NMDA receptor antagonist 4
Modify Date: 2024-01-08 01:20:50
NMDA receptor antagonist 4 structure
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Common Name | NMDA receptor antagonist 4 | ||
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| CAS Number | 1607589-56-9 | Molecular Weight | 231.31 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C15H18FN | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of NMDA receptor antagonist 4NMDA 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]. |
| Name | NMDA receptor antagonist 4 |
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| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 1.93 µM (NMDAR)[1] |
| 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]. 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). |
| 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: 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. |
| References |
| Molecular Formula | C15H18FN |
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| Molecular Weight | 231.31 |