Home Transmembrane Transporters Sodium Channel inhibitor - GluR antagonist Riluzole For research use only.

Riluzole

Synonyms: RP-54274, PK 26124

Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

Riluzole Chemical Structure

Riluzole Chemical Structure

CAS: 1744-22-5

Selleck's Riluzole has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.88%
99.88

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Biological Activity

Description Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Targets
Sodium channel [1] NMDA receptor [1] Glutamate release [2]
In vitro
In vitro Riluzole inhibits the release of glutamic acid from cultured neurons, and from brain slices. These effects may be partly due to inactivation of voltage-dependent sodium channels on glutamatergic nerve terminals, as well as activation of a G-protein-dependent signal transduction process. Electrophysiologic experiments performed on isolated excitatory amino acid receptors expressed in the Xenopus oocyte have revealed that Riluzole inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). Riluzole has been shown to stabilize inactivated sodium channels in frog sciatic nerve, in rat cerebellar granule cells, and on recombinant rat sodium channels expressed in Xenopus oocytes (Ki = 0.2 μM). Riluzole also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. Tiluzole 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. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT p-Smad2 / Smad2 / p-Smad3 / Smad3 23077590
In Vivo
In vivo Riluzole can easily cross the blood-brain barrier. Riluzole has neuroprotective, anticonvulsant, and sedative properties in vivo. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed by Riluzole treatment (8 mg/kg i.p.). [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05292209 Recruiting Atrial Fibrillation Paroxysmal University of Utah|Ohio State University June 15 2022 Phase 2
NCT04819438 Completed Bioequivalence Cross Research S.A.|Zambon SpA January 15 2021 Phase 1
NCT02859792 Recruiting Spinal Cord Injury Assistance Publique Hopitaux De Marseille May 27 2019 Phase 2
NCT04630444 Completed Posttraumatic Stress Disorder Mclean Hospital|Brain & Behavior Research Foundation March 16 2017 Early Phase 1
NCT02238626 Completed Amyotrophic Lateral Sclerosis MediciNova|Wake Forest University Health Sciences September 2014 Phase 2

Chemical lnformation & Solubility

Molecular Weight 234.2 Formula

C8H5F3N2OS
CAS No. 1744-22-5 SDF Download Riluzole SDF
Smiles C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 47 mg/mL ( (200.68 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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