Home Transmembrane Transporters Sodium Channel inhibitor - GluR antagonist Riluzole (PK 26124)

Riluzole (PK 26124)

Catalog No.S1614 Synonyms: RP-54274

For research use only.

Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.

Riluzole (PK 26124) Chemical Structure

CAS No. 1744-22-5

Selleck's Riluzole (PK 26124) has been cited by 10 Publications

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Biological Activity

Description Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Targets
Sodium channel [1] NMDA receptor [1] Glutamate release [2]
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]
Assay
Methods Test Index PMID
Western blot p-AKT / AKT ; p-Smad2 / Smad2 / p-Smad3 / Smad3 23077590
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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 234.2
Formula

C8H5F3N2OS
CAS No. 1744-22-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04819438 Completed Drug: Riluzole 50 mg Oral Film|Drug: Rilutek 50Mg Tablet Bioequivalence Cross Research S.A.|Zambon SpA January 15 2021 Phase 1
NCT02859792 Unknown status Drug: Riluzole|Drug: Placebo|Biological: Blood Samples Spinal Cord Injury Assistance Publique Hopitaux De Marseille May 2019 Phase 2
NCT04630444 Completed Drug: Riluzole Posttraumatic Stress Disorder Mclean Hospital|Brain & Behavior Research Foundation March 16 2017 Early Phase 1
NCT02238626 Completed Drug: Placebo (for MN-166)|Drug: MN-166|Drug: riluzole Amyotrophic Lateral Sclerosis MediciNova|Atrium Health September 2014 Phase 2
NCT01661855 Completed Drug: Riluzole|Drug: Placebo Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|The Hospital for Sick Children|University of Western Ontario Canada|Unity Health Toronto|University of Toronto|Anagnostou Evdokia M.D. September 2013 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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