| 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.
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| 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
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| 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 |
