NMDA receptor antagonist 4_product_DataBase

Bioactivity	NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease[1].
Target	IC50: 1.93 µM (NMDAR)
Invitro	NMDA receptor antagonist 4 (IIc) shows competitive interaction with endogenous blocker Mg2+, and shows dependence on membrane potential in the NMDAR channel[1].NMDA receptor antagonist 4 shows high metabolic stability in human and mice liver microsomes, and shows hERG safety, without obvious cytotoxicity[1]. Cell Cytotoxicity Assay[1] Cell Line:
In Vivo	NMDA receptor antagonist 4 (IIc) (0-10 µM) rescues the motor deficits, and protects against Aβ toxicity-related neuronal dysfunction[1].NMDA receptor antagonist 4 (5 mg/kg/day; p.o.; 4 weeks) improves cell survival and synaptic function in AD through increasing the activity of cell-survival signaling pathways (Fyn-GluN2B-CREB signaling) and preventing internalization of synaptic NMDARs[1]. Animal Model:
Name	NMDA receptor antagonist 4
CAS	1607589-56-9
Formula	C15H18FN
Molar Mass	231.31
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Andreea L. Turcu, et al. Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease. Eur J Med Chem. 2022 Apr 8;236:114354.

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