-1,3-dimethylxanthine
8-pt
AKOS002153928
1,3-dimethyl-8-phenyl-7h-purine-2,6-dione
cas_1922
bdbm82015
1,3-dimethyl-8-phenyl-3,9-dihydro-purine-2,6-dione
nsc_1922
VU0254233-3
HMS3262H16
1,3-dimethyl-8-phenyl-3,7-dihydro-purine-2,6-dione
CCG-204999
e6m543p3bl ,
unii-e6m543p3bl
NCGC00015807-03
FT-0633195
LP00917
AKOS015905559
SCHEMBL516432
NCGC00261602-01
tox21_500917
mfcd00005582
1h-purine-2,6-dione, 3,9-dihydro-1,3-dimethyl-8-phenyl-
3,9-dihydro-1,3-dimethyl-8-phenyl-1h-purine-2,6-dione
3,7-dihydro-1,3-dimethyl-8-phenyl-1h-purine-2,6-dione
DTXSID90242119
SR-01000076062-1
sr-01000076062
Q4644289
1,3-dimethyl-8-phenyl-1h-purine-2,6(3h,7h)-dione
1,3-dimethyl-8-phenyl-3,9-dihydro-1h-purine-2,6-dione
SDCCGSBI-0050892.P002
NCGC00015807-06
1,3-dimethyl-8-phenyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
CS-0044810
PD015130

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" We conclude that the emetic side effect of xanthine bronchodilators results from the inhibition of one or more forms of PDE rather than from adenosine antagonism."( Mechanism for the emetic side effect of xanthine bronchodilators.
Howell, RE; Kinnier, WJ; Muehsam, WT, 1990
)
0.28

Pharmacokinetics

ExcerptReferenceRelevance
" It is concluded that the pharmacokinetic properties of 8-PT are likely to complicate its use in-vivo."( Pharmacokinetics of 8-phenyltheophylline in the rat.
Bowmer, CJ; Collis, MG; Wormald, A; Yates, MS, 1989
)
0.6

Dosage Studied

8-phenyltheophylline (8-PT) was used to shift the adenosine dose-response curve 12-fold. 8-PT was significantly more potent than Adenosine deaminase. The study also investigated the effects of a known adenosin antagonist, namely, the xanthine derivative 8-phenolsyltheophylli.

