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Author Notes:

The authors would like to thank D Menaldino and F Menniti for their comments and suggestions, and also P Burger for his assistance in generating Figure 1.

Declaration of Interest: Some of the authors (KL Strong, Y Jing, AR Prosser, SF Traynelis, DC Liotta) are inventors on Emory-owned IP involving NMDA receptor modulators. Authors have an equity position (SF Traynelis, DC Liotta), are Board members (DC Liotta), and are paid consultants (SF Traynelis) for NeurOp, Inc., a company that is developing NMDA receptor modulators.

Subjects:

Research Funding:

This work was supported by the NIH (NS036654, NS065371 SFT).

Keywords:

  • Science & Technology
  • Life Sciences & Biomedicine
  • Chemistry, Medicinal
  • Pharmacology & Pharmacy
  • channel blockers
  • deuterated analogs
  • glycine site antagonists
  • glycine transport inhibitors
  • NMDA receptor subunit-selective antagonists
  • NMDA receptor subunit-selective positive modulators
  • D-ASPARTATE RECEPTORS
  • PROTEIN-KINASE-C
  • POSITIVE ALLOSTERIC MODULATORS
  • LONG-TERM POTENTIATION
  • SUBUNIT MESSENGER-RNAS
  • SITE PARTIAL AGONIST
  • SPINAL-CORD NEURONS
  • SICKLE-CELL-DISEASE
  • LOW-DOSE KETAMINE

NMDA receptor modulators: an updated patent review (2013-2014)

Tools:

Journal Title:

Expert Opinion on Therapeutic Patents

Volume:

Volume 24, Number 12

Publisher:

, Pages 1349-1366

Type of Work:

Article | Post-print: After Peer Review

Abstract:

Introduction: The NMDA receptor mediates a slow component of excitatory synaptic transmission, and NMDA receptor dysfunction has been implicated in numerous neurological disorders. Thus, interest in developing modulators that are capable of regulating the channel continues to be strong. Recent research has led to the discovery of a number of compounds that hold therapeutic and clinical value. Deeper insight into the NMDA intersubunit interactions and structural motifs gleaned from the recently solved crystal structures of the NMDA receptor should facilitate a deeper understanding of how these compounds modulate the receptor. Areas covered: This article discusses the known pharmacology of NMDA receptors. A discussion of the patent literature since 2012 is also included, with an emphasis on those that claimed new chemical entities as regulators of the NMDA receptor. Expert opinion: The number of patents involving novel NMDA receptor modulators suggests a renewed interest in the NMDA receptor as a therapeutic target. Subunit-selective modulators continue to show promise, and the development of new subunit-selective NMDA receptor modulators appears poised for continued growth. Although a modest number of channel blocker patents were published, successful clinical outcomes involving ketamine have led to a resurgent interest in low-affinity channel blockers as therapeutics.

Copyright information:

© 2014 Informa UK, Ltd.

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