Page last updated: 2024-12-11

licostinel

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Description

licostinel: a glycine site NMDA receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
GlycinegenusA non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID5486198
CHEMBL ID289832
SCHEMBL ID464947
SCHEMBL ID5274587
MeSH IDM0243078

Synonyms (43)

Synonym
6,7-dichloro-3-hydroxy-5-nitro-3,4-dihydro-1h-quinoxalin-2-one
bdbm50038161
6,7-dichloro-5-nitro-1,4-dihydro-quinoxaline-2,3-dione
6,7-dichloro-5-nitro-1,4-dihydro-quinoxaline-2,3-dione(acea 1021)
153504-81-5
D04728
licostinel (usan/inn)
licostinel [usan]
acea-1021
6,7-dichloro-5-nitro-2,3-quinoxalinedione
5-nitro-6,7-dichloro-2,3-quinoxalinedione
6,7-dichloro-1,4-dihydro-5-nitro-2,3-quinoxalinedione
licostinel
2,3-quinoxalinedione, 6,7-dichloro-1,4-dihydro-5-nitro-
acea 1021
CHEMBL289832 ,
6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione
licostinel [usan:inn]
unii-3z3037ljtc
3z3037ljtc ,
5-nitro-6,7-dichloro-1,4-dihydro-2,3-quinoxalinedione
smr002530535
MLS006010858
licostinel [mi]
licostinel [inn]
SCHEMBL464947
CHFSOFHQIZKQCR-UHFFFAOYSA-N
6,7-dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione
SCHEMBL5274587
DTXSID60165346
W13173
J-009022
AS-55059
6,7-dichloro-5-nitroquinoxaline-2,3(1h,4h)-dione
AKOS030627460
popsosesquisodiumsalt
mfcd00672687
Q19597740
BRD-K81881550-001-01-2
SY245109
HY-117547
CS-0066423
AKOS040748747

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Recently, halogenated derivatives of quinoxaline-2,3-dione have been synthesized that possess bioavailability when parenterally administered and minimal psychotomimetic properties."( In vivo models of cerebral ischemia: effects of parenterally administered NMDA receptor glycine site antagonists.
Keana, JF; Ludwig, P; Martin, H; McAllister, A; Warner, DS; Weber, E, 1995
)
0.29

Dosage Studied

ExcerptRelevanceReference
" After obtaining dose-response curves for each agent, combinations of morphine and AP-5, ACEA 1021 or ACEA 2752 were tested for their effect on the number of flinches in the formalin test and for associated side-effects, such as motor disturbances, flaccidity, and agitation/allodynia."( Interaction between intrathecal morphine and glutamate receptor antagonists in formalin test.
Nishiyama, T, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)IC50 (µMol)2,944.22290.00401.73519.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)IC50 (µMol)2,944.22290.00401.65799.8000AID143443; AID143444
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.76600.00011.617910.0000AID92360
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)0.76600.00011.700010.0000AID92360
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)0.76600.00011.700010.0000AID92360
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)0.76600.00011.700010.0000AID92360
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.600310.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.630610.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.00680.00061.525710.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.747210.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC50 (µMol)2,944.22290.00101.88779.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC50 (µMol)2,944.22290.00101.99589.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)IC50 (µMol)2,944.22290.00401.33259.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)IC50 (µMol)2,944.22290.00401.86339.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.741110.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)IC50 (µMol)2,944.22290.00401.65799.8000AID143443; AID143444
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.741110.0000AID143473; AID143475; AID143606; AID144455; AID242732
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)0.00680.00071.741110.0000AID143473; AID143475; AID143606; AID144455; AID242732
[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)
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor 1Rattus norvegicus (Norway rat)Kb1.50000.59003.33007.0000AID147418
Glutamate receptor 2Rattus norvegicus (Norway rat)Kb1.50000.59003.17337.0000AID147418
Glutamate receptor 3Rattus norvegicus (Norway rat)Kb1.50000.59003.17787.0000AID147418
Glutamate receptor 4Rattus norvegicus (Norway rat)Kb1.50000.59003.28567.0000AID147418
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Activity0.01000.00700.00850.0100AID145254
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kb0.00590.00592.09697.0000AID143296
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Kb0.00500.00500.00500.0050AID143220
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kb0.00590.00592.41137.0000AID143296
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (63)

