Synonym: Rilutek, PK-26124, RP-54274
Riluzole is a compound 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 45 mg/mL
Ethanol 45 mg/mL
Quantitative estimation of riluzole in human plasma by LC-ESI-MS/MS and its application to a bioequivalence study.
Chandu BR, et al. Anal Bioanal Chem. 2010 Oct;398(3):1367-74. PMID: 20683584.
Riluzole rapidly attenuates hyperemotional responses in olfactory bulbectomized rats, an animal model of depression.
Takahashi K, et al. Behav Brain Res. 2011 Jan 1;216(1):46-52. PMID: 20620171.
Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1.
Fumagalli E, et al. Eur J Pharmacol. 2008 Jan 14;578(2-3):171-6. PMID: 18036519.
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