Page last updated: 2024-11-07

ym 872

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

Description

YM 872: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID148200
CHEMBL ID119625
SCHEMBL ID678832
MeSH IDM0286767

Synonyms (30)

Synonym
ym-872
zonampanel
(7-imidazol-1-yl-6-nitro-2,3-dioxo-3,4-dihydro-2h-quinoxalin-1-yl)-acetic acid
bdbm50133599
ym872
CHEMBL119625 ,
ym 872
ym872 anhydrous
ym 872 anhydrous
zonampanel anhydrous
ym-872 anhydrous
2-(7-imidazol-1-yl-6-nitro-2,3-dioxo-4h-quinoxalin-1-yl)acetic acid
zonampanel (inn/usan)
210245-80-0
D09035
1(2h)-quinoxalineacetic acid, 3,4-dihydro-7-(1h-imidazol-1-yl)-6-nitro-2,3-dihydro-
unii-9x33544ils
7-(1h-imidazol-1-yl)-6-nitro-2,3-dioxo-3,4-dihydro-1(2h)-quinoxalineacetic acid
9x33544ils ,
7-(1h-imidazol-1-yl)-6-nitro-2,3-dioxo-3,4-dihydroquinoxalin-1(2h)-yl)acetic acid
zonampanel [usan:inn]
zonampanel [inn]
SCHEMBL678832
DTXSID50175232
CS-6830
HY-15072
[2,3-dioxo-7-(1h-imidazol-1-yl)-6-nitro-1,2,3,4-tetrahydro-1-quinoxalinyl] acetic acid
Q21098871
MS-24979
AKOS040742836

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" to rats with or without probenecid (50 mg/kg) or cimetidine (40 mg/kg), and pharmacokinetic parameters were compared."( Role of organic anion transporters in the pharmacokinetics of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in rats.
Aoki, T; Hashimoto, T; Kamimura, H; Minematsu, T; Usui, T, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.600310.0000AID496836; AID496837
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.630610.0000AID496836; AID496837
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00061.525710.0000AID496836; AID496837
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.747210.0000AID496836; AID496837
Solute carrier family 22 member 6Homo sapiens (human)IC50 (µMol)3.00000.27004.53069.9000AID496844
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.741110.0000AID496836; AID496837
Solute carrier family 22 member 8Homo sapiens (human)IC50 (µMol)6.60004.93007.39009.9200AID496845
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.741110.0000AID496836; AID496837
Solute carrier family 22 member 11Homo sapiens (human)IC50 (µMol)300.00002.03004.66507.3000AID496846
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.741110.0000AID496836; AID496837
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
monoatomic anion transportSolute carrier family 22 member 6Homo sapiens (human)
response to organic cyclic compoundSolute carrier family 22 member 6Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 6Homo sapiens (human)
organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transportSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 6Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 6Homo sapiens (human)
renal tubular secretionSolute carrier family 22 member 6Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 8Homo sapiens (human)
response to toxic substanceSolute carrier family 22 member 8Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 8Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 8Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 8Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 11Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 11Homo sapiens (human)
organic anion transportSolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 11Homo sapiens (human)
urate metabolic processSolute carrier family 22 member 11Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
solute:inorganic anion antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
protein bindingSolute carrier family 22 member 6Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
chloride ion bindingSolute carrier family 22 member 6Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 8Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 11Homo sapiens (human)
protein bindingSolute carrier family 22 member 11Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
caveolaSolute carrier family 22 member 6Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 6Homo sapiens (human)
protein-containing complexSolute carrier family 22 member 6Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 8Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
external side of plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 11Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 11Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID496836Inhibition of NMDA receptor glutamate site from rat cortical membrane2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496843Cardioprotective effect against middle cerebral artery occlusion-induced focal cerebral ischemia in spontaneously hypertensive rat assessed as reduction in infarct volume at 20 mg/kg, iv after 2 hrs of occlusion2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496845Inhibition of human OAT32010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID239653Displacement of [3H]AMPA (5 nM) from ionotropic glutamate receptor AMPA of rat cerebral cortex synaptic membrane preparation2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID496842Neuroprotective effect against middle cerebral artery occlusion-induced focal cerebral ischemia in spontaneously hypertensive rat at 20 mg/kg, iv after 2 hrs of occlusion2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID237720Solubility at pH 7.42004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group.
AID496846Inhibition of human OAT42010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496844Inhibition of human OAT12010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496835Displacement of [3H]kainate from kainate receptor in rat cortical membrane2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID496834Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID169555Neuroprotective effect in rat after iv administration at a dose of 30 mg/kg/h for 4 h2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.
AID496841Neuroprotective effect against middle cerebral artery occlusion-induced focal cerebral ischemia in spontaneously hypertensive rat at 20 mg/kg, iv after 3 hrs of occlusion2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID252188In vivo protective effect in focal ischemia rat model was determined after intravenous dosage at 30 mg/kg/h for 4 hr2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group.
AID244246Selectivity as ratio of Ki for N-methyl-D-aspartate glutamate receptor and ionotropic glutamate receptor AMPA2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group.
AID92643Binding affinity for ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand, bound to synaptic membranes prepared from rat cerebral cortex2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.
AID184019In vitro inhibitory effect on AMPA-induced DC potential in rat cortical slices; active2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID143457Ratio of binding affinity towards N-methyl-D-aspartate glutamate receptor (NMDA-R) to that of AMPA-R2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID496837Inhibition of NMDA receptor glycine site from rat cortical membrane2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (26.83)18.2507
2000's24 (58.54)29.6817
2010's6 (14.63)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: 10.70

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 Index10.70 (24.57)
Research Supply Index3.74 (2.92)
Research Growth Index4.44 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (9.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other37 (90.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]