Page last updated: 2024-12-08

cp 101,606

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

Description

traxoprodil mesylate: a selective NMDA antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID219101
CHEMBL ID17350
SCHEMBL ID4248
MeSH IDM0451275

Synonyms (54)

Synonym
1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol
bdbm50032651
1-[(s)-2-(s)-hydroxy-2-(4-hydroxy-phenyl)-1-methyl-ethyl]-4-phenyl-piperidin-4-ol
1-((1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol ,
1-[(1s,2s)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methyl-ethyl]-4-phenyl-piperidin-4-ol
(+)-cp 101606
utc046r5hm ,
unii-utc046r5hm
BB 0261961
cp101606
cp 98113
traxoprodil [inn]
traxoprodil
1-piperidineethanol, 4-hydroxy-alpha-(4-hydroxyphenyl)-beta-methyl-4-phenyl-, (s-(r*,r*))-
1-piperidineethanol, 4-hydroxy-alpha-(4-hydroxyphenyl)-beta-methyl-4-phenyl-, (alphas,betas)-
cp 101606
cp-101606
CHEMBL17350 ,
cp-101,606
134234-12-1
BCP9000547
AKOS015959795
traxoprodil mesylate
cp 101,606
(1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol
(.alpha.s,.beta.s)-4-hydroxy-.alpha.-(p-hydroxyphenyl)-.beta.-methyl-4-phenyl-1-piperidineethanol
traxoprodil [who-dd]
1-piperidineethanol, 4-hydroxy-.alpha.-(4-hydroxyphenyl)-.beta.-methyl-4-phenyl-, (s-(r*,r*))-
gtpl4163
MLS006010672
smr004701654
SCHEMBL4248
8Y-7002
(1 s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol
QEMSVZNTSXPFJA-HNAYVOBHSA-N
(1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol
traxoprodil(cp-101,606)
1-[(1s,2s)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-4-phenylpiperidin-4-ol
DTXSID90158605
mfcd00926469
(1s,2s)-1-(4-hydroxy-phenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol
cp-101,606, >=98% (hplc)
J-006502
NCGC00386543-02
nective
CS-W018847
134234-12-1 (free base)
188591-67-5 (mesylate)
BCP13195
cp-101606;cp101606;cp 101606;cp101,606;cp-101,606;cp 101,606
Q7836470
HY-W018061
BRD-K38158531-001-01-3
cp101606cp101606

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

Compound-Compound Interactions

ExcerptReferenceRelevance
" In current experiments, the authors investigated its neuroprotective effect alone and in combination with recombinant tissue plasminogen activator (rt-PA) in thromboembolic focal cerebral ischemia in rats."( Reduced brain infarct volume and improved neurological outcome by inhibition of the NR2B subunit of NMDA receptors by using CP101,606-27 alone and in combination with rt-PA in a thromboembolic stroke model in rats.
Hussain, M; Li, Q; Shuaib, A; Yang, T; Yang, Y, 2003
)
0.32
"The data in this study suggested that postischemia treatment with CP-101,606-27 is neuroprotective in the current stroke model; however, the authors also note that although rt-PA may offer modest protection when used alone, combination with CP-101,606-27 did not appear to enhance its effects."( Reduced brain infarct volume and improved neurological outcome by inhibition of the NR2B subunit of NMDA receptors by using CP101,606-27 alone and in combination with rt-PA in a thromboembolic stroke model in rats.
Hussain, M; Li, Q; Shuaib, A; Yang, T; Yang, Y, 2003
)
0.32

Bioavailability

ExcerptReferenceRelevance
"To assess the single-dose absolute oral bioavailability of traxoprodil in healthy male volunteers phenotyped as either CYP2D6 extensive or poor metabolisers."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
"In poor metabolisers (n = 6), oral bioavailability was approximately 80% and was consistent with a liver extraction ratio of approximately 20% (plasma clearance of approximately 4 mL/min/kg) indicating near complete absorption."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
" In extensive metabolisers, the oral bioavailability was nonlinear and dose-dependent, while in poor metabolisers, oral bioavailability appeared to be linear and dose-independent."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"Oxidation presents a constant challenge for formulation scientists trying to develop stable dosage forms."( Antioxidant-accelerated oxidative degradation: a case study of transition metal ion catalyzed oxidation in formulation.
Carter, JC; Hong, J; Lee, E; Masse, JA; Oksanen, DA, 2004
)
0.32
" Excretion of radioactivity was rapid and nearly complete within 48 h after dosing in both species."( Metabolism, distribution and excretion of a selective N-methyl-D-aspartate receptor antagonist, traxoprodil, in rats and dogs.
Butler, T; Cui, D; Potchoiba, MJ; Prakash, C, 2007
)
0.34
" Using extracellular field recordings in rat hippocampal slices, we show that a single dose of the non-selective NMDA receptor antagonist ketamine or CP-101,606, a selective antagonist of the NR2B subunit of the NMDA receptor, enhances hippocampal synaptic plasticity induced with high frequency stimulation (HFS) 24h after dosing - a time at which plasma concentrations of the drug are no longer detectable in the animal."( Effect of acute NR2B antagonist treatment on long-term potentiation in the rat hippocampus.
Bristow, LJ; Graef, JD; Kiss, L; Li, YW; Luan, FN; Luchetti, D; Newberry, K; Newton, A; Pieschl, R; Schaeffer, E; Shields, E; Simmermacher, J, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency4.77240.00108.379861.1304AID1645840
[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 ionotropic, NMDA 2DHomo sapiens (human)IC50 (µMol)0.00700.00401.73519.8000AID241037
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki0.01100.00120.70256.0000AID143451
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)IC50 (µMol)0.00700.00401.65799.8000AID241037
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki0.01100.00120.70256.0000AID143451
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)20.00000.00011.753610.0000AID598084
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)7.12500.00002.015110.0000AID309310; AID598083
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)12.61000.00021.874210.0000AID36105
Prolyl endopeptidaseSus scrofa (pig)IC50 (µMol)0.00700.00020.01050.1300AID241037
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)12.61000.00021.270410.0000AID36105
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00700.00010.729810.0000AID241037
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)66.69100.00071.600310.0000AID143779; AID143785; AID143788
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)12.61000.00001.819410.0000AID36105
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.630610.0000AID143779
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.03380.00061.525710.0000AID143785; AID280088; AID280089; AID309309
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.747210.0000AID143788
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC50 (µMol)0.01850.00101.88779.8000AID241037; AID242374
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki0.01100.00120.48246.0000AID143451; AID144050
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)10.00000.00091.901410.0000AID309312
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC50 (µMol)0.00700.00101.99589.8000AID241037
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki0.01100.00120.62056.0000AID143451
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)IC50 (µMol)0.03700.00401.33259.8000AID241037; AID242374; AID598080
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki0.01100.00120.32686.0000AID143451; AID144050
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)IC50 (µMol)0.00700.00401.86339.8000AID241037
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki0.01100.00120.70256.0000AID143451
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)IC50 (µMol)0.00700.00401.65799.8000AID241037
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki0.01100.00120.70256.0000AID143451
[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)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC20 (µMol)0.15000.15000.22500.3000AID309316
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (109)

