Description
Riluzole is clinically used to treat symptoms of amyotrophic lateral sclerosis (ALS). Riluzole inhibits Na+, K+, and Ca2+ currents and may display anticonvulsant activity, inhibiting rhythmic motor disorders. Riluzole also exhibits antinociceptive, anxiolytic, and