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.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NMDA Receptor |
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.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NMDAR blocker 1 Related Classifications
HY-131691 Related Classifications
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