Riluzole

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Description

Riluzole is a drug used to treat amyotrophic lateral sclerosis. Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with damaged neurons. This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors. Riluzole (Rilutek) inhibits glutamate release from presynaptic terminals and increases Na+-dependent glutamate uptake in rat cortical synaptosomes. It blocks voltage-dependent Na+ channels and inhibits GABA uptake by striatal synaptosomes; neuroprotective. Riluzole protects cultured neurons from anoxic damage, from the toxic effects of glutamic-acid-uptake inhibitors, and from the toxic factor in the CSF of patients with amyotrophic lateral sclerosis in vitro. In vivo, riluzole has neuroprotective, anticonvulsant, and sedative properties. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed. Research shows that Riluzole (Rilutek) activates the TREK family of potassium channels and directly affects the glutamatergic system.

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