2-Styryl-pyridines and 2-(3,4-Dihydro-naphthalen-2-yl)pyridines as Potent NR1/2B Subtype Selective NMDA Receptor Antagonists

Authors

  • Bernd Buettelmann
  • Alexander Alanine
  • Anne Bourson
  • Ramanjit Gill
  • Marie-Paule Heitz
  • Vincent Mutel
  • Emmanuel Pinard
  • Gerhard Trube
  • René Wyler

DOI:

https://doi.org/10.2533/000942904777677579

Keywords:

Neurodegeneration, Nmda, Nr1/2b antagonists, Structure-activity relationship

Abstract

A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. ?1 and M1 receptors) and are active in vivo .

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Published

2004-09-01