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^[1].

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.

NMDAR blocker 1 (Compound N20C) (5-50 μg/g; i.p.; single dose) provides dose-dependent in vivo neuroprotection against acute ammonia-induced excitotoxicity in male Swiss mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

268.36

C₁₇H₂₀N₂O

76991-05-4

O=C(N)CNCCC(C=1C=CC=CC1)C=2C=CC=CC2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Planells-Cases R, et al. A novel N-methyl-D-aspartate receptor open channel blocker with in vivo neuroprotectant activity. J Pharmacol Exp Ther. 2002;302(1):163-173.  [Content Brief]