Processvia Protein(s)Taxonomy
startle responseGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
adult locomotory behaviorGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
regulation of sensory perception of painGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
cellular response to L-glutamateGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
protein insertion into membraneGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
regulation of calcium ion transportGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
calcium ion transmembrane transportGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of calcium ion transport into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
propylene metabolic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of membrane potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein heterotetramerizationGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion homeostasisGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to glycineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
startle responseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to amphetamineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
learning or memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to xenobiotic stimulusGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to woundingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sensory perception of painGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
neurogenesisGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sleepGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
directional locomotionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
negative regulation of protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dopamine metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
serotonin metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of apoptotic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
activation of cysteine-type endopeptidase activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein localization to postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
learning or memoryGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
protein heterotetramerizationGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
negative regulation of dendritic spine maintenanceGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
response to woundingGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
directional locomotionGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
negative regulation of protein catabolic processGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
neuromuscular process controlling balanceGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
protein localization to postsynaptic membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium ion transportGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
dendrite developmentGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
rhythmic processGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
prepulse inhibitionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
negative regulation of dendritic spine developmentGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
calcium ion transmembrane transportGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
glutamate-gated receptor activityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
glutamate bindingGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
voltage-gated monoatomic cation channel activityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
calcium channel activityGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
monoatomic cation channel activityGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
glycine bindingGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
neurotransmitter receptor activityGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
glutamate receptor activityGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
amyloid-beta bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calmodulin bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glycine bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glutamate bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein-containing complex bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
signaling receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
ligand-gated monoatomic ion channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
amyloid-beta bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
zinc ion bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
amyloid-beta bindingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
zinc ion bindingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
glycine bindingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
glutamate bindingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
calcium channel activityGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
glycine bindingGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
identical protein bindingGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
protein phosphatase 2A bindingGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
glutamate receptor activityGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
presynaptic active zone membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
hippocampal mossy fiber to CA3 synapseGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
neuronal cell bodyGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
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)
cytoplasmGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendriteGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic cleftGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
terminal boutonGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cytoplasmic vesicle membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cytoplasmGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
lysosomeGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
late endosomeGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
cytoskeletonGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
membraneGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
neuronal cell bodyGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
presynapseGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
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 (43)

