NMDAR blocker 1
NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases.
For research use only. We do not sell to patients.
- CAS No.: 76991-05-4
- Formula: C17H20N2O
- Molecular Weight:268.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NMDA Receptor |
In Vitro
NMDAR blocker 1 (Compound N20C) (5-500 μM) potently and selectively inhibits rat NR1/NR2A NMDA receptor channel activity in Xenopus laevis oocytes with an IC50 of 5.0 ± 0.2 μM[1].
NMDAR blocker 1 (0.1-100 μM; 4 h) protects primary rat cerebellar and hippocampal neuron cultures from excitotoxic death, with maximal 85 ± 6% survival of cerebellar neurons at 30 μM[1].
NMDAR blocker 1 (0.01-30 μM; 5 min) dose-dependently inhibits NMDA-induced cGMP formation in primary rat cerebellar neurons[1].
NMDAR blocker 1 (0.01-100 μM; 10 min) potently blocks NMDA-induced intracellular Ca2+ overload in primary rat cerebellar neurons, with complete inhibition at 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ammonia-induced Swiss mice (male, 25-35 g)[1]
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Dosage:5 μg/g; 10 μg/g; 30 μg/g; 50 μg/g
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Administration:i.p.; single dose
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Result:Increased survival rate.
Caused no conspicuous behavioral or motor deficits in treated animals.
Chemical Information
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CAS No. 76991-05-4
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Molecular Weight 268.36
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Formula C17H20N2O
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SMILES
O=C(N)CNCCC(C=1C=CC=CC1)C=2C=CC=CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
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Primary Embryonic Hippocampal Neuron Culture
Primary embryonic hippocampal neuron culture is an in vitro method in which hippocampi from embryonic rodents are dissected, enzymatically or mechanically dissociated, plated on adhesive substrates, and maintained in defined neuronal medium or in low-density sandwich/co-culture formats to support neuronal attachment, neurite extension, polarity formation, dendritic arborization, and synapse formation. The main readouts are cell survival, neuronal purity, neurite outgrowth, axon-dendrite polarization, synaptic marker development, and functional neuronal activity, assessed by phase-contrast microscopy, immunocytochemistry for neuronal/glial markers, live imaging, or electrophysiology depending on the downstream experiment.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)