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 No. 1744-22-5

Purity & Quality Control

Riluzole Related Products

Signaling Pathway

Sodium Channel Signaling Pathways

Sodium Channel Signaling Pathway

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
NCT06270108 Recruiting
Treatment-resistant Schizophrenia|Treatment-responsive Schizophrenia|Healthy Controls
King''s College London|South London and Maudsley NHS Foundation Trust
 November 14 2022 Early Phase 1
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

Chemical Information & 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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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.

Handling Instructions

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