Riluzole (PK 26124)

For research use only.

Catalog No.S1614 Synonyms: RP-54274

7 publications

Riluzole (PK 26124) Chemical Structure

CAS No. 1744-22-5

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

Selleck's Riluzole (PK 26124) has been cited by 7 publications

2 Customer Reviews

  • Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (*p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (*p≤0.036). c Swim Speed. Aged rats swam the most slowly (*p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (*p<0.001).

    J Neuroimmune Pharmacol, 2013, 8(5):1098-105.. Riluzole (PK 26124) purchased from Selleck.

    The effect of intrathecal administration of riluzole on changes of tail flick latency in EA-treated rats (Mean ± SD, %, n = 6). EA was given once per day for eight consecutive days. Riluzole or vehicle was given once daily 30 min prior to EA. The significance of differences was calculated by a one-way ANOVA. EA + V: EA plus vehicle; EA + R20: EA plus 20 μg riluzole; EA + R10: EA plus 10 μg riluzole; EA + R5: EA plus 5 μg riluzole; R20, 20 μg riluzole. The values with different letters (a–d) at the same day differ (p < 0.05).

    Int J Mol Sci, 2016, 17(3):357. Riluzole (PK 26124) purchased from Selleck.

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Biological Activity

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

Methods Test Index PMID
Western blot
p-AKT / AKT ; 

PubMed: 23077590     

Riluzole decreases AKT phosphorylation. Serum-starved melanoma cells were incubated in the absence (−) or presence (+) of 25 µM of riluzole for 4 and 8 hours. Immunoblots were performed using antibodies against AKT phosphorylated at serine 473 (pAKT (S473)) or at threonine 308 (pAKT (T308)). Anti-total AKT and GAPDH antibodies were used for normalization. 

p-Smad2 / Smad2 / p-Smad3 / Smad3 ; 

PubMed: 23077590     

Riluzole does not affect the C-terminal phosphorylation of Smads. After serum starvation, cells were incubated in the absence (−) or presence (+) of riluzole for 9 hours.

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]


Solubility (25°C)

In vitro DMSO 46 mg/mL (196.41 mM)
Water Insoluble
Ethanol '46 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 234.2


CAS No. 1744-22-5
Storage powder
in solvent
Synonyms RP-54274
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 Active not recruiting 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

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Sodium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID