Page last updated: 2024-11-10

6-cyano-7-nitroquinoxaline-2,3-dione

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Description

6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3721046
CHEMBL ID222418
CHEBI ID34468
SCHEMBL ID3675781
SCHEMBL ID1662279
SCHEMBL ID8122733
MeSH IDM0028085

Synonyms (65)

Synonym
HMS3266C05
BRD-K19438463-001-01-4
BRD-K53545112-304-01-6
2,3-dihydroxy-7-nitro-6-quinoxalinecarbonitrile
AE-641/00585012
NCGC00024491-01
tocris-0190
BPBIO1_001232
LOPAC0_000384
BIOMOL-NT_000200
cnqx
6-cyano-7-nitroquinoxaline-2,3-dione
115066-14-3
cnqx, >=98% (hplc), solid
NCGC00024491-02
fg-9065
6-quinoxalinecarbonitrile, 1,2,3,4-tetrahydro-7-nitro-2,3-dioxo-
1,4-dihydro-2,3-dihydroxy-7-nitro-6-quinoxalinecarbonitrile
fg 9065
cyanquixaline
fg9065
6-cyano-2,3-dihydroxy-7-nitroquinoxaline
7-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-carbonitrile
chebi:34468 ,
CHEMBL222418
AKOS005067433
7-nitro-2,3-dioxo-1,4-dihydroquinoxaline-6-carbonitrile
6ote87sccw ,
unii-6ote87sccw
ST50405216 ,
cnqx disodium salt hydrate
FT-0621098
6-quinoxalinecarbonitrile,1,2,3,4-tetrahydro-7-nitro-2,3-dioxo-
[3h]cnqx
gtpl4081
gtpl5475
2,3-dioxo-7-nitro-1,2,3,4-tetrahydroquinoxaline-6-carbonitrile
AKOS022488634
SCHEMBL3675781
SCHEMBL1662279
SCHEMBL8122733
RPXVIAFEQBNEAX-UHFFFAOYSA-N
7-nitro-2,3-dioxo-1,2,3,4-tetrahydro-quinoxaline-6-carbonitrile
114828-88-5
HB0204
c9h4n4o4
AC-33200
mfcd00069232
6-cyano-7-nitro-1,4-dihydroquinoxaline-2,3-dione
sr-01000597684
SR-01000597684-1
AS-71696
CS-6970
HY-15066
DTXSID40893918
6-cyano-7-nitroquinoxaline-2,3-dionecnqx
Q4386534
Q27458884
6-cyano-2,3-dihydroxy-7-nitro-quinoxaline
HMS3678G09
HMS3414G09
BRD-K19438463-001-02-2
NCGC00024491-11
EX-A5681
C3725

Research Excerpts

Toxicity

ExcerptReferenceRelevance
") were also resistant to the toxic effects of quisqualic acid, indicating the possible involvement of NMDA receptors in quisqualic acid toxicity."( Quisqualic acid-induced neurotoxicity is protected by NMDA and non-NMDA receptor antagonists.
Pai, KS; Ravindranath, V, 1992
)
0.28
" Solutions of TOPA were also toxic to mesencephalic neurons after acute or chronic exposure, displaying the same leftward shift in LD50."( Characterization of 2,4,5-trihydroxyphenylalanine neurotoxicity in vitro and protective effects of ganglioside GM1: implications for Parkinson's disease.
Dal Toso, R; Facci, L; Leon, A; Moroni, F; Schiavo, N; Skaper, SD; Vantini, G, 1992
)
0.28
" Reducing the glutamate level of macrophage SN, either by exposure to astrocytes or by enzymatic degradation abolished the toxic effect."( Murine brain macrophages induced NMDA receptor mediated neurotoxicity in vitro by secreting glutamate.
Cuénod, M; Do, KQ; Fontana, A; Frei, K; Piani, D, 1991
)
0.28
"There is now convincing evidence that excessive accumulation of the excitatory amino acid glutamate (GLU) in the extracellular space is toxic to central mammalian neurons."( Glutamate neurotoxicity in vitro: antagonist pharmacology and intracellular calcium concentrations.
Michaels, RL; Rothman, SM, 1990
)
0.28
" When present during the exposure, 6-cyano-2,3-dihydroxy-7-nitroquinoxaline (CNQX, 10 microM), an antagonist with preferential action on non-N-methyl-D-aspartate receptors, did not prevent this toxic effect of QA."( Quisqualate neurotoxicity: a delayed, CNQX-sensitive process triggered by a CNQX-insensitive mechanism in young rat hippocampal slices.
Garthwaite, G; Garthwaite, J, 1989
)
0.28
" The constant perfusion (1 h) of glutamate 50 microM was toxic to the neurons."( Glutamate effect on synaptic transmission mediates neurotoxicity in dissociated rat hippocampal neurons.
Yoon, KW, 1995
)
0.29
"Glutamate (Glu), the major excitatory neurotransmitter in the nervous system, is toxic to neurons when it accumulates at high concentrations in the extracellular space."( Rapid desensitization determines the pharmacology of glutamate neurotoxicity.
Moudy, AM; Rothman, SM; Yamada, KA, 1994
)
0.29
" After a 5 min toxic insult, [Ca2+]i increased immediately and remained elevated for an hour."( Intracellular calcium levels during the period of delayed excitotoxicity.
Dubinsky, JM, 1993
)
0.29
" Activation of the coagulation system and adverse effects of homocysteine on the endothelium and vessel wall are believed to underlie disease pathogenesis."( Neurotoxicity associated with dual actions of homocysteine at the N-methyl-D-aspartate receptor.
Arnelle, DR; Choi, YB; D'Emilia, DM; Kim, WK; Kumar, S; Lipton, SA; Rayudu, PV; Stamler, JS, 1997
)
0.3
" We conclude that exposures to toxic levels of NO cause prolonged disruption of [Ca2+]i homeostatic mechanisms, and that the resulting persistent [Ca2+]i elevations contribute to the delayed neurotoxicity of NO."( Disrupted [Ca2+]i homeostasis contributes to the toxicity of nitric oxide in cultured hippocampal neurons.
Brorson, JR; Zhang, H, 1997
)
0.3
" Pretreatment with rotenone significantly augmented the toxic effect of L-DOPA on DA neurons."( Metabolic inhibition enhances selective toxicity of L-DOPA toward mesencephalic dopamine neurons in vitro.
Itakura, T; Nakai, K; Nakao, N, 1997
)
0.3
" Our findings suggest that the toxic effects of MPP+ on dopaminergic terminals are not mediated through a direct interaction with the NMDA subtype of glutamate receptor, but with the AMPA-kainate subtype."( The non-NMDA glutamate receptor antagonists 6-cyano-7-nitroquinoxaline-2,3-dione and 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline, but not NMDA antagonists, block the intrastriatal neurotoxic effect of MPP+.
Cano, J; Machado, A; Merino, M; Vizuete, ML, 1999
)
0.56
" We report that, at high concentrations (300 microM-30 mM), a folic acid hexaglutamate analog is dose-dependently toxic to dissociated rat cortical cultures and that this toxicity is reversed by 2-PMPA, a potent and selective NAALADase inhibitor."( Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition.
Olkowski, JL; Slusher, BS; Thomas, AG; Vornov, JJ, 1999
)
0.3
" The compounds were divided into four groups, excitotoxins, neurotoxic but non-excitotoxic compounds, neuroactive but non-toxic compounds, and compounds that were toxic to other target organelles."( Improvements in an in-vitro assay for excitotoxicity by measurement of early gene (c-fos mRNA) levels.
Campiani, G; Griffiths, R; Meredith, C; Rogers, A; Schmuck, G; Scholz, G; Schousboe, A; Williams, DC, 2005
)
0.33
" Coadministration of the donor with Tempol (1 mM), a one-electron oxidant that converts NO- to NO, prevented its toxic effect, as did the concomitant addition of Fe(III)TPPS."( Neurotoxicity of nitroxyl: insights into HNO and NO biochemical imbalance.
Espey, MG; Hewett, SJ; Uliasz, TF; Wink, DA, 2005
)
0.33
"05-1mM, 24h) was highly toxic for mature CGNs while young CGNs were insensitive to the toxic effect of Glu."( Paraquat potentiates glutamate toxicity in immature cultures of cerebellar granule neurons.
Isaev, NK; Stelmashook, EV; Zorov, DB, 2007
)
0.34

Compound-Compound Interactions

ExcerptReferenceRelevance
" With appropriate design of push-pull cannula and recording chamber, therefore, stable electrophysiological recordings can be combined with localized extracellular fluid sampling and rapid and localized application of test solutions in an interface slice chamber."( Push-pull cannula for localized application of drugs and sampling of medium, combined with electrophysiological recordings in an interface slice chamber.
Do, KQ; Thomson, AM; West, DC, 1992
)
0.28
" Present results raise the possibility that Na+ channel blockers may be useful in protecting gray matter from hypoxic-ischemic injury, especially when combined with antiexcitotoxic approaches."( Sodium channel blockers reduce oxygen-glucose deprivation-induced cortical neuronal injury when combined with glutamate receptor antagonists.
Canzoniero, LM; Choi, DW; Lynch, JJ; Sensi, SL; Yu, SP, 1995
)
0.29

Bioavailability

ExcerptReferenceRelevance
" Together, these data support the idea that the synthesis of estrogen can be rapidly regulated in the brain, thus producing rapid changes in local estrogen bioavailability that could rapidly modify brain function with a time course similar to what has previously been described for neurotransmitters and neuromodulators."( Rapid control of brain aromatase activity by glutamatergic inputs.
Baillien, M; Ball, GF; Balthazart, J, 2006
)
0.33