Assay IDTitleYearJournalArticle
AID131040Compound was tested in vivo (intra peritoneally) in the mouse maximal electroshock convulsion test2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
AID129008Anticonvulsant activity tested in mouse1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
AID143473Affinity for the glycine binding site on rat N-methyl-D-aspartate glutamate receptor 1, determined by displacement of the glycine site antagonist [3H]L-689,560 from rat cortical membranes1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID33696Binding to rat serum albumin1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Substituted analogues of GV150526 as potent glycine binding site antagonists in animal models of cerebral ischemia.
AID129170Anticonvulsant activity was measured by mouse maximal electroshock (MES) assay.1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
AID19623Partition coefficient (logP)1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID145254Tested in vivo for affinity against glycine-binding site of NMDA receptor using [3H]DCKA radioligand1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists.
AID251488Reduction of infarct volume in rat with proximal middle cerebral artery occlusion at total dose of 52 mg/kg after 180 min of initiation (duration of effect 6 h); nd=Not determined2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID143616Potency for the N-methyl-D-aspartate glutamate receptor 1 glycine site by displacement of [3H]5,7-dichlorokynurenic acid (DCKA) binding in rat brain cortical membranes.1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
AID143443Inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
CoMFA and homology-based models of the glycine binding site of N-methyl-d-aspartate receptor.
AID19631Partition coefficient determined using octanol versus pH 7.4 buffer1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
AID143220Compound was evaluated for in vitro inhibition of cortical neurone at NMDA receptor.1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID251455Reduction of infarct volume in rat with distal middle cerebral artery occlusion at total dose of 52 mg/kg after 30 min of initiation (duration of effect 6 h)2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID246987In vivo effective dose to protect the mouse (DBA/2J) from audiogenic seizures upon intraperitoneal administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID133133Ability to prevent NMDA-induced hyperlocomotion in the mouse following iv administration of 15 mg/kg dose; 3/102001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
AID246999In vivo effective dose to protect rats against maximal electroshock induced seizures upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID133002Ability to prevent NMDA-induced hyperlocomotion in the mouse following iv administration of 10 mg/kg dose; 5/102001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
AID114658Compound was evaluated for nociception in electroshock mice model in vivo through ip route1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID251487Reduction of infarct volume in rat with proximal middle cerebral artery occlusion at total dose of 52 mg/kg after 30 min of initiation (duration of effect 6 h); nd=Not determined2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID92360Displacement of [3H]-AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
AID109893Antagonist activity in nociception formalin paw seizure model in vivo through ip route; 1-201994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
AID251457Reduction of infarct volume in rat with distal middle cerebral artery occlusion at total dose of 52 mg/kg after -15 min of initiation (duration of effect 6 h)2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID246981In vivo effective dose of compound to protect mice from quinolinic acid seizures upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID203505Human serum albumin index was measured by retention time on an HPLC column containing human albumin1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID143296Binding affinity towards rat brain NMDA receptor glycine site expressed in Xenopus oocyte1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.
AID251461Reduction of infarct volume in rat with proximal middle cerebral artery occlusion at total dose of 52 mg/kg after -15 min of initiation (duration of effect 6 h)2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID92343Binding affinity in rat brain cortical membranes by the displacement of [3H]AMPA at Ionotropic glutamate receptor AMPA1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
AID143606Displacement of [3H]DCKA at N-methyl-D-aspartate glutamate receptor 11997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
AID113804Anticonvulsant activity measured by its ability to protect against audiogenic seizure in DBA/2 mice when dosed intraperitoneally 30 min prior to seizure induction.1997Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
AID246996In vivo effective dose against harmaline induced cGMP elevation in mouse cerebellum upon intravenous administration2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID251479Reduction of infarct volume in rat with distal middle cerebral artery occlusion at total dose of 52 mg/kg after 180 min of initiation (duration of effect 6 h); nd=Not determined2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID175869Inhibition of NMDA-induced depolarizations in rat cortical wedges.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
AID114334Effective dose to inhibit convulsions induced by NMDA in mice, when administered intravenous route.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
AID19828Partition coefficient (logP)1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
AID143444Compound was tested for inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
CoMFA and homology-based models of the glycine binding site of N-methyl-d-aspartate receptor.
AID242732In vitro inhibitory concentration against binding of the [3H]glycine to strychnine-insensitive glycine binding sites of rat N-methyl-D-aspartate glutamate receptor2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID143771Inhibition of [3H]glycine to glycine binding site, associated with the N-methyl-D-aspartate glutamate receptor 1 in crude synaptic membranes prepared from adult rat cerebral cortex.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
AID248671In vitro inhibitory concentration against glutamate stimulated accumulation of cyclic GMP in neonatal rat cerebral slices2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antag
AID147418Binding affinity against rat brain Non N-methyl-D-aspartate glutamate receptor glutamate site expressed in Xenopus oocyte1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.
AID133139Ability to prevent NMDA-induced hyperlocomotion in the mouse following iv administration of 3 mg/kg dose; 3/102001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
AID144455Binding affinity at glycine binding site of NMDA receptor in rat cortical membranes by [3H]L-689,560 displacement.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
AID234072Selectivity for glycine site1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.
AID143475Displacement of [3H]dichlorokynurenate ([3H]-DCKA) from N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (49)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's33 (67.35)18.2507
2000's15 (30.61)29.6817
2010's1 (2.04)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: 15.46

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index15.46 (24.57)
Research Supply Index3.93 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.04%)5.53%
Reviews2 (4.08%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other46 (93.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]