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Riluzole

Description References

Riluzole

CAS No.1744-22-5
Chemical Name:Riluzole
CBNumber:CB3353226
Molecular Formula:C8H5F3N2OS
Formula Weight:234.2
MOL File:1744-22-5.mol

Riluzole Property

Melting point 116-118°C
Boiling point 296.3±50.0 °C(Predicted)
Density 1.572±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: ≥25 mg/mL
form solid
pka 2.96±0.10(Predicted)
color white
Merck 14,8223
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
InChIKey FTALBRSUTCGOEG-UHFFFAOYSA-N
EWG's Food Scores 1
NCI Dictionary of Cancer Terms Rilutek; riluzole
FDA UNII 7LJ087RS6F
NCI Drug Dictionary Rilutek
ATC code N07XX02
UNSPSC Code 41116107
NACRES NA.77

Safety

Hazard Codes :T,Xi
Risk Statements :25
Safety Statements :45
RIDADR :UN 2811 6.1/PG 3
WGK Germany :3
RTECS :DL2830000
Hazard Note :Irritant
HazardClass :6.1
PackingGroup :II
HS Code :29342000
Toxicity :LD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule)

NFPA 704:

	1
4		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordDanger
Hazard statements H300
Precautionary statements P301+P310+P330

Riluzole Price More Price(6)

Brand: Sigma-Aldrich(India)
Product number: R116
Product name : Riluzole
Purity: solid
Packaging: 25MG
Price: ₹10013.13
Updated: 2022/06/14
Buy: Buy

Brand: Sigma-Aldrich(India)
Product number: R116
Product name : Riluzole
Purity: solid
Packaging: 250MG
Price: ₹65848.48
Updated: 2022/06/14
Buy: Buy

Brand: Sigma-Aldrich(India)
Product number: R116
Product name : Riluzole
Purity: solid
Packaging: 500MG
Price: ₹114008.9
Updated: 2022/06/14
Buy: Buy

Brand: Sigma-Aldrich(India)
Product number: 557324
Product name : Riluzole - CAS 1744-22-5 - Calbiochem
Purity: A cell-permeable benzothiazole compound that potently inhibits glutamate release and blocks Na+ channels.
Packaging: 50MG
Price: ₹15280
Updated: 2022/06/14
Buy: Buy

Brand: TCI Chemicals (India)
Product number: A2423
Product name : Riluzole
Purity:
Packaging: 5G
Price: ₹5100
Updated: 2022/05/26
Buy: Buy

Riluzole Chemical Properties,Usage,Production

Description Riluzole belongs to the derivative of benzothiazole with neuroprotective, potential anti-depressant and anxiolytic activities, which is used in the treatment of a certain type of nerve disease called amyotrophic lateral sclerosis (ALS, also known as Lou Gehrig's disease). It is effective to delay the onset of ventilator-dependence or tracheostomy in selected patients, slow down the deterioration of this disease and probably prolong survival by approximately two to three months. Besides, studies have proved that riluzole has anti-depressant activity for refractory depression and serves as an anxiolytic in the treatment of obsessive-compulsive disorder and generalized anxiety disorder.
However, riluzole does not cure the ALS and reverse nerve damage or muscle weakness. It is believed to function as an inhibitor of a natural substance called glutamate. It helps protect the nerves in the brain and spinal cord from too much of glutamate which may contribute to the nerve damage. Riluzole is available in both tablet and liquid form. The liquid formulation may be more suitable for patients with swallowing difficulties.
References https://en.wikipedia.org/wiki/Riluzole
http://www.medicinenet.com/riluzole_oral_tablets/article.htm
https://pubchem.ncbi.nlm.nih.gov/compound/5070#section=Top
Description Rilutek was launched in Germany, the UK and US (orphan drug status) for treatment of amyotrophic lateral sclerosis (ALS) and is the first drug approved for this indication. A one step synthesis from 4-(trifluoromethoxy)aniline provides a supply of the compound. The source of its neuroprotective and anticonvulsant activity is not clearly understood. It antagonizes excitatory amino acids and blocks presynaptic release of glutamate, is an antagonist of NMDA-induced acetylcholine release and inhibited glutamate and quisqualate induced increases in cGMP but does not bind to NMDA or Kainic receptors. Rilutek has no affinity for glutamate, GABAbenzodiazepine, glycine and adenosine receptors. It easily crosses the blood brain barrier and depresses glutamatergic neurotransmission, stabilizes voltagedependent Na channels in their inactive form and activates G-protein dependent processes.
Chemical Properties White Crystalline Solid
Originator Rhone-Poulenc Rorer (France)
Uses anticonvulsant, glutamate release inhibitor, anti-ALS
Uses A neuroprotective agent. Modulates glutamatergic transmission. A glutamate release inhibitor. An anticonvulsant.
Uses A neuroprotective agent. A glutamate release inhibitor. An anticonvulsant
Uses Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.
Definition ChEBI: Riluzole is a member of benzothiazoles.
brand name Rilutek (Sanofi Aventis).
Biological Activity Novel psychotropic agent with anticonvulsant, hypnotic, anxiolytic, anti-ischemic and anesthetic properties. Riluzole is able to act as a glutamate release inhibitor, blocks voltage-dependent Na + channels and inhibits GABA uptake by striatal synaptosomes.
Biochem/physiol Actions Glutamate release inhibitor; anticonvulsant
storage Room temperature
References 1) Bellingham (2011), A review of the neural mechanisms of action and clinical efficiency of riluzole in treating amyotrophic lateral sclerosis: what have we learned in the last decade; CNS Neurosci. Ther. 17 4 2) Urbani and Belluzzi (2000), Riluzole inhibits the persistent sodium current in mammalian CNS neurons; Eur. J. Neurosci. 12 3567 3) Frizzo et al. (2004), Riluzole enhances glutamate uptake in rat astrocyte cultures; Cell Mol. Neurobiol. 24 123 4) Doble (1996), The pharmacology and mechanism of action of riluzole; Neurology 47 S233 5) Pittenger et al. (2008), Riluzole in the treatment of mood and anxiety disorders; CNS Drugs 22 761 6) Namkoong et al. (2007), Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma; Cancer Res. 67 2298 7) Zhang et al. (2015), Anti-cancer effect of metabotropic glutamate receptor inhibition in human glioma U87 cells: involvement of PI3K/Akt/mTOR pathway; Cell Physiol. Biochem. 35 419 8) Sperling et al. (2017), Riluzole: a potential therapeutic intervention in human brain tumor stem-like cells; Oncotarget 8 96697