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.
화학적 성질
White Crystalline Solid
용도
Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry.
생물학적 활성
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.
