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Cognitive enhancers, also known as "smart drugs," are substances used to enhance memory, mental alertness, and concentration. These can be natural or synthetic and improve cognition in conditions like Alzheimer's disease (AD) and other neurodegenerative diseases. Some common examples include caffeine, amphetamines, methylphenidate, modafinil, arecoline, donepezil, vortioxetine, and piracetam. These enhancers work on the principle of synaptic plasticity and altered circuit function. They...
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Novel NMDA receptor modulators: an update.

Rose M Santangelo1, Timothy M Acker, Sommer S Zimmerman

  • 1Emory University, Department of Chemistry, Atlanta, GA 30322, USA.

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NMDA receptor antagonists show promise for neurological conditions like Alzheimer's and depression. Further research into NMDA receptor pharmacology is key for developing new therapeutic strategies.

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Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • The N-methyl-D-aspartate (NMDA) receptor is a crucial ligand-gated ion channel in brain function.
  • It is implicated in neurological and psychiatric disorders, with recent NMDA receptor antagonist success in conditions beyond neuroprotection.

Purpose of the Study:

  • To review NMDA receptor pharmacology and function.
  • To discuss pre-clinical and clinical relevance.
  • To highlight advancements in targeting NMDA receptors since 2010 through patent literature.

Main Methods:

  • Review of NMDA receptor pharmacology and function.
  • Discussion of pre-clinical and clinical data.
  • Patent literature review focusing on NMDA receptor targets since 2010.

Main Results:

  • NMDA receptor antagonists are showing clinical promise in diverse indications.
  • Understanding NMDA receptor structure and function is improving.
  • New therapeutic strategies are emerging, focusing on potentiators and subunit-selective agents.

Conclusions:

  • Increased understanding of NMDA receptors offers new therapeutic avenues.
  • Further development of novel strategies and technologies is required for clinical success.
  • Future approaches emphasize potentiators, subunit-selective agents, and minimizing off-target effects.