Page last updated: 2024-11-07

dihydrokainate

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

Dihydrokainate is a synthetic analog of kainate, a potent agonist at the kainate receptor subtype of ionotropic glutamate receptors. It is structurally similar to kainate, but it lacks the double bond in the cyclopentene ring. This structural difference results in a lower affinity for kainate receptors, making dihydrokainate a less potent agonist than kainate. Dihydrokainate has been shown to be a selective antagonist of the AMPA receptor subtype of glutamate receptors, suggesting that it may have therapeutic potential in the treatment of neurological disorders such as epilepsy and stroke. Dihydrokainate is also a potent inhibitor of the enzyme glutamate decarboxylase, which catalyzes the synthesis of the inhibitory neurotransmitter GABA. This activity may contribute to its neuroprotective effects. Dihydrokainate is widely studied in research to understand the roles of kainate receptors and AMPA receptors in the central nervous system. It is also being investigated as a potential therapeutic agent for various neurological disorders. '

Cross-References

ID SourceID
PubMed CID107883
CHEMBL ID279561
CHEBI ID43562
SCHEMBL ID155919
MeSH IDM0075155

Synonyms (43)

Synonym
dihydrokainic acid, >=98% (hplc), powder
1XHY
1FTK
(2s,3s,4r)-2-carboxy-4-isopropyl-3-pyrrolidineacetic acid
PDSP2_001490
dihydrokainic acid
CHEBI:43562 ,
(2s,3s,4r)-3-(carboxymethyl)-4-(propan-2-yl)pyrrolidine-2-carboxylic acid
52497-36-6
(2s,3s,4r)-2-carboxy-4-(1-methylethyl)-3-pyrrolidineacetic acid
(3s,4r)-3-(carboxymethyl)-4-(propan-2-yl)-l-proline
(2s,3s,4r)-4-isopropyl-3-(2-oxido-2-oxoethyl)pyrrolidinium-2-carboxylate
(2s,3s,4r)-3-(carboxymethyl)-4-isopropylpyrrolidine-2-carboxylic acid
(2r,3r,4s)-3-(carboxymethyl)-4-isopropylpyrrolidinium-2-carboxylate
bdbm50240399
dihydrokainate
CHEMBL279561 ,
(2s,3s,4r)-3-(carboxymethyl)-4-propan-2-ylpyrrolidine-2-carboxylic acid
HMS3261K11
A829114
3-pyrrolidineacetic acid, 2-carboxy-4-(1-methylethyl)-, (2s,3s,4r)-
unii-mq4lmc2hn5
mq4lmc2hn5 ,
(2s-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethyl)-3-pyrrolidineacetic acid
LP00375
c10h17no4
CCG-221679
SCHEMBL155919
NCGC00261060-01
tox21_500375
(2s,3s,4r)-2-carboxy-4-isopropyl-3-pyrrolidineaceticacid
HB0246
AKOS024456387
DTXSID20200489
sr-01000597697
SR-01000597697-1
SDCCGSBI-0633704.P001
MS-23180
3-pyrrolidineacetic acid, 2-carboxy-4-(1-methylethyl)-, (2s-(2.alpha.,3.beta.,4.beta.))-
.alpha.-dihydrokainic acid
XD160600
CS-0020424
HY-100784

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
dicarboxylic acidAny carboxylic acid containing two carboxy groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, GLUTAMATE RECEPTOR SUBUNIT 2Rattus norvegicus (Norway rat)IC50 (µMol)14.50000.82105.439714.5000AID977608
Chain A, Glutamate Receptor Subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)14.50000.82105.439714.5000AID977608
Chain B, Glutamate Receptor Subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)14.50000.82105.439714.5000AID977608
Chain A, Glutamate receptor 2Rattus norvegicus (Norway rat)Ki0.66200.66200.66200.6620AID977610
Chain A, Glutamate receptor 2Rattus norvegicus (Norway rat)Ki0.66200.66200.66200.6620AID977610
Chain A, Glutamate receptorRattus norvegicus (Norway rat)Ki0.66200.66200.66200.6620AID977610
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)Ki8.15420.00071.71758.1800AID339913; AID339927
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)Ki12.16130.00370.80254.1000AID339914; AID339928
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki0.36950.00380.79754.1000AID339915; AID339929
Excitatory amino acid transporter 1Homo sapiens (human)IC50 (µMol)3,081.14000.120089.38251,000.0000AID339902
Excitatory amino acid transporter 2Homo sapiens (human)IC50 (µMol)84.21640.95504.465411.0000AID339905
Excitatory amino acid transporter 3Homo sapiens (human)IC50 (µMol)3,081.14000.800015.9060161.0000AID339906
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (82)

