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

被引：192

作者：

Fumagalli, Elena ^{[1
]}

Funicello, Marcella ^{[1
]}

Rauen, Thomas ^{[2
]}

Gobbi, Marco ^{[1
]}

Mennini, Tiziana ^{[1
]}

机构：

[1] Ist Ric Farmacol Mario Negri, I-20156 Milan, Italy

[2] Univ Osnabruck, Fachbereich Biol Chem, Biophys Abt, D-49076 Osnabruck, Germany

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2008年 / 578卷 / 2-3期

关键词：

riluzole; glutamate; transporter; uptake; cell lines; synaptosomes;

D O I：

10.1016/j.ejphar.2007.10.023

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：171 / 176

页数：6

共 28 条

[21] A novel neuroprotective mechanism of riluzole: Direct inhibition of protein kinase C [J].