ExcerptRelevanceReference
" A2 receptors by N-0861 was evaluated by generating dose-response curves to adenosine-induced bradycardia (A1 effect), and vasodilation in the in situ constant-flow perfused rat hindquarter vasculature (A2 effect)."( N-0861 selectively antagonizes adenosine A1 receptors in vivo.
Barrett, RJ; Droppleman, DA; Wright, KF, 1992
)
0.28
" Dose-response curves to the agonists were similar for both age groups."( Cerebrovascular reactivity to adenosine analogues in 0.6-0.7 gestation and near-term fetal sheep.
Kurth, CD; Wagerle, LC, 1992
)
0.28
" The adenosine receptor antagonist 8-(p-sulphophenyl)theophylline (8-SPT, 50 microM) produced approximately 50 fold shifts of the dose-response curves to adenosine, AMP and AMPPCP, whereas those to ATP, MeSATP and substance P (SP) were unaffected."( A study of the purinoceptors mediating contraction in the rat colon.
Bailey, SJ; Hourani, SM, 1990
)
0.28
" BMA caused "flattening" of the dose-response curves for 86Rb efflux induced by L-PIA, adenosine and carbachol with a significant reduction in response at the highest concentrations of adenosine and carbachol."( 86Rubidium efflux and negative inotropy induced by P1- and muscarinic-receptor agonists in guinea-pig left atria. Effects of potassium channel blockers.
Broadley, KJ; Rothaul, AL; Urquhart, RA, 1991
)
0.28
" Dose-response curves for adenosine and its analogues 5'-N-ethyl-carboxamido-adenosine (NECA), the 2-substituted NECA analogue CGS 21680C, and R- and S-N6-phenyl-isopropyl-adenosine (R- and S-PIA) were obtained after their injection into the hepatic arterial supply."( Adenosine-induced dilatation of the rabbit hepatic arterial bed is mediated by A2-purinoceptors.
Alexander, B; Burnstock, G; Mathie, RT; Ralevic, V, 1991
)
0.28
" Dose-response measurements with tissues from intact or sympathectomized (6-OHDA) animals indicate that the thermogenic effects of low concentrations of ephedrine and also of caffeine are entirely dependent upon the presence of intact sympathetic nerve endings, and thus depend on presynaptic mechanisms."( Peripheral mechanisms of thermogenesis induced by ephedrine and caffeine in brown adipose tissue.
Dulloo, AG; Girardier, L; Seydoux, J, 1991
)
0.28
" This effect of acetate was fully blocked by the adenosine receptor blocker 8-phenyltheophylline (8PT), whereas the dose-response relationship for ethanol was shifted to the right by about 30%."( Central nervous system effects of acetate: contribution to the central effects of ethanol.
Campisi, P; Carmichael, FJ; Crawford, M; Israel, Y; Minhas, K; Orrego, H; Saldivia, V; Sandrin, S, 1991
)
0.51
" In preparations precontracted by a higher concentration of KCl, 40 mM, forskolin produced full relaxation with a shift of the dose-response curve to the right; adenosine did not produce full relaxation."( Vasodilation produced by forskolin compared with that produced by adenosine in rabbit coronary artery.
Fujiwara, M; Hama, T; Hisajima, H; Kurahashi, K; Usui, H,
)
0.13
" The adenosine receptor antagonist 8-phenyltheophylline (10 microM) displaced the dose-response curve for NECA to the right, increasing the EC50 for NECA about one order of magnitude."( Evidence for A2 adenosine receptor-mediated effects on adenylate cyclase activity in rat ovarian membranes.
Billig, H; Rosberg, S, 1988
)
0.55
" ANP produced dose-related coronary vasodilation with a threshold dosage of 2 ng/kg; a dosage of 2 micrograms/kg caused a 27 +/- 4% decrease in coronary vascular resistance."( Effects of atrial natriuretic peptide in the canine coronary circulation.
Bache, RJ; Chen, DG; Dai, XZ; Schwartz, JS, 1988
)
0.27
" Dose-response curves were determined for each drug by administering cumulative doses IV during timeout periods that preceded sequential components of the FI schedule."( Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism.
Spealman, RD, 1988
)
0.27
" Both adenosine deaminase and 8-phenyltheophylline caused a rightward shift of the dose-response curve to intracoronary adenosine; 8-phenyltheophylline was significantly more potent than adenosine deaminase."( Role of adenosine in coronary vasodilation during exercise.
Bache, RJ; Dai, XZ; Homans, DC; Schwartz, JS, 1988
)
0.56
" The study also investigated the effects of a known adenosine antagonist, namely, the xanthine derivative 8-phenyltheophylline, which at concentrations having no intrinsic effect (10(-8) and 10(-7) M) produced a significant shift to the right only for the NECA dose-response curve."( Effects of adenosine and its analogues on porcine basilar arteries: are only A2 receptors involved?
Harper, AM; McBean, DE; Rudolphi, KA, 1988
)
0.49
