Riluzole
Sodium channel blocker / Neuroprotective / Riluzole is a clinically useful drug for the treatment of amyotrophic lateral sclerosis (ALS).1 Riluzole inhibits glutamate release via inactivation of voltage-dependent ion channels, effects expression and signal transduction of glutamate receptors, and facilitates glutamate uptake.2,3,4 It has also been investigated as a treatment for depression and anxiety.5 Riluzole induced apoptosis in mGluR1-expressing melanoma cells6, inhibited cell proliferation in a U87MG glioblastoma model via blockage of glutamate release7, and inhibited the growth of brain tumor stem-like cells via downregulation of GLUT3.
Biochemicals & reagents
1744-22-5
1) Bellingham (2011), A review of the neural mechanisms of action and clinical efficiency of riluzole in treating amyotrophic lateral sclerosis: what have we learned in the last decade; CNS Neurosci. Ther. 17 4 2) Urbani and Belluzzi (2000), Riluzole inhibits the persistent sodium current in mammalian CNS neurons; Eur.J.Neurosci. 12 3567 3) Frizzo et al. (2004), Riluzole enhances glutamate uptake in rat astrocyte cultures; Cell Mol. Neurobiol. 24 123 4) Doble (1996), The pharmacology and mechanism of action of riluzole; Neurology 47 S233 5) Pittenger et al. (2008), Riluzole in the treatment of mood and anxiety disorders; CNS Drugs 22 761 6) Namkoong et al. (2007), Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma; Cancer Res. 67 2298 7) Zhang et al. (2015), Anti-cancer effect of metabotropic glutamate receptor inhibition in human glioma U87 cells: involvement of PI3K/Akt/mTOR pathway; Cell Physiol. Biochem. 35 419 8) Sperling et al. (2017), Riluzole: a potential therapeutic intervention in human brain tumor stem-like cells; Oncotarget 8 96697
RT
TARGET: Ion channel -- PATHWAY: Proliferation; Sodium channel; Apoptosis inducer -- RESEARCH AREA: Cancer Stem Cells; Neuroscience; Cell death -- DISEASE AREA: Mood disorders