Page last updated: 2024-12-08

bw a522

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

BW A522: blocks adenosine A3 receptor-mediated hypotensive responses in rats [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID163889
CHEMBL ID355370
MeSH IDM0229944

Synonyms (20)

Synonym
gtpl446
PDSP2_001184
PDSP1_001200
bw a522
L001152
CHEMBL355370 ,
112533-64-9
2-[4-[3-[(4-amino-3-iodophenyl)methyl]-2,6-dioxo-1-propyl-7h-purin-8-yl]phenoxy]acetic acid
i-abopx
bw-a522
3-(3-iodo-4-aminobenzyl)-8-(4-oxyacetate)-1-propylxanthine
acetic acid, (4-(3-((4-amino-3-iodophenyl)methyl)-2,3,6,7-tetrahydro-2,6-dioxo-1-propyl-1h-purin-8-yl)phenoxy)-
nsc_163889
bdbm82558
cas_163889
DTXSID40150098
2-(4-{3-[(4-amino-3-iodophenyl)methyl]-2,6-dioxo-1-propyl-2,3,6,9-tetrahydro-1h-purin-8-yl}phenoxy)acetic acid
3-(4-amino-3-iodobenzyl)-8-[4-[[[carboxy]methyl]oxy]-phenyl]-1-propylxanthine
Q27078012
2-(4-(3-(4-amino-3-iodobenzyl)-2,6-dioxo-1-propyl-2,3,6,9-tetrahydro-1h-purin-8-yl)phenoxy)acetic acid

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" When measured in the presence of antagonists, the dose-response curves of NECA-induced inhibition of forskolin-stimulated cAMP accumulation were right-shifted."( Molecular cloning and characterization of the human A3 adenosine receptor.
Jacobson, MA; Johnson, RG; Linden, J; Salvatore, CA; Taylor, HE, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)0.02000.00020.552110.0000AID31397; AID31398
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.03700.00011.20929.9700AID32514
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki1.17000.00030.91969.0000AID33486
Adenosine receptor A2aHomo sapiens (human)Ki0.70000.00001.06099.7920AID30798
Adenosine receptor A2bHomo sapiens (human)Ki0.70000.00021.635210.0000AID30798
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki0.70000.00021.494010.0000AID33940
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A1Bos taurus (cattle)Kd0.03700.01700.02700.0370AID31972
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (61)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
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 adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
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)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1345822Human A3 receptor (Adenosine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Nov-01, Volume: 90, Issue:21
Molecular cloning and characterization of the human A3 adenosine receptor.
AID1345721Human A2B receptor (Adenosine receptors)1999Molecular pharmacology, Oct, Volume: 56, Issue:4
Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
AID230535Ratio of selectivity for A3 and A2a receptors at rat brain1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
AID31972Displacement of [125-I]-labeled aminobenzyl adenosine binding to adenosine A1 receptor of bovine brain membranes1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
AID32514Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
AID31243Bmax value against A1 receptor1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Photoaffinity labeling adenosine A1 receptors with an antagonist 125I-labeled aryl azide derivative of 8-phenylxanthine.
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.
AID31398Binding affinity to adenosine A1 receptor of rat brain membranes with 1 M 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.
AID31699Binding affinity towards adenosine A1 receptor in rat brain membrane(KD)1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Photoaffinity labeling adenosine A1 receptors with an antagonist 125I-labeled aryl azide derivative of 8-phenylxanthine.
AID30798Inhibition of NECA binding to adenosine A2 receptor mediates reduced adenylate cyclase activity in human platelets1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors.
AID33940Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
AID230534Ratio of selectivity for A3 and A1 receptors at rat brain1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
AID33486Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (20.00)18.7374
1990's7 (70.00)18.2507
2000's1 (10.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.24

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 Index12.24 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]