Riluzole

Catalog No.S1614 Synonyms: RP-54274, PK 26124

Riluzole Chemical Structure

Molecular Weight(MW): 234.2

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

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Cited by 4 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 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 purchased from Selleck.

Purity & Quality Control

Choose Selective Sodium Channel Inhibitors

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

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 ; 

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.

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

Solubility (25°C)

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

* 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
Formula

C8H5F3N2OS

CAS No. 1744-22-5
Storage powder
in solvent
Synonyms RP-54274, PK 26124

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02859792 Not yet recruiting Drug: Riluzole|Drug: Placebo|Biological: Blood Samples Spinal Cord Injury Assistance Publique Hopitaux De Marseille May 2019 Phase 2
NCT02796755 Recruiting Drug: Riluzole|Drug: Placebo Inflammation|Fatigue Emory University April 2016 Phase 4
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|St. Michael''s Hospital Toronto|University of Toronto|Anagnostou Evdokia M.D. September 2013 Phase 2
NCT01486849 Completed Drug: CK-2017357|Drug: Placebo|Drug: Riluzole 50 MG Amyotrophic Lateral Sclerosis Cytokinetics November 2011 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