NR2B Selective NMDA Receptor Antagonists

Author(s): Sham S. Nikam , Leonard T. Meltzer .

Journal Name: Current Pharmaceutical Design

Volume 8 , Issue 10 , 2002


NR2B antagonists have received considerable attention in recent years. In this class of excitatory amino acid receptor antagonists NR2B antagonists have shown efficacy in neuroprotection, anti-hyperalgesic and anti-Parkinson animal models. Several groups are involved in developing these compounds as therapeutic agents and evaluating newer therapeutic targets for these agents. Until recently benzylpiperidine and phenylpiperidine templates, which were based on the structures of Ifenprodil and Eliprodil, formed the basis of most SAR in this area. A few chemical leads in this class such as CP-101,606, Ro25,6981 and PD0196860 have been identified as possible development leads which have generated significant interest in this area. In addition to the efforts of Pfizer (Parke-Davis), Roche and E.Merck, several other industrial and academic research groups have continued to work in the NR2B area and recently Merck and Roche have reported new chemical leads as NR2B antagonists with significantly different biaryl templates. These new advances have raised hope, for potential success of the NR2B antagonists as new therapeutic agents, for the treatment of several pathophysiological indications.

Keywords: nr2b antagonists, acyclic amines, piperidines, phenyl piperidines, benzoxazolone, parkinsons disease

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Article Details

Year: 2002
Page: [845 - 855]
Pages: 11
DOI: 10.2174/1381612024607072
Price: $58

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