Riluzole
Description References- Product Name
- Riluzole
- CAS No.
- 1744-22-5
- Chemical Name
- Riluzole
- Synonyms
- RILUTEK;CBI-BB ZERO/001785;6-TRIFLUOROMETHOXYBENZOTHIAZOLE-2-YL-AMINE;6-(Trifluoromethoxy)benzo[d]thiazol-2-amine;uzoL;BF-37;NSC8463;RP-54274;RILUZOLE;PK 26124
- 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
N-Bromosuccinimide Price
- Product number
- 557324
- Product name
- Riluzole
- Packaging
- 50mg
- Price
- $155
- Updated
- 2024/03/01
- Product number
- 1604337
- Product name
- Riluzole
- Purity
- United States Pharmacopeia (USP) Reference Standard
- Packaging
- 200mg
- Price
- $527
- Updated
- 2024/03/01
- Product number
- A2423
- Product name
- 2-Amino-6-(trifluoromethoxy)benzothiazole
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 5g
- Price
- $59
- Updated
- 2024/03/01
- Product number
- A2423
- Product name
- 2-Amino-6-(trifluoromethoxy)benzothiazole
- Purity
- >98.0%(HPLC)(T)
- Packaging
- 25g
- Price
- $198
- Updated
- 2024/03/01
- Product number
- H61328
- Product name
- 2-Amino-6-(trifluoromethoxy)benzothiazole, 98%
- Packaging
- 5g
- Price
- $88.65
- Updated
- 2024/03/01
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
A neuroprotective agent. Modulates glutamatergic transmission. A glutamate release inhibitor. An anticonvulsant.
Uses
anticonvulsant, glutamate release inhibitor, anti-ALS
Uses
Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.
Uses
A neuroprotective agent. A glutamate release inhibitor. An anticonvulsant
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
Riluzole Preparation Products And Raw materials
Raw materials
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View Lastest Price from Riluzole manufacturers
- Product
- Riluzole 1744-22-5
- Price
- US $0.00/KG
- Min. Order
- 100g
- Purity
- 98%+
- Supply Ability
- 100kg
- Release date
- 2021-04-12
- Product
- Riluzole 1744-22-5
- Price
- US $10.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1000kg
- Release date
- 2023-10-19
- Product
- Riluzole 1744-22-5
- Price
- US $66.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 20T
- Release date
- 2023-07-21