Recent Advances in the Development of NR2B Subtype-Selective NMDA Receptor Antagonists

Author(s): Mark E. Layton, Michael J. Kelly III, Kevin J. Rodzinak

Journal Name: Current Topics in Medicinal Chemistry

Volume 6 , Issue 7 , 2006

Become EABM
Become Reviewer


Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which have shown efficacy without the side effects observed with nonspecific NMDA antagonists. Classical ifenprodil-like molecules containing benzyl- and phenylpiperidines attached to a phenol or an appropriate isostere by a linker have provided valuable chemical leads as potential therapeutic agents. In this review, recent efforts in the discovery and development of structurally unique NR2B subtype-selective NMDA antagonists that do not fit the classical "ifenprodil-like" pharmacophore will be discussed.

Keywords: NMDA, subtype-selective, NR2B, antagonist, review

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2006
Page: [697 - 709]
Pages: 13
DOI: 10.2174/156802606776894447
Price: $65

Article Metrics

PDF: 16