Riluzole Inhibitor CAS No. 1744-22-5

Cat. No.	Name	Size	Price	Add Cart
KI0988	Riluzole	50 mg	$154

Chemical Characteristic

Product Name	Riluzole
Synonyms	Rilutek
CAS No.	1744-22-5
Molecular Weight	234.2
Formula	C₈H₅F₃N₂OS
Chemical Name	6-?(trifluoromethoxy)?-2-?benzothiazolamine
Smiles	Nc1sc2c(n1)ccc(c2)OC(F)(F)F
Chemical Structure

Biological activities

Riluzole is a novel agent that exhibits a broad spectrum of actions (anticonvulsive, neuroprotective, anesthetic, anxiolytic) in the central nervous system. At the postsynaptic level, riluzole blocks the responses mediated by excitatory amino acids. At the presynaptic level, riluzole blocks the release of glutamate and the reuptake of GABA. At both sites, riluzole stabilizes the inactivated state of the sodium voltage-dependent channels. Riluzole at 25 and 100 µM significantly antagonizes the increase in cGMP formation induced by glutamate (1 mM) and quisqualate (0.1 mM).^[1] Riluzole inhibits both glutamate secretion and glutamate-induced postsynaptic responses via G protein-dependent events. At glutamate receptors expressed in Xenopus oocytes and at native glutamate receptors in cerebellar granule cells, riluzole attenuates cation influx elicited by N-methyl-D-aspartate (NMDA) and kainate with IC50s of 12.8-18.2 and 167 µM, respectively.^[2] Riluzole (0.1-100 µM) increases Na⁺-dependent _{L-[³H]glutamate uptake in rat cortical synaptosomes in a dose-dependent manner.^[3]}

Protocols

Riluzole is dissolved (10?) in assay buffer with 20% absolute ethanol, then diluted to working concentrations using assay buffer with 2% absolute ethanol.^[3]

References

[1] Mantz J, et al. Riluzole. CNS Drug Reviews. 1996, 2(1): 40-51. [2] Yokoo H, et al. Selective inhibition by riluzole of voltage-dependent sodium channels and catecholamine secretion in adrenal chromaffin cells. Naunyn Schmiedebergs Arch Pharmacol. 2998, 357 (5): 526-531. [3] Fumagalli E, et al. Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1. Eur J Pharmacol. 2008, 578 (2-3): 171-176.

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