Riluzole

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H300：Lebensgefahr bei Verschlucken.

Riluzole Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R25:Giftig beim Verschlucken.

• S-Sätze Betriebsanweisung:

  S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).

• Beschreibung

  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.

• Chemische Eigenschaften

  White Crystalline Solid

• Originator

  Rhone-Poulenc Rorer (France)

• Verwenden

  Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.

• Verwenden

  anticonvulsant, glutamate release inhibitor, anti-ALS

• Verwenden

  A neuroprotective agent. Modulates glutamatergic transmission. A glutamate release inhibitor. An anticonvulsant.

• Verwenden

  A neuroprotective agent. A glutamate release inhibitor. An anticonvulsant

• Definition

  ChEBI: Riluzole is a member of benzothiazoles.

• Trademarks

  Rilutek (Sanofi Aventis).

• Biologische Aktivität

  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

• Lager

  Room temperature

• Einzelnachweise

  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 Upstream-Materialien And Downstream Produkte

Riluzole Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(428)Suppliers

1744-22-5, Riluzole Verwandte Suche: