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编 号：F746032
分子式：C15H18FN
分子量：231.31
分子式：C15H18FN
分子量：231.31
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CAS No: 1607589-56-9
产品详情
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.
体内研究：
NMDA receptor antagonist 4 (IIc) (0-10 μM) rescues the motor deficits, and protects against Aβ toxicity-related neuronal dysfunction.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.Animal Model:C. elegans (N2 wild-type, CL2006, CL2122, CL2355)
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
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.
体外研究：
NMDA receptor antagonist 4 (IIc) shows competitive interaction with endogenous blocker Mg2+, and shows dependence on membrane potential in the NMDAR channel.NMDA receptor antagonist 4 shows high metabolic stability in human and mice liver microsomes, and shows hERG safety, without obvious cytotoxicity.
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.
体内研究：
NMDA receptor antagonist 4 (IIc) (0-10 μM) rescues the motor deficits, and protects against Aβ toxicity-related neuronal dysfunction.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.Animal Model:C. elegans (N2 wild-type, CL2006, CL2122, CL2355)
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
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.
体外研究：
NMDA receptor antagonist 4 (IIc) shows competitive interaction with endogenous blocker Mg2+, and shows dependence on membrane potential in the NMDAR channel.NMDA receptor antagonist 4 shows high metabolic stability in human and mice liver microsomes, and shows hERG safety, without obvious cytotoxicity.
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