Description
Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na
+ channels (ED
50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED
50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals at an ED
50 value of 4 mg/kg. Formulations containing riluzole have been explored as therapeutics for slowing disease progression of amyotrophic lateral sclerosis.
Uses
Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals at an ED50 value of 4 mg/kg. Riluzole has been explored as a therapeutic for slowing disease progression of amyotrophic lateral sclerosis.