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To date, drugs targeting NMDARs have had only limited success clinically The strong depolarization required to remove Mg block from synaptically The permeation pathway of the NMDAR is formed by two NR1 and two NR2 subunits (A). LBDs to the ion channel portion of the receptor is free to change conformation.

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NCBI Bookshelf. Van Dongen AM, editor. Marie L. Blanke and Antonius M. NMDA receptors NMDARs are glutamate-gated cation channels with high calcium permeability that play important roles in many aspects of the biology of higher organisms. They are critical for the development of the central nervous system CNS , generation of rhythms for breathing and locomotion, and the processes underlying learning, memory, and neuroplasticity.

Consequently, abnormal expression levels and altered NMDAR function have been implicated in numerous neurological disorders and pathological conditions.

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