" Dose-response curves were obtained for the effect of intraportal adenosine infusion on hepatic arterial conductance in doses that did not lead to recirculation and secondary effects on the hepatic artery via altered portal blood flow."( The use of 8-phenyltheophylline as a competitive antagonist of adenosine and an inhibitor of the intrinsic regulatory mechanism of the hepatic artery.
Lautt, WW; Legare, DJ, 1985
)
0.66
" When dose-response relationships could be determined, the adenyl compounds were found to be of similar potency."( Ionic basis of the hyperpolarizing action of adenyl compounds on sinus venosus of the tortoise heart.
Hutter, OF; Rankin, AC, 1984
)
0.27
"05) rightward shift of the dose-response curve for the depressor effects of adenosine (ED50 = 13."( The involvement of ATP-sensitive potassium channels and adenosine in the regulation of coronary flow in the isolated perfused rat heart.
Randall, MD, 1995
)
0.29
" In conclusion, basal interstitial adenosine concentration is at the threshold of a remarkably steep dose-response curve for increasing coronary blood flow."( Quantitative relation between interstitial adenosine concentration and coronary blood flow.
Feigl, EO; Kroll, K; Stepp, DW; Van Bibber, R, 1996
)
0.29
" Dose-response data for both agonists were best represented by two-site models."( A biphasic response to adenosine in the coronary vasculature of the K(+)-arrested perfused rat heart.
Harden, FA; Harrison, GJ; Headrick, J; Jordan, LR; Willis, RJ, 1996
)
0.29
" Adenosine receptor blockade with 8-phenyltheophylline (8-PT) was used to shift the adenosine dose-response curve 12-fold."( Role of adenosine in norepinephrine-induced coronary vasodilation.
Feigl, EO; Kroll, K; Stepp, DW; Van Bibber, R, 1997
)
0.58
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency3.16230.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency3.16230.025120.237639.8107AID886
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency15.84890.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency44.66845.623417.292931.6228AID2323
thioredoxin reductaseRattus norvegicus (Norway rat)Potency2.88920.100020.879379.4328AID588453; AID588456
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.28180.540617.639296.1227AID2364; AID2528
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.07080.00106.000935.4813AID943
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.25120.015812.3113615.5000AID1461
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ReninHomo sapiens (human)Ki0.50000.00001.80787.4000AID195542
Adenosine receptor A3Homo sapiens (human)IC50 (µMol)1.25000.00001.89408.5470AID34425
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)0.27560.00020.552110.0000AID31389; AID31397; AID31399
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.19220.00011.20929.9700AID195542; AID31831; AID31856; AID31887; AID32039; AID32040; AID32177; AID32194; AID32324; AID32487; AID32491; AID32500
Adenosine receptor A1Bos taurus (cattle)IC50 (µMol)1,509,975.00150.00001.09106.7400AID31836; AID31838
Adenosine receptor A1Bos taurus (cattle)Ki0.00310.00000.71316.0000AID31831
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki0.50000.00030.91969.0000AID195542
Adenosine receptor A2aHomo sapiens (human)IC50 (µMol)0.45400.00071.559410.0000AID34081
Adenosine receptor A2aHomo sapiens (human)Ki1.75000.00001.06099.7920AID30797; AID33734
Adenosine receptor A2bHomo sapiens (human)IC50 (µMol)0.31250.00050.30231.5000AID33171; AID33174
Adenosine receptor A2bHomo sapiens (human)Ki1.08250.00021.635210.0000AID30797; AID33176; AID33180; AID33734
Adenosine receptor A2bRattus norvegicus (Norway rat)IC50 (µMol)1.10000.00240.68169.0000AID227793
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki1.25100.00061.353610.0000AID195542; AID30797; AID33579; AID33728; AID33734
Adenosine receptor A1Homo sapiens (human)IC50 (µMol)1.34000.00020.68187.7010AID30301
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki1.21980.00021.494010.0000AID195542; AID30797; AID32862; AID33579; AID33728; AID33734
Adenosine receptor A2aCavia porcellus (domestic guinea pig)Ki0.55000.11002.63858.0000AID30621
Adenosine receptor A1Cavia porcellus (domestic guinea pig)Ki1.60000.00030.45466.9000AID32292
Adenosine receptor A1Gallus gallus (chicken)Ki0.00310.00313.00166.0000AID31831
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A2aHomo sapiens (human)Affinity constant0.20000.20006.028610.0000AID33909
Adenosine receptor A2aHomo sapiens (human)Kb1.90000.00131.08292.7000AID30635
Adenosine receptor A2bHomo sapiens (human)Affinity constant0.20000.20006.028610.0000AID33909
Adenosine receptor A2bHomo sapiens (human)Kb1.90000.00601.08342.7000AID30635
Adenosine receptor A2bRattus norvegicus (Norway rat)Ratio0.85000.00330.82929.6000AID33746
Adenosine receptor A1Homo sapiens (human)Affinity constant0.20000.00301.069110.0000AID30353
Adenosine receptor A2aRattus norvegicus (Norway rat)Ratio0.85000.00330.82309.6000AID33746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (123)

