2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NMDA receptor antagonist 4

NMDA receptor antagonist 4 (IIc) 是一个非竞争性、电压依赖的、具有口服活性的 NMDAR 阻断剂，其 IC50 值为1.93 µM。NMDA receptor antagonist 4 可透过血脑屏障，能被用于研究阿兹海默症 (Alzheimer's disease)。

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NMDA receptor antagonist 4 Chemical Structure

NMDA receptor antagonist 4 Chemical Structure

CAS No. : 1607589-56-9

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NMDA receptor antagonist 4 相关抗体

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  • 生物活性

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生物活性

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].

IC50 & Target

IC50: 1.93 µM (NMDAR)[1]
体外研究
(In Vitro)

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].

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

NMDA receptor antagonist 4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Neuro2A cells
Concentration: 1, 10, and 100 µM
Incubation Time: 24 h
Result: Did not show cytotoxic at the highest concentration tested (100 µM).
体内研究
(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].

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

Animal Model: C. elegans (N2 wild-type, CL2006, CL2122, CL2355)[1]
Dosage: 0, 0.1, 0.5, 1.5, and 10 µM
Administration:
Result: Reduced defective locomotion in CL2006 nematodes. Significantly reversed the chemotaxis behavior of CL2355 nematodes disrupted by Aβ expression.
Animal Model: Six months old female 5XFAD mice[1]
Dosage: 5 mg/kg/day
Administration: Oral administration, 4 weeks
Result: Enhanced working memory function. Rescued the expression of GluN2A and postsynaptic density protein (PSD) 95. Increased Fyn phosphorylated levels and correspondingly elevated GluN2B phosphorylation at Tyr1472. Significantly increased p-CREB protein levels in the nucleus. Reverted calbindin D-28K protein levels.
分子量

231.31

Formula

C15H18FN
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NMDA receptor antagonist 4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

NMDA receptor antagonist 41607589-56-9NMDA receptor antagonist4NMDA receptor antagonist-4iGluRIonotropic glutamate receptorsC. elegans5XFADMemantine analogsInhibitorinhibitorinhibit

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