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NMDAR/TRPM4-IN-2

Names

[ CAS No. ]:
2243506-33-2

[ Name ]:
NMDAR/TRPM4-IN-2

Biological Activity

[Description]:

NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR
Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Signaling Pathways >> MAPK/ERK Pathway >> ERK
Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Signaling Pathways >> Stem Cell/Wnt >> ERK

[In Vitro]

NMDAR/TRPM4-IN-2 (compound 8) (0-10 μM) reduces the interactions of GluN2A and GluN2B with TRPM4 in a dose-dependent manner[1]. NMDAR/TRPM4-IN-2 eliminates the CREB shutoff pathway and restores ERK1/2 activation and IEG induction while sparing the synaptic activity-driven, transcription-promoting activities of NMDARs[1].

[References]

[1]. Yan J, et al. Coupling of NMDA receptors and TRPM4 guides discovery of unconventional neuroprotectants. Science. 2020 Oct 9;370(6513):eaay3302.  

Chemical & Physical Properties

[ Molecular Formula ]:
C11H19BrCl2N2

[ Molecular Weight ]:
330.09

Related Compounds