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)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo 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)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 (55)

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)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo 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)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo 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 (34)

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)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
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)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (48)

Assay IDTitleYearJournalArticle
AID598085Antagonist activity at NR2A transfected in oocytes upto 90 uM2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID242374Inhibition of NMDA-evoked increased intracellular [Ca2+] in cells expressing NR1/NR2B receptor2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Oxamides as novel NR2B selective NMDA receptor antagonists.
AID132752In vivo inhibition of NMDA-stimulated fos induction in mouse following i.p. administration.1995Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
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.
AID309316Blockade of hERG channel expressed in HEK293 cells by electrophysiological method2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID598082Intrinsic clearance in human liver microsomes2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID598084Iinhibition of CYP3A42011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID177137In vivo inhibition of haloperidol-induced catalepsy in rat following s.c. administration.1995Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
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.
AID280089Displacement of [3H]Ro 25,6981 from NR2B NMDA receptor in rat forebrain2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
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.
AID112519In vivo activity was measured in mice after ip administration using standard sound-induced seizures assay2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
AID179222Compound was tested for neuroprotection against NMDA-Induced toxicity in cultured hippocampal neurons.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
AID598081Equilibrium solubility of the compound at pH 7.42011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID280088Antagonist activity at NR2B NMDA receptor in Wistar rat neocortical cells assessed as inhibition of NMDA-evoked elevation of intracellular calcium concentration2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID309311Ratio of Half life of compound in human liver microsome HHM0168 to half life in human liver microsome HHM0168 in presence of CYP2D62007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID309310Displacement of [3H]bufuralol from CYP2D62007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID233255Selectivity between protection against glutamate-induced neuronal damage and alpha 1 adrenergic affinity1995Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
AID127841Compound was evaluated in vivo for blockade of NMDA-stimulated fos induction in mouse1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
AID280092Inhibition of formalin induced nociception in orally dosed NMRI mouse by measuring pain-related licking behavior in late phase2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
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.
AID36105In vitro binding affinity against Alpha-1 adrenergic receptor using [3H]prazosin as radioligand1995Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
AID143785Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID144050Displacement of [3H]ifenprodil binding to recombinant human NR1a/NR2B receptors expressed in L(tk-) cells2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.
AID143918Displacement of racemic [3H]CP-101606 from rat forebrain membrane N-methyl-D-aspartate glutamate receptor 2B1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
AID197260In vitro inhibition of glutamate induced neuronal death in primary cultures of rat hippocampal neurons.1995Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
AID246885In vivo analgesic activity was tested using formalin test in mouse upon p.o. administration2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Oxamides as novel NR2B selective NMDA receptor antagonists.
AID241037Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Oxamides as novel NR2B selective NMDA receptor antagonists.
AID598078Displacement of [3H]CP101606 from NR2B in rat brain minus cerebellum membrane2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID540211Fraction unbound 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.
AID598083Iinhibition of CYP2D62011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID143779Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID246886In vivo analgesic activity was tested using formalin test in mouse upon s.c. administration2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Oxamides as novel NR2B selective NMDA receptor antagonists.
AID730401Neuroprotective activity in Parkinson disease patient assessed as reduction of L-DOPA-induced dyskinesia administered as infusion treated prior to L-DOPA-challenge relative to control2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Target- and mechanism-based therapeutics for neurodegenerative diseases: strength in numbers.
AID143451Binding affinity against NMDA receptor by displacement of [3H]Ro-2569812003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
AID598080Antagonist activity at human NR2B expressed in HEK293 cells assessed as glutamate-induced changes in intracellular calcium concentration2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
AID309313Ratio of IC50 for rat NR2B to IC50 for hERG channel2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID143788Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2C.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID309312Displacement of [3H]bufuralol from hERG channel expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID309309Displacement of [3H]racemic CP-101606 from rat NR2B receptor in P2 membrane2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
AID177805Compound was evaluated in vivo for blockade of haloperidol induced catalepsy in rat when administered subcutaneously1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (93)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's19 (20.43)18.2507
2000's41 (44.09)29.6817
2010's25 (26.88)24.3611
2020's8 (8.60)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (6.45%)5.53%
Reviews6 (6.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other81 (87.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]