Processvia Protein(s)Taxonomy
neurotransmitter uptakeExcitatory amino acid transporter 1Homo sapiens (human)
monoatomic ion transportExcitatory amino acid transporter 1Homo sapiens (human)
neurotransmitter transportExcitatory amino acid transporter 1Homo sapiens (human)
intracellular sodium ion homeostasisExcitatory amino acid transporter 1Homo sapiens (human)
chemical synaptic transmissionExcitatory amino acid transporter 1Homo sapiens (human)
sensory perception of soundExcitatory amino acid transporter 1Homo sapiens (human)
response to xenobiotic stimulusExcitatory amino acid transporter 1Homo sapiens (human)
response to light stimulusExcitatory amino acid transporter 1Homo sapiens (human)
gamma-aminobutyric acid biosynthetic processExcitatory amino acid transporter 1Homo sapiens (human)
response to woundingExcitatory amino acid transporter 1Homo sapiens (human)
neutral amino acid transportExcitatory amino acid transporter 1Homo sapiens (human)
L-glutamate transmembrane transportExcitatory amino acid transporter 1Homo sapiens (human)
cranial nerve developmentExcitatory amino acid transporter 1Homo sapiens (human)
auditory behaviorExcitatory amino acid transporter 1Homo sapiens (human)
response to antibioticExcitatory amino acid transporter 1Homo sapiens (human)
cell morphogenesis involved in neuron differentiationExcitatory amino acid transporter 1Homo sapiens (human)
positive regulation of synaptic transmissionExcitatory amino acid transporter 1Homo sapiens (human)
neuromuscular process controlling balanceExcitatory amino acid transporter 1Homo sapiens (human)
L-glutamate importExcitatory amino acid transporter 1Homo sapiens (human)
transepithelial transportExcitatory amino acid transporter 1Homo sapiens (human)
D-aspartate import across plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
cellular response to cocaineExcitatory amino acid transporter 1Homo sapiens (human)
potassium ion transmembrane transportExcitatory amino acid transporter 1Homo sapiens (human)
L-glutamate import across plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
L-aspartate import across plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
transport across blood-brain barrierExcitatory amino acid transporter 1Homo sapiens (human)
chloride transmembrane transportExcitatory amino acid transporter 1Homo sapiens (human)
glutathione biosynthetic processExcitatory amino acid transporter 2Homo sapiens (human)
monoatomic ion transportExcitatory amino acid transporter 2Homo sapiens (human)
neurotransmitter transportExcitatory amino acid transporter 2Homo sapiens (human)
chemical synaptic transmissionExcitatory amino acid transporter 2Homo sapiens (human)
visual behaviorExcitatory amino acid transporter 2Homo sapiens (human)
response to xenobiotic stimulusExcitatory amino acid transporter 2Homo sapiens (human)
response to woundingExcitatory amino acid transporter 2Homo sapiens (human)
L-glutamate transmembrane transportExcitatory amino acid transporter 2Homo sapiens (human)
telencephalon developmentExcitatory amino acid transporter 2Homo sapiens (human)
adult behaviorExcitatory amino acid transporter 2Homo sapiens (human)
multicellular organism growthExcitatory amino acid transporter 2Homo sapiens (human)
response to amino acidExcitatory amino acid transporter 2Homo sapiens (human)
positive regulation of glucose importExcitatory amino acid transporter 2Homo sapiens (human)
protein homotrimerizationExcitatory amino acid transporter 2Homo sapiens (human)
transepithelial transportExcitatory amino acid transporter 2Homo sapiens (human)
L-aspartate transmembrane transportExcitatory amino acid transporter 2Homo sapiens (human)
D-aspartate import across plasma membraneExcitatory amino acid transporter 2Homo sapiens (human)
cellular response to cocaineExcitatory amino acid transporter 2Homo sapiens (human)
monoatomic anion transmembrane transportExcitatory amino acid transporter 2Homo sapiens (human)
L-glutamate import across plasma membraneExcitatory amino acid transporter 2Homo sapiens (human)
neurotransmitter reuptakeExcitatory amino acid transporter 2Homo sapiens (human)
L-aspartate import across plasma membraneExcitatory amino acid transporter 2Homo sapiens (human)
transport across blood-brain barrierExcitatory amino acid transporter 2Homo sapiens (human)
cysteine transmembrane transportExcitatory amino acid transporter 2Homo sapiens (human)
maintenance of blood-brain barrierExcitatory amino acid transporter 3Homo sapiens (human)
blood vessel morphogenesisExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to organic cyclic compoundExcitatory amino acid transporter 3Homo sapiens (human)
behavioral fear responseExcitatory amino acid transporter 3Homo sapiens (human)
regulation of protein phosphorylationExcitatory amino acid transporter 3Homo sapiens (human)
