Compounds > cns 5161
Page last updated: 2024-12-08

cns 5161

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

Description

CNS 5161: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID192711
CHEMBL ID41306
SCHEMBL ID499356
MeSH IDM0442548

Synonyms (19)

Synonym
160754-76-7
cns5161
cns-5161
CHEMBL41306 ,
cns 5161
n''-(2-chloro-5-methylsulfanyl-phenyl)-n-methyl-n-(3-methylsulfanyl-phenyl)-guanidine
bdbm50096974
2-(2-chloro-5-methylsulfanylphenyl)-1-methyl-1-(3-methylsulfanylphenyl)guanidine
guanidine, n'-(2-chloro-5-(methylthio)phenyl)-n-methyl-n-(3-(methylthio)phenyl)-
unii-58s83m36v6
58s83m36v6 ,
DB05824
SCHEMBL499356
DTXSID20166975
AKOS027382365
Q27095700
cns5161;cns 5161
3-(2-chloro-5-(methylthio)phenyl)-1-methyl-1-(3-(methylthio)phenyl)guanidine
cns-5161,n-(2-chloro-5-methylsulfanyl-phenyl)-n-methyl-n-(3-methylsulfanyl-phenyl)-guanidine

Research Excerpts

Overview

CNS 5161 is a novel NMDA ion-channel antagonist. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

ExcerptReferenceRelevance
"CNS 5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate."( Early clinical experience with the novel NMDA receptor antagonist CNS 5161.
Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002)		1.27

Toxicity

ExcerptReferenceRelevance
" All adverse events to study drug, blood pressure, heart rate, ECG, drug level and clinical laboratory values were monitored."( Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain.
Forst, T; Marcus, P; Pfützner, A; Schütte, K; Smith, T, 2007)		0.62
" The most common adverse events were hypertension, headache and mild visual disorders."( Dose escalating safety study of CNS 5161 HCl, a new neuronal glutamate receptor antagonist (NMDA) for the treatment of neuropathic pain.
Forst, T; Marcus, P; Pfützner, A; Schütte, K; Smith, T, 2007)		0.62

Dosage Studied

ExcerptRelevanceReference
" A dose escalation design was adopted and the volunteers were stratified into eight dosage groups, ranging from 30 microg to 2000 microg."( Early clinical experience with the novel NMDA receptor antagonist CNS 5161.
Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002)		0.55
" A dose dependent rise in systolic, mean arterial and diastolic blood pressure was seen in subsequent dosage groups, reaching 23/19 mmHg."( Early clinical experience with the novel NMDA receptor antagonist CNS 5161.
Bradford, AP; Fischer, J; Lees, KR; Walters, MR, 2002)		0.55
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki0.00190.00120.70256.0000AID143453
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki0.00190.00120.70256.0000AID143453
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC50 (µMol)1.75000.00232.82969.0000AID146732
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki0.00190.00120.48246.0000AID143453
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki0.00190.00120.62056.0000AID143453
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki0.00190.00120.32686.0000AID143453
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki0.00190.00120.70256.0000AID143453
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki0.00190.00120.70256.0000AID143453
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC50 (µMol)1.75000.00003.740110.0000AID146732
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC50 (µMol)1.75000.00532.80859.0000AID146732
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (82)

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)
sodium ion transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
adult walking behaviorSodium channel protein type 1 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potential propagationSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuromuscular process controlling postureSodium channel protein type 1 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painSodium channel protein type 1 subunit alphaHomo sapiens (human)
establishment of localization in cellSodium channel protein type 1 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 1 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
regulation of presynaptic membrane potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of calcium ion transport into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
propylene metabolic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of membrane potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein heterotetramerizationGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion homeostasisGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to glycineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
startle responseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to amphetamineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
learning or memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to xenobiotic stimulusGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to woundingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sensory perception of painGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
neurogenesisGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sleepGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
directional locomotionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
negative regulation of protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dopamine metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
serotonin metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of apoptotic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
activation of cysteine-type endopeptidase activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein localization to postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
learning or memoryGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
protein heterotetramerizationGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
negative regulation of dendritic spine maintenanceGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
response to woundingGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
directional locomotionGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
negative regulation of protein catabolic processGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
neuromuscular process controlling balanceGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
protein localization to postsynaptic membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
calcium ion transportGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
dendrite developmentGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
rhythmic processGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
prepulse inhibitionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
negative regulation of dendritic spine developmentGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
calcium ion transmembrane transportGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 3AHomo sapiens (human)
sodium ion transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuron apoptotic processSodium channel protein type 2 subunit alphaHomo sapiens (human)
memorySodium channel protein type 2 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 2 subunit alphaHomo sapiens (human)
dentate gyrus developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 2 subunit alphaHomo sapiens (human)
cellular response to hypoxiaSodium channel protein type 2 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 3 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 3 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

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

Ceullar Components (39)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
presynaptic active zone membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
hippocampal mossy fiber to CA3 synapseGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2DHomo sapiens (human)
neuronal cell bodyGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 3BHomo sapiens (human)
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 1 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 1 subunit alphaHomo sapiens (human)
nuclear bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 1 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 1 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal cell bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 1 subunit alphaHomo sapiens (human)
cytoplasmGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendriteGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic cleftGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
terminal boutonGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cytoplasmic vesicle membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cytoplasmGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
lysosomeGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
late endosomeGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
cytoskeletonGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2BHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2CHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 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)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 2 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 2 subunit alphaHomo sapiens (human)
axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 2 subunit alphaHomo sapiens (human)
paranode region of axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 2 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
sarcoplasmSodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 3 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID188219Compound was tested in hypoxia -ischemia reduction model for percent reduction in lesion volume at the dose 4 mg/kg (iv)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID178880Compound was tested in rotarod motor assay and the effective intravenous dose required to fall from the rod was reported.2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID233151Lowest effective intravenous dose required to observe the behavioral effects (excitation)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID146731Cardiac sodium channel blocking activity by [14C]guanidinium flux assay2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID189394Tested in rat middle cerebral artery occlusion model (MACO model) and percent reduction in total lesion volume at the dose of 1.5 mg/kg (combination ip and iv)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID132239Effective dose required to block the audiogenic seizures.2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID26784Partition coefficient (logP)2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands.
AID145330In vitro binding to N-methyl-D-aspartate glutamate receptor using [3H]MK-801 (1 nM) and rat brain membrane suspensions2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands.
AID146732Neuronal sodium channel blocking activity by [14C]guanidinium flux assay2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID143453In vitro displacement of [3H]MK-801 from N-methyl-D-aspartate glutamate receptor2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
AID493017Wombat Data for BeliefDocking2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (55.56)29.6817
2010's4 (44.44)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.97

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 Index11.97 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
dizocilpine
[no description available]		2.0110secondary amino compound;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.0310maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
ConditionIndicatedRelationship StrengthStudiesTrials
Apoplexy
[description not available]		0210
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		0210
Nerve Pain
[description not available]		02.4620
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.4620