Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1

Elena Fumagalli, Marcella Funicello, Thomas Rauen, Marco Gobbi, Tiziana Mennini

Research output: Contribution to journalArticle

Abstract

Riluzole exerts a neuroprotective effect through different mechanisms, including action on glutamatergic transmission. We investigated whether this drug affects glutamate transporter-mediated uptake, using clonal cell lines stably expressing the rat glutamate transporters GLAST, GLT1 or EAAC1. We found that riluzole significantly increased glutamate uptake in a dose-dependent manner; kinetic analysis indicated that the apparent affinity of glutamate for the transporters was significantly increased, with similar effects in the three cell lines. This may facilitate the buffering of excessive extracellular glutamate under pathological conditions suggesting that riluzole's neuroprotective action might be partly mediated by its activating effect on glutamate uptake.

Original languageEnglish
Pages (from-to)171-176
Number of pages6
JournalEuropean Journal of Pharmacology
Volume578
Issue number2-3
DOIs
Publication statusPublished - Jan 14 2008

Keywords

  • Cell lines
  • Glutamate transporter
  • Riluzole
  • Synaptosomes
  • Uptake

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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