Processvia Protein(s)Taxonomy
kidney developmentReninHomo sapiens (human)
mesonephros developmentReninHomo sapiens (human)
angiotensin maturationReninHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionReninHomo sapiens (human)
proteolysisReninHomo sapiens (human)
regulation of blood pressureReninHomo sapiens (human)
male gonad developmentReninHomo sapiens (human)
hormone-mediated signaling pathwayReninHomo sapiens (human)
response to lipopolysaccharideReninHomo sapiens (human)
response to immobilization stressReninHomo sapiens (human)
drinking behaviorReninHomo sapiens (human)
regulation of MAPK cascadeReninHomo sapiens (human)
cell maturationReninHomo sapiens (human)
amyloid-beta metabolic processReninHomo sapiens (human)
response to cAMPReninHomo sapiens (human)
response to cGMPReninHomo sapiens (human)
cellular response to xenobiotic stimulusReninHomo sapiens (human)
juxtaglomerular apparatus developmentReninHomo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Bos taurus (cattle)
response to purine-containing compoundAdenosine receptor A1Bos taurus (cattle)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulusAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A2bHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
positive regulation of chemokine productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of interleukin-6 productionAdenosine receptor A2bHomo sapiens (human)
mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
positive regulation of mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
relaxation of vascular associated smooth muscleAdenosine receptor A2bHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2bHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
vasodilationAdenosine receptor A2bHomo sapiens (human)
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Gallus gallus (chicken)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Gallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
aspartic-type endopeptidase activityReninHomo sapiens (human)
signaling receptor bindingReninHomo sapiens (human)
insulin-like growth factor receptor bindingReninHomo sapiens (human)
protein bindingReninHomo sapiens (human)
peptidase activityReninHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2bHomo sapiens (human)
protein bindingAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor activityAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
G protein-coupled adenosine receptor activityAdenosine receptor A1Gallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular regionReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
plasma membraneReninHomo sapiens (human)
apical part of cellReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A2bHomo sapiens (human)
presynapseAdenosine receptor A2bHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
plasma membraneAdenosine receptor A1Gallus gallus (chicken)
synapseAdenosine receptor A1Gallus gallus (chicken)
dendriteAdenosine receptor A1Gallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (123)

