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

Autor(en): Fumagalli, Elena
Funicello, Marcella
Rauen, Thomas
Gobbi, Marco
Mennini, Tiziana
Stichwörter: AMYOTROPHIC-LATERAL-SCLEROSIS; cell lines; CENTRAL-NERVOUS-SYSTEM; glutamate; HIGH-AFFINITY; INHIBITION; MECHANISM; MODULATION; NEURONS; NEUROPROTECTIVE AGENT RILUZOLE; Pharmacology & Pharmacy; riluzole; SODIUM; SPINAL-CORD; synaptosomes; transporter; uptake
Erscheinungsdatum: 2008
Herausgeber: ELSEVIER SCIENCE BV
Journal: EUROPEAN JOURNAL OF PHARMACOLOGY
Volumen: 578
Ausgabe: 2-3
Startseite: 171
Seitenende: 176
Zusammenfassung: 
Riluzole exerts a neuroprotective effect through different mechanisms, including action on glutamatergic transmission. We investigated whether this drug affects glatamate 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. (C) 2007 Elsevier B.V. All rights reserved.
ISSN: 00142999
DOI: 10.1016/j.ejphar.2007.10.023

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