An NMDA receptor antagonist
Memantine hydrochloride is an antagonist of NMDA receptor with IC50 values of 0.93μM, 0.82μM and 0.47μM for NRIa/NR2A, NRIa/NR2B and NRIa/NR2D, respectively [1].
Memantine is an uncompetitive NMDA receptor antagonist. When using HEK293 cells express recombinant rat NMDA receptors, memantine shows inhibition of L-glutamate-mediated response with a dose- and voltage-dependent manner. Memantine also has a rapid unblocking kinetics [1].
Memantine is used clinically in spasticity, Parkinson's disease and Alzheimer’s disease. Memantine is found to attenuate the deleterious action of Aβ in the in vitro numerous studies. It is probably due to the decreased tau phosphorylation caused by memantine [2].
参考文献:
[1] Bresink I, Benke T A, Collett V J, et al. Effects of memantine on recombinant rat NMDA receptors expressed in HEK 293 cells. British journal of pharmacology, 1996, 119(2): 195-204.
[2] Danysz W, Parsons C G. Alzheimer's disease, β-amyloid, glutamate, NMDA receptors and memantine–searching for the connections. British journal of pharmacology, 2012, 167(2): 324-352.
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