response to amphetamineExcitatory amino acid transporter 3Homo sapiens (human)
glutathione biosynthetic processExcitatory amino acid transporter 3Homo sapiens (human)
superoxide metabolic processExcitatory amino acid transporter 3Homo sapiens (human)
monoatomic ion transportExcitatory amino acid transporter 3Homo sapiens (human)
neurotransmitter transportExcitatory amino acid transporter 3Homo sapiens (human)
intracellular zinc ion homeostasisExcitatory amino acid transporter 3Homo sapiens (human)
dopamine receptor signaling pathwayExcitatory amino acid transporter 3Homo sapiens (human)
glutamate receptor signaling pathwayExcitatory amino acid transporter 3Homo sapiens (human)
chemical synaptic transmissionExcitatory amino acid transporter 3Homo sapiens (human)
brain developmentExcitatory amino acid transporter 3Homo sapiens (human)
memoryExcitatory amino acid transporter 3Homo sapiens (human)
grooming behaviorExcitatory amino acid transporter 3Homo sapiens (human)
locomotory behaviorExcitatory amino acid transporter 3Homo sapiens (human)
response to xenobiotic stimulusExcitatory amino acid transporter 3Homo sapiens (human)
positive regulation of heart rateExcitatory amino acid transporter 3Homo sapiens (human)
gene expressionExcitatory amino acid transporter 3Homo sapiens (human)
retina layer formationExcitatory amino acid transporter 3Homo sapiens (human)
L-glutamate transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
cytokine-mediated signaling pathwayExcitatory amino acid transporter 3Homo sapiens (human)
neurogenesisExcitatory amino acid transporter 3Homo sapiens (human)
adult behaviorExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to oxidative stressExcitatory amino acid transporter 3Homo sapiens (human)
response to decreased oxygen levelsExcitatory amino acid transporter 3Homo sapiens (human)
dopamine metabolic processExcitatory amino acid transporter 3Homo sapiens (human)
cysteine transportExcitatory amino acid transporter 3Homo sapiens (human)
response to morphineExcitatory amino acid transporter 3Homo sapiens (human)
negative regulation of neuron apoptotic processExcitatory amino acid transporter 3Homo sapiens (human)
response to axon injuryExcitatory amino acid transporter 3Homo sapiens (human)
synapse organizationExcitatory amino acid transporter 3Homo sapiens (human)
L-glutamate importExcitatory amino acid transporter 3Homo sapiens (human)
righting reflexExcitatory amino acid transporter 3Homo sapiens (human)
heart contractionExcitatory amino acid transporter 3Homo sapiens (human)
long-term synaptic potentiationExcitatory amino acid transporter 3Homo sapiens (human)
motor behaviorExcitatory amino acid transporter 3Homo sapiens (human)
transepithelial transportExcitatory amino acid transporter 3Homo sapiens (human)
D-aspartate transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
L-aspartate transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
D-aspartate import across plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to ammonium ionExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to mercury ionExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to cocaineExcitatory amino acid transporter 3Homo sapiens (human)
zinc ion transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
response to anestheticExcitatory amino acid transporter 3Homo sapiens (human)
regulation of protein targeting to membraneExcitatory amino acid transporter 3Homo sapiens (human)
intracellular glutamate homeostasisExcitatory amino acid transporter 3Homo sapiens (human)
motor neuron apoptotic processExcitatory amino acid transporter 3Homo sapiens (human)
L-glutamate import across plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
neurotransmitter receptor transport to plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionExcitatory amino acid transporter 3Homo sapiens (human)
L-aspartate import across plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
transport across blood-brain barrierExcitatory amino acid transporter 3Homo sapiens (human)
chloride transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
cysteine transmembrane transportExcitatory amino acid transporter 3Homo sapiens (human)
cellular response to bisphenol AExcitatory amino acid transporter 3Homo sapiens (human)
conditioned place preferenceExcitatory amino acid transporter 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
L-glutamate transmembrane transporter activityExcitatory amino acid transporter 1Homo sapiens (human)
high-affinity L-glutamate transmembrane transporter activityExcitatory amino acid transporter 1Homo sapiens (human)
protein bindingExcitatory amino acid transporter 1Homo sapiens (human)
glutamate:sodium symporter activityExcitatory amino acid transporter 1Homo sapiens (human)
glutamate bindingExcitatory amino acid transporter 1Homo sapiens (human)
