Page last updated: 2024-12-10

mdl 100453

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

Description

4-oxo-5-phosphononorvaline: structure given in first source; competitive glutamate antagonist at the NMDA receptor complex; RN given refers to (R)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3035602
CHEMBL ID431029
SCHEMBL ID195547
MeSH IDM0181931

Synonyms (16)

Synonym
mdl 100453
CHEMBL431029 ,
mdl-100483
(2r)-2-amino-4-oxo-5-phosphonopentanoic acid
(r)-2-amino-4-oxo-5-phosphono-pentanoic acid
bdbm50010893
2-amino-4-oxo-5-phosphono-pentanoic acid
d-norvaline, 4-oxo-5-phosphono-
129938-34-7
4-opnv
mdl-100,453
4-oxo-5-phosphononorvaline
SCHEMBL195547
(r)-4-oxo-5-phosphononorvaline
mdl 100,453
DTXSID80926532

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" The aim of the present study was to measure the dose-response of cerebral infarcted volume to the agent administered 30 min after permanent middle cerebral artery occlusion and to test whether short-term infusion of this drug reduces ischemic cell damage."( Administration of a competitive NMDA antagonist MDL-100,453 reduces infarct size after permanent middle cerebral artery occlusion in rat.
Baron, BM; Chopp, M; Jiang, N; Zhang, RL, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki100.00000.00000.41052.7800AID92947
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki100.00000.00380.79754.1000AID91469
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)0.11000.00071.630610.0000AID241940
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID241940Inhibition of [3H]CPP binding to rat N-methyl-D-aspartic acid receptor 2A2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit.
AID180480Percent inhibition of glutamate activity against cGMP was determined1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID242397Inhibition of [3H]Glu binding to rat N-methyl-D-aspartic acid receptor; nd=not determined2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit.
AID143309In vitro binding affinity towards N-methyl-D-aspartate glutamate receptor of the glutamate receptor using [3H]CPP as radioligand in rat cerebral cortical membranes.1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID91469Binding affinity towards Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID92947Binding affinity towards AMPA receptor using [3H]AMPA as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (87.50)18.2507
2000's1 (12.50)29.6817
2010's0 (0.00)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 Index2.20 (2.92)
Research Growth Index4.17 (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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]