title: NMDA receptor modulators: an updated patent review (2013-2014).
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Emory University, Department of Chemistry , 1521 Dickey Drive, Atlanta, GA 30322 , USA dliotta@emory.edu.
authors.forename: Katie L
authors.initials: KL
authors.lastname: Strong
authors.forename: Yao
authors.initials: Y
authors.lastname: Jing
authors.forename: Anthony R
authors.initials: AR
authors.lastname: Prosser
authors.forename: Stephen F
authors.initials: SF
authors.lastname: Traynelis
authors.forename: Dennis C
authors.initials: DC
authors.lastname: Liotta
mesh_terms: D000818:Animals; D001665:Binding Sites; D002118:Calcium / Q000378:metabolism; D006801:Humans; D010330:Patents as Topic; D016194:Receptors, N-Methyl-D-Aspartate / Q000737:chemistry / Q000187:drug effects* / Q000502:physiology
chemical_list: D016194:Receptors, N-Methyl-D-Aspartate; D002118:Calcium
keywords: NMDA receptor subunit-selective antagonists; NMDA receptor subunit-selective positive modulators; channel blockers; deuterated analogs; glycine site antagonists; glycine transport inhibitors