metal ion bindingExcitatory amino acid transporter 1Homo sapiens (human)
neutral L-amino acid transmembrane transporter activityExcitatory amino acid transporter 1Homo sapiens (human)
L-glutamate transmembrane transporter activityExcitatory amino acid transporter 2Homo sapiens (human)
high-affinity L-glutamate transmembrane transporter activityExcitatory amino acid transporter 2Homo sapiens (human)
protein bindingExcitatory amino acid transporter 2Homo sapiens (human)
monoatomic anion transmembrane transporter activityExcitatory amino acid transporter 2Homo sapiens (human)
glutamate:sodium symporter activityExcitatory amino acid transporter 2Homo sapiens (human)
cysteine transmembrane transporter activityExcitatory amino acid transporter 2Homo sapiens (human)
metal ion bindingExcitatory amino acid transporter 2Homo sapiens (human)
neutral L-amino acid transmembrane transporter activityExcitatory amino acid transporter 2Homo sapiens (human)
monoatomic anion channel activityExcitatory amino acid transporter 3Homo sapiens (human)
L-glutamate transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
high-affinity L-glutamate transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
protein bindingExcitatory amino acid transporter 3Homo sapiens (human)
chloride transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
L-aspartate transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
glutamate:sodium symporter activityExcitatory amino acid transporter 3Homo sapiens (human)
glutamate bindingExcitatory amino acid transporter 3Homo sapiens (human)
cysteine transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
identical protein bindingExcitatory amino acid transporter 3Homo sapiens (human)
metal ion bindingExcitatory amino acid transporter 3Homo sapiens (human)
D-aspartate transmembrane transporter activityExcitatory amino acid transporter 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
basal plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
cell surfaceExcitatory amino acid transporter 1Homo sapiens (human)
membraneExcitatory amino acid transporter 1Homo sapiens (human)
cytoplasmic vesicleExcitatory amino acid transporter 1Homo sapiens (human)
neuron projectionExcitatory amino acid transporter 1Homo sapiens (human)
neuronal cell bodyExcitatory amino acid transporter 1Homo sapiens (human)
synapseExcitatory amino acid transporter 1Homo sapiens (human)
perinuclear region of cytoplasmExcitatory amino acid transporter 1Homo sapiens (human)
membrane protein complexExcitatory amino acid transporter 1Homo sapiens (human)
plasma membraneExcitatory amino acid transporter 1Homo sapiens (human)
presynaptic membraneExcitatory amino acid transporter 2Homo sapiens (human)
plasma membraneExcitatory amino acid transporter 2Homo sapiens (human)
cell surfaceExcitatory amino acid transporter 2Homo sapiens (human)
membraneExcitatory amino acid transporter 2Homo sapiens (human)
axolemmaExcitatory amino acid transporter 2Homo sapiens (human)
vesicleExcitatory amino acid transporter 2Homo sapiens (human)
cell bodyExcitatory amino acid transporter 2Homo sapiens (human)
neuron projection terminusExcitatory amino acid transporter 2Homo sapiens (human)
membrane raftExcitatory amino acid transporter 2Homo sapiens (human)
astrocyte projectionExcitatory amino acid transporter 2Homo sapiens (human)
glutamatergic synapseExcitatory amino acid transporter 2Homo sapiens (human)
membrane protein complexExcitatory amino acid transporter 2Homo sapiens (human)
plasma membraneExcitatory amino acid transporter 2Homo sapiens (human)
plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
endoplasmic reticulumExcitatory amino acid transporter 3Homo sapiens (human)
plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
cell surfaceExcitatory amino acid transporter 3Homo sapiens (human)
membraneExcitatory amino acid transporter 3Homo sapiens (human)
apical plasma membraneExcitatory amino acid transporter 3Homo sapiens (human)
axonExcitatory amino acid transporter 3Homo sapiens (human)
dendriteExcitatory amino acid transporter 3Homo sapiens (human)
early endosome membraneExcitatory amino acid transporter 3Homo sapiens (human)
late endosome membraneExcitatory amino acid transporter 3Homo sapiens (human)
asymmetric synapseExcitatory amino acid transporter 3Homo sapiens (human)
neuronal cell bodyExcitatory amino acid transporter 3Homo sapiens (human)
synaptic cleftExcitatory amino acid transporter 3Homo sapiens (human)
dendritic spineExcitatory amino acid transporter 3Homo sapiens (human)
dendritic shaftExcitatory amino acid transporter 3Homo sapiens (human)
perikaryonExcitatory amino acid transporter 3Homo sapiens (human)
axon terminusExcitatory amino acid transporter 3Homo sapiens (human)
membrane raftExcitatory amino acid transporter 3Homo sapiens (human)
recycling endosome membraneExcitatory amino acid transporter 3Homo sapiens (human)
