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Basic information Description References Safety Related Supplier
Riluzole Basic information
Riluzole Chemical Properties
  • 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
  • pka2.96±0.10(Predicted)
  • color white
  • Merck 14,8223
  • CAS DataBase Reference1744-22-5
Safety Information
  • 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 IRRITANT
  • HazardClass 6.1
  • PackingGroup II
  • HS Code 29342000
  • ToxicityLD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule)
Riluzole Usage And Synthesis
  • DescriptionRiluzole 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
  • DescriptionRilutek 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 PropertiesWhite Crystalline Solid
  • OriginatorRhone-Poulenc Rorer (France)
  • UsesA neuroprotective agent. Modulates glutamatergic transmission. A glutamate release inhibitor. An anticonvulsant.
  • Usesanticonvulsant, glutamate release inhibitor, anti-ALS
  • UsesLabeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.
  • UsesA neuroprotective agent. A glutamate release inhibitor. An anticonvulsant
  • brand nameRilutek (Sanofi Aventis).
  • Biological ActivityNovel 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 ActionsGlutamate release inhibitor; anticonvulsant
Riluzole Preparation Products And Raw materials
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