Assay IDTitleYearJournalArticle
AID191195Oral diuretic activity was measured after oral administration of 1.6 mg/kg to rats(control volume is 1.4+/-0.05)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID174535Serum creatinine concentration measured after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 3.86+/-0.27)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32636Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as radioligand, PCY = log (100000/IC50).1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
AID33752Ratio of A2 to A1.1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID33174Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID33586Binding affinity towards adenosine A2 receptor in rat striatal membranes using N-[3H]-ethyladenosin-5''-uronamide as radioligand1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID194957Percent inhibition of Urea nitrogen by the compound given as ratio of UN value in treated to vehicle treated ones after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 178+/-11.3)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33587Binding affinity against adenosine A2 receptor in rat striatal membranes using N-[3H]-ethyladenosin-5''-uronamide as radioligand in the presence of 50 nM cyclopentyladenosine1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33728Inhibition of binding of [3H]5'-(N-ethylcarbamoyl)-adenosine to adenosine A2 receptor in rat striatal membranes1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
AID189935Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID232222Selectivity for A2 and A1 receptors was evaluated1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
AID190190Urea nitrogen concentration measured after intraperitoneal administration of 10 mg/kg of compound to rats(vehicle 141.3+/-6.6)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30335Log IC50 value was determined against adenosine A1 receptor in rat brain membranes1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID34081Inhibitory activity against cyclic AMP production in rat Adenosine A2A receptor assay2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID32500Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
AID30635Antagonism of NECA-induced stimulation of adenylate cyclase activity in human platelet membranes at A2-adenosine receptor1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.
AID189927Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 6.25 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID31831Displacement of [3H]CPX from adenosine A1 receptor of calf brain cortical membrane1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
AID32868Binding affinity for adenosine A2A receptor using [3H]-NECA in rat brain striatal membranes2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID189937Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 25 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189925Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 25 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID230229Inhibitory selectivity for A2 receptor in rat striatal membranes and A1 receptor in rat cortical membranes1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
AID229822Ratio of antagonism at A2 versus A1 receptors (Ki values)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID30802Ratio of Ki for adenosine A2 and A1 receptors in rat1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
AID188099Effect on urinary excretion potassium and sodium after oral administration of 25 mg/kg to rats(potassium and sodium excretion in control rat is 0.134+/-0.004)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32487Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
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.
AID33734Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via Adenosine A2 receptor in rat PC12 membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
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.
AID32046Binding affinity for adenosine A1 receptor using [3H]PIA in rat brain cortical membrane2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID78489Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID32495Inhibition of [3H]- PIA binding at adenosine A1 receptor on rat cerebral cortex membranes.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.
AID30353Affinity constant for inhibition of A1 receptor control of adenylate cyclase in adipocytes, heart and brain cells1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID35023Binding affinity to the adenosine A2A receptor by displacement of [3H]CGS-21680 in rat brain striatal membrane2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID33441Binding affinity against adenosine A2 receptor in rat striatum by the displacement of [3H]N-ethyladenosine-5''-uronamide(NECA).1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
AID78495Ability to inhibit 2-chloroadenosine (15 uM)-elicited accumulations of cyclic AMP in guinea pig cerebral cortical membranes1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Mesoionic xanthine analogues: antagonists of adenosine receptors.
AID30621Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID31861Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
AID30797Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
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.
AID228357Ratio of Ki at A2 receptor to that of A1 receptor1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID236904Partition coefficient (logP)2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives.
AID31836Binding affinity against bovine brain adenosine A1 receptor by using N6-[3H]- cyclohexyladenosine1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID30301Binding Affinity for Adenosine A1 receptor expressed in CHO-K1 cells compared to [3H]CCPA2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID191202Oral diuretic activity was measured after oral administration of 25 mg/kg to rats(control volume is 0.80+/-0.04)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID34160Inhibition of Adenylate Cyclase in Rat adipocytes1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
AID190350Urea nitrogen concentration measured after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 178+/-11.3)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32177Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID34425Inhibitory activity against cyclic AMP production in human adenosine A3 receptor assay2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID31858Binding affinity against Adenosine A1 receptor by displacing [3H]CHA radioligand in rat brain cortical membrane2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID31397Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
AID31389Antagonism of adenosine A1 receptor assessed from the ability to inhibit binding of [3H]cyclohexyladenosine to rat cerebral cortical membranes1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Mesoionic xanthine analogues: antagonists of adenosine receptors.
AID191352Oral diuretic activity was measured after oral administration of 6.25 mg/kg to rats(control volume is 0.80+/-0.02)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189939Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 6.25 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID31869Binding affinity against adenosine A1 receptor in rat cortex by the displacement of [3H]cyclohexyladenosine (CHA).1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
AID32292Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30176Water solubility of the compound2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID33909Affinity constant for A2 receptor control of adenylate cyclase in adipocytes, heart and brain cells1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID54313log(1000/IC50 determined from bovine brain membrane) expressed as potency1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID188282Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 25 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33580Binding affinity for adenosine A2 receptor using [3H]NECA in rat striatal membrane1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
AID33746Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID33579Binding affinity to A2 adenosine receptor from rat striatal membrane in presence of [3H]5'-(N-ethylcarboximido)-adenosine1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
AID187958Effect on urinary excretion potassium and sodium after oral administration of 1.6 mg/kg to rats(potassium and sodium excretion in control rat is 0.261+/-0.008)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32194Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID31399Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding 1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
AID42825Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID32040Displacement of [3H]CPX from adenosine A1 receptor of rat brain cortical membrane1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
AID33180Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID33435Binding affinity against Adenosine A2 receptor in rat brain membrane, using [3H]-NECA as the radioligand.1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.
AID32324Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
AID33753Ratio of the binding affinities of A2 /A1 receptor1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
AID192514Percent inhibition of Urea nitrogen by the compound given as ratio of UN value in treated to vehicle treated ones fter intraperitoneal administration of 10 mg/kg of compound to rats(vehicle 141.3+/-6.6)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID227793Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID192688Percent inhibition of serum creatinine by the compound given as ratio of Cr value in treated to vehicle treated ones after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 3.86+/-0.27)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32039Binding affinity to A1 adenosine receptor from rat cortical membrane in presence of [3H]R-(phenylisopropyl)-adenosine1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
AID195542Antagonist binding of 2-chloro-[3H]-adenosine to rat brain1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID31856Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes1985Journal of medicinal chemistry, Apr, Volume: 28, Issue:4
1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
AID31390Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as a radioligand1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
AID227036A1 selectivity is the ratio between A2 and A1 receptor1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
AID188407Ratio of sodium ion/potassium ion concentration in urine of rats following 6.25 mg/kg p.o.1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33176Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
AID189923Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID34728Binding affinity for human adenosine A3 receptor using [3H]-PBS-11 in CHO cell membranes; Not determined2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
AID34158Inhibition of adenyl cyclase via P site in adipocytes; Inactive1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Adenosine receptors: targets for future drugs.
AID33171Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
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.
AID192807Percent inhibition of serum creatinine by the compound given as ratio of Cr value in treated to vehicle treated ones fter intraperitoneal administration of 10 mg/kg of compound to rats(vehicle 3.94+/-0.24)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID31838Log IC50 value was determined against adenosine A1 receptor in bovine brain membranes1985Journal of medicinal chemistry, Aug, Volume: 28, Issue:8
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
AID32862Binding affinity for adenosine A2A receptor from rat brain membranes using [3H]CGS-216801993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
AID188248Effect on urinary excretion potassium and sodium after oral administration of 6.25 mg/kg to rats(potassium and sodium excretion in control rat is 0.146+/-0.005)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID174520Serum creatinine concentration measured after intraperitoneal administration of 10 mg/kg of compound to rats(vehicle 3.94+/-0.24)1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33591Binding of Adenosine A2 receptor in whole rat brain membrane using [3H]CHA as a Radioligand1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
AID32491Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
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.
AID188280Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID31887Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID493017Wombat Data for BeliefDocking1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (502)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990173 (34.46)18.7374
1990's260 (51.79)18.2507
2000's55 (10.96)29.6817
2010's8 (1.59)24.3611
2020's6 (1.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.03

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.03 (24.57)
Research Supply Index6.25 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews6 (1.16%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other512 (98.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]