ABSTRACT

N-methyl-d-aspartate (NMDA) receptor is a subtype of ionotropic glutamate receptor. NMDA receptor plays a decisive role in significant high-level brain processes and has been involved in diverse neuropsychological conditions. NMDA receptor antagonists have exposed their clinical effectiveness in neurodegenerative diseases such as epilepsy, Alzheimer’s disease, Parkinson’s disease, pain, and depression. Depending on the clinical observations and insights into NMDA receptor pharmacology, novel modulatory approaches are beginning to emerge with potential therapeutic benefits. Hence, NMDA receptor is considered to be a prospective target for the treatment of neurodegenerative diseases. NMDA receptor has diverse sites where ligands can bind to provoke bioactivity in a subunit selective manner; the recent pharmacological data also disclosed molecular determinants for their subunit selectivity. By addressing the role of NMDA receptor modulators in neuropsychological consequences, we would certainly be a step closer to a goal of improving the quality of life of individuals suffered from neurodegenerative diseases. We discussed more recent results and significance of subunit selective NMDA receptor ligands, which have proven to be antagonists that are particularly useful in the management of neurological diseases. A flurry of clinical, functional, and chemical studies summarized in this chapter reinvigorated efforts to identify subunit selective modulators of NMDA receptor as initial proof-of-concept molecules to treat neurodegenerative diseases.