Amide-containing NR2B/NMDA receptor antagonists

Abstract

Discovery of the NR2A-D subtypes of the NMDA receptor and of an allosteric binding site on the NR2B receptor subunit has renewed interest in the therapeutic potential of NMDA receptor antagonists for a variety of CNS disease states. Recently, there has been a significant interest in increasing the selectivity of NR2B compounds versus hERG activity. This article will focus on a recent series of NR2B antagonists from Pfizer that show good selectivity over dofetilide binding.

Keywords::

• glutamate
• hERG
• NMDA
• NR2B antagonist

Patent Details

• Title Therapeutic amide derivatives

• Assignee Pfizer Inc

• Inventors Kawai M, Kawamura M, Sakurada I, Morita A

• Priority date 11/02/2004

• Filing date 01/02/2005

• Publication date 01/09/2005

• Publication no. WO2005080317