extracellular exosomeExcitatory amino acid transporter 3Homo sapiens (human)
cell peripheryExcitatory amino acid transporter 3Homo sapiens (human)
glial cell projectionExcitatory amino acid transporter 3Homo sapiens (human)
apical dendriteExcitatory amino acid transporter 3Homo sapiens (human)
Schaffer collateral - CA1 synapseExcitatory amino acid transporter 3Homo sapiens (human)
presynapseExcitatory amino acid transporter 3Homo sapiens (human)
perisynaptic spaceExcitatory amino acid transporter 3Homo sapiens (human)
distal dendriteExcitatory amino acid transporter 3Homo sapiens (human)
proximal dendriteExcitatory amino acid transporter 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID339905Inhibition of glutamate-induced depolarization in human EAAT2 expressed in HEK293 cells by FMP assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID196746Potential inhibitory activity of EAAT2 by the ability (250 uM) to attenuate the Na-dependent uptake of [3H]D-aspartate (5 uM) into synaptosomes of rat forebrain2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and preliminary evaluation of trans-3,4-conformationally-restricted glutamate and pyroglutamate analogues as novel EAAT2 inhibitors.
AID611792Agonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID339928Displacement of [3H]SYM2081 from rat recombinant iGluR62008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
AID611796Antagonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID179409Concentration that produces 50% displacement of [3H]-kainic acid from nerve cell membrane receptor sites1984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Palladium (II)-catalyzed olefin-coupling reactions of kainic acid: effects of substitution on the isopropenyl group on receptor binding.
AID339913Displacement of [3H]SYM2081 from rat cloned iGluR52008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID339906Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID611784Agonist activity at rat GluK2 mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID339927Displacement of [3H]SYM2081 from rat recombinant iGluR52008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
AID339929Displacement of [3H]SYM2081 from rat recombinant iGluR72008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
AID339911Displacement of CGP-39653 from KA receptor in rat synaptosomes2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID339912Displacement of CGP-39653 from NMDA receptor in rat synaptosomes2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID339915Displacement of [3H]SYM2081 from rat cloned iGluR72008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID339902Inhibition of glutamate-induced depolarization in human EAAT1 expressed in HEK293 cells by FMP assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID339914Displacement of [3H]SYM2081 from rat cloned iGluR62008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID611794Antagonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID611795Agonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID174973Comparative inhibition of L-Glutamate uptake at the concentration of 5 uM of [3H]-L- glutamate radioligand1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Conformationally defined neurotransmitter analogues. Selective inhibition of glutamate uptake by one pyrrolidine-2,4-dicarboxylate diastereomer.
AID611793Antagonist activity at non-desensitized homomeric rat GluK2 mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
AID339910Displacement of CGP-39653 from AMPA receptor in rat synaptosomes2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2000Neuron, Oct, Volume: 28, Issue:1
Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core.
AID1811Experimentally measured binding affinity data derived from PDB2000Neuron, Oct, Volume: 28, Issue:1
Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core.
AID1811Experimentally measured binding affinity data derived from PDB2005Molecular pharmacology, Mar, Volume: 67, Issue:3
Tyr702 is an important determinant of agonist binding and domain closure of the ligand-binding core of GluR2.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2005Molecular pharmacology, Mar, Volume: 67, Issue:3
Tyr702 is an important determinant of agonist binding and domain closure of the ligand-binding core of GluR2.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (178)

TimeframeStudies, This Drug (%)All Drugs %
pre-199014 (7.87)18.7374
1990's46 (25.84)18.2507
2000's65 (36.52)29.6817
2010's50 (28.09)24.3611
2020's3 (1.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.69

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 Index9.69 (24.57)
Research Supply Index5.20 (2.92)
Research Growth Index4.89 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other180 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]