Dosage Studied

ExcerptRelevanceReference
" Dose-response studies using kainate indicated that at least two agonist molecules bind to gate the channel."( The kinetics of the response to glutamate and kainate in neurons of the avian cochlear nucleus.
Raman, IM; Trussell, LO, 1992
)
0.28
" Application of solutions of TOPA to cerebellar granule cells resulted in a concentration- and time-dependent neuronal death, with prolonged (24 hr) exposure producing a clear left-handed shift in the dose-response relationship from the one observed with a 60-min exposure (LD50: 4 and 29 microM, respectively)."( Characterization of 2,4,5-trihydroxyphenylalanine neurotoxicity in vitro and protective effects of ganglioside GM1: implications for Parkinson's disease.
Dal Toso, R; Facci, L; Leon, A; Moroni, F; Schiavo, N; Skaper, SD; Vantini, G, 1992
)
0.28
" L-Aspartate (L-Asp) produced a similar dose-response relationship."( Electrogenic uptake contributes a major component of the depolarizing action of L-glutamate in rat hippocampal slices.
Blake, JF; Brown, MW; Collingridge, GL; Frenguelli, BG, 1991
)
0.28
" Dose-response curves obtained in oocytes were bell shaped, with a negative slope for high concentrations of QA."( Reduction of desensitization of a glutamate ionotropic receptor by antagonists.
Audinat, E; Crepel, F; Geoffroy, M; Hamon, B; Kado, RT; Lambolez, B; Rossier, J, 1991
)
0.28
" Analyses of dose-response curves of these inward currents indicate that both the QA and KA currents were competitively blocked by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), while the NMDA current was blocked non-competitively."( Glutamate receptor agonist-induced inward currents in spinal dorsal horn neurons dissociated from the adult rats.
Arancio, O; MacDermott, AB; Murase, K; Yoshimura, M, 1991
)
0.49
" Apomorphine-induced cage climbing behavior was partially decreased by lower dosages of GDEE, but was almost completely blocked by the highest dosage tested."( A possible role of AA2 excitatory amino acid receptors in the expression of stimulant drug effects.
Cannon-Spoor, HE; Freed, WJ, 1990
)
0.28
" At a concentration of 10 microM, CNQX reversibly antagonized responses to alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualate and kainate; it produced a parallel shift in their log dose-response curves."( 6-Cyano-7-nitroquinoxaline-2,3-dione as an excitatory amino acid antagonist in area CA1 of rat hippocampus.
Blake, JF; Brown, MW; Collingridge, GL; Yates, RG, 1989
)
1.72
" Dose-response curves showed that DCG-IV was weaker than NMDA but more potent than glutamate in eliciting agonist-gated currents."( Metabotropic glutamate receptor agonist DCG-IV as NMDA receptor agonist in immature rat hippocampal neurons.
Opitz, T; Pidoplichko, VI; Reymann, KG; Shinozaki, H; Wilsch, VW, 1994
)
0.29
" Bath-application of kainate, quisqualate and L-glutamate elicited concentration-dependent membrane depolarizations in both cell types as demonstrated by dose-response curves."( Effects of glutamatergic agonists and antagonists on membrane potential and intracellular Na+ activity of leech glial and nerve cells.
Dörner, R; Schlue, WR; Zens, M, 1994
)
0.29
" The actions of the hepoxilins showed a sharp dose-response relationship, with minimal threshold or no effect at 3 nM (n = 21) and maximal effects at 10 nM (n = 33)."( Formation and electrophysiological actions of the arachidonic acid metabolites, hepoxilins, at nanomolar concentrations in rat hippocampal slices.
Carlen, PL; Gurevich, N; Pace-Asciak, CR; Reynaud, D; Wu, PH; Zhang, L, 1994
)
0.29
" Dose-response curves for inhibition of [3H]CNQX by AMPA and kainate were biphasic."( Autoradiographic characterization of the non-N-methyl-D-aspartate binding sites in human cerebellum using the antagonist [3H]6-cyano-7-nitroquinoxaline-2,3-dione.
Hatziefthimiou, A; Kouvelas, ED; Mitsacos, A, 1994
)
0.49
" A thorough dose-response study using microdialysis in conscious rats indicated that low doses of ketamine (10, 20, and 30 mg/kg) increase glutamate outflow in the PFC, suggesting that at these doses ketamine may increase glutamatergic neurotransmission in the PFC at non-NMDA glutamate receptors."( Activation of glutamatergic neurotransmission by ketamine: a novel step in the pathway from NMDA receptor blockade to dopaminergic and cognitive disruptions associated with the prefrontal cortex.
Adams, B; Daly, D; Moghaddam, B; Verma, A, 1997
)
0.3
" Evoked inhibitory postsynaptic currents (IPSCs) were decreased by kainate by up to 90%, showing a bell-shaped dose-response curve similar to that of native kainate-selective receptors."( Kainate receptors presynaptically downregulate GABAergic inhibition in the rat hippocampus.
Herreras, O; Lerma, J; Rodríguez-Moreno, A, 1997
)
0.3
" The role of different Ca2+ channel subtypes in shaping the Ca2+ dose-response relationship was studied using the selective Ca2+ channel blockers omega-agatoxin GIVA (omega-Aga), which blocks P/Q-type channels, and omega-conotoxin GVIA (omega-CTx), which blocks N-type channels."( N- and P/Q-type Ca2+ channels mediate transmitter release with a similar cooperativity at rat hippocampal autapses.
Bekkers, JM; Clements, JD; Reid, CA, 1998
)
0.3
" In fact it showed: (1) very sensitive dose-response not affected by TTX in the bath; (2) an equilibrium potential compatible with Cl-channel conductance; (3) a massive reduction with the competitive GABA(A) antagonist bicuculline; (4) a small reduction, if any, with the potent competitive GABA(B) antagonist CGP55845A; (5) persistence of the responses under 4-AP (4-aminopyridine), the potassium channel blocker, and inhibition of the 4-AP-induced calcium bursts of spikes."( Purkinje cell inhibitory responses to 3-APPA (3-aminopropylphosphinic acid) in RAT cerebellar slices.
Batini, C; Vigot, R, 1999
)
0.3
" We investigated the dose-response relationship for each alcohol and determined that the order of potency was methanol < EtOH << octanol, with EC(50) values of 291 mM, 39."( Effect of ethanol upon respiratory-related hypoglossal nerve output of neonatal rat brain stem slices.
Berger, AJ; Gibson, IC, 2000
)
0.31
" After AMPA stimulation, dose-response inhibition curves showed an IC(50) of 3 microM for CNQX and 25 microM for trimetazidine."( Trimetazidine modulates AMPA/kainate receptors in rat vestibular ganglion neurons.
Chabbert, C; Dayanithi, G; Desmadryl, G; Sans, A; Travo, C, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinoxaline derivativeAny naphthyridine derivative that is a derivative of quinoxaline (1,4-naphthyridine).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
USP1 protein, partialHomo sapiens (human)Potency63.09570.031637.5844354.8130AID504865
Microtubule-associated protein tauHomo sapiens (human)Potency3.16230.180013.557439.8107AID1460
glucocerebrosidaseHomo sapiens (human)Potency18.25630.01268.156944.6684AID2101
lethal factor (plasmid)Bacillus anthracis str. A2012Potency0.63100.020010.786931.6228AID912
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency12.58931.000010.475628.1838AID901
[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)
Glutamate receptor 1Homo sapiens (human)IC50 (µMol)1.02000.01901.70836.5100AID1859112; AID1859129; AID1859130
Glutamate receptor 2Homo sapiens (human)IC50 (µMol)1.02000.01901.64035.5000AID1859112; AID1859129; AID1859130
Glutamate receptor 3Homo sapiens (human)IC50 (µMol)1.02000.01901.13424.8000AID1859112; AID1859129; AID1859130
Glutamate receptor 4Homo sapiens (human)IC50 (µMol)1.02000.01901.22234.8000AID1859112; AID1859129; AID1859130
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
regulation of receptor recyclingGlutamate receptor 1Homo sapiens (human)
signal transductionGlutamate receptor 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor 1Homo sapiens (human)
synapse assemblyGlutamate receptor 1Homo sapiens (human)
long-term memoryGlutamate receptor 1Homo sapiens (human)
response to xenobiotic stimulusGlutamate receptor 1Homo sapiens (human)
response to lithium ionGlutamate receptor 1Homo sapiens (human)
positive regulation of gene expressionGlutamate receptor 1Homo sapiens (human)
neuronal action potentialGlutamate receptor 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor 1Homo sapiens (human)
spinal cord developmentGlutamate receptor 1Homo sapiens (human)
cerebral cortex developmentGlutamate receptor 1Homo sapiens (human)
receptor internalizationGlutamate receptor 1Homo sapiens (human)
response to estradiolGlutamate receptor 1Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 1Homo sapiens (human)
response to cocaineGlutamate receptor 1Homo sapiens (human)
positive regulation of membrane potentialGlutamate receptor 1Homo sapiens (human)
response to arsenic-containing substanceGlutamate receptor 1Homo sapiens (human)
response to electrical stimulusGlutamate receptor 1Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
long-term synaptic potentiationGlutamate receptor 1Homo sapiens (human)
long-term synaptic depressionGlutamate receptor 1Homo sapiens (human)
response to fungicideGlutamate receptor 1Homo sapiens (human)
cellular response to amino acid stimulusGlutamate receptor 1Homo sapiens (human)
cellular response to ammonium ionGlutamate receptor 1Homo sapiens (human)
cellular response to dsRNAGlutamate receptor 1Homo sapiens (human)
cellular response to peptide hormone stimulusGlutamate receptor 1Homo sapiens (human)
cellular response to amine stimulusGlutamate receptor 1Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationGlutamate receptor 1Homo sapiens (human)
cellular response to brain-derived neurotrophic factor stimulusGlutamate receptor 1Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 1Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 1Homo sapiens (human)
signal transductionGlutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 2Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 2Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor 2Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
calcium-mediated signalingGlutamate receptor 3Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 3Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
protein homotetramerizationGlutamate receptor 3Homo sapiens (human)
protein heterotetramerizationGlutamate receptor 3Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
long-term synaptic potentiationGlutamate receptor 3Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 3Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 3Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 4Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic processGlutamate receptor 4Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 4Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
amyloid-beta bindingGlutamate receptor 1Homo sapiens (human)
G-protein alpha-subunit bindingGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 1Homo sapiens (human)
protein bindingGlutamate receptor 1Homo sapiens (human)
glutamate receptor activityGlutamate receptor 1Homo sapiens (human)
adenylate cyclase bindingGlutamate receptor 1Homo sapiens (human)
immunoglobulin bindingGlutamate receptor 1Homo sapiens (human)
protein kinase bindingGlutamate receptor 1Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor 1Homo sapiens (human)
PDZ domain bindingGlutamate receptor 1Homo sapiens (human)
small GTPase bindingGlutamate receptor 1Homo sapiens (human)
myosin V bindingGlutamate receptor 1Homo sapiens (human)
G-protein beta-subunit bindingGlutamate receptor 1Homo sapiens (human)
beta-2 adrenergic receptor bindingGlutamate receptor 1Homo sapiens (human)
glutamate receptor bindingGlutamate receptor 1Homo sapiens (human)
identical protein bindingGlutamate receptor 1Homo sapiens (human)
protein kinase A bindingGlutamate receptor 1Homo sapiens (human)
scaffold protein bindingGlutamate receptor 1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 1Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 2Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
protein bindingGlutamate receptor 2Homo sapiens (human)
ligand-gated monoatomic cation channel activityGlutamate receptor 2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 3Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 3Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor 3Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 4Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 4Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 1Homo sapiens (human)
cell-cell junctionGlutamate receptor 1Homo sapiens (human)
cell surfaceGlutamate receptor 1Homo sapiens (human)
ER to Golgi transport vesicle membraneGlutamate receptor 1Homo sapiens (human)
postsynaptic densityGlutamate receptor 1Homo sapiens (human)
dendriteGlutamate receptor 1Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 1Homo sapiens (human)
synaptic vesicle membraneGlutamate receptor 1Homo sapiens (human)
neuromuscular junctionGlutamate receptor 1Homo sapiens (human)
early endosome membraneGlutamate receptor 1Homo sapiens (human)
dendritic spine membraneGlutamate receptor 1Homo sapiens (human)
neuronal cell body membraneGlutamate receptor 1Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneGlutamate receptor 1Homo sapiens (human)
neuronal cell bodyGlutamate receptor 1Homo sapiens (human)
dendritic spineGlutamate receptor 1Homo sapiens (human)
dendritic shaftGlutamate receptor 1Homo sapiens (human)
axonal spineGlutamate receptor 1Homo sapiens (human)
neuron spineGlutamate receptor 1Homo sapiens (human)
postsynaptic membraneGlutamate receptor 1Homo sapiens (human)
presynaptic active zone membraneGlutamate receptor 1Homo sapiens (human)
recycling endosomeGlutamate receptor 1Homo sapiens (human)
recycling endosome membraneGlutamate receptor 1Homo sapiens (human)
excitatory synapseGlutamate receptor 1Homo sapiens (human)
synaptic membraneGlutamate receptor 1Homo sapiens (human)
presynapseGlutamate receptor 1Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 1Homo sapiens (human)
glutamatergic synapseGlutamate receptor 1Homo sapiens (human)
postsynaptic density, intracellular componentGlutamate receptor 1Homo sapiens (human)
perisynaptic spaceGlutamate receptor 1Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 1Homo sapiens (human)
dendritic spineGlutamate receptor 1Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 1Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
external side of plasma membraneGlutamate receptor 2Homo sapiens (human)
postsynaptic densityGlutamate receptor 2Homo sapiens (human)
dendriteGlutamate receptor 2Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 2Homo sapiens (human)
asymmetric synapseGlutamate receptor 2Homo sapiens (human)
neuronal cell bodyGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
excitatory synapseGlutamate receptor 2Homo sapiens (human)
postsynapseGlutamate receptor 2Homo sapiens (human)
postsynaptic endocytic zoneGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic membraneGlutamate receptor 3Homo sapiens (human)
parallel fiber to Purkinje cell synapseGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 3Homo sapiens (human)
dendritic spineGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendriteGlutamate receptor 4Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 4Homo sapiens (human)
neuronal cell bodyGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
extracellular vesicleGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 4Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 4Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
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.
AID1347154Primary 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.
AID1859129Displacement of [3H]CNQX from AMPA receptor (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
AID1859112Displacement of [3H]AMPA from AMPA receptor (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
AID1859130Displacement of [3H]kainic acid from AMPA receptor (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,653)

TimeframeStudies, This Drug (%)All Drugs %
pre-199042 (1.58)18.7374
1990's1288 (48.55)18.2507
2000's901 (33.96)29.6817
2010's398 (15.00)24.3611
2020's24 (0.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.64

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 Index13.64 (24.57)
Research Supply Index7.90 (2.92)
Research Growth Index6.36 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (13.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.04%)5.53%
Reviews11 (0.41%)6.00%
Case Studies1 (0.04%)4.05%
Observational0 (0.00%)0.25%
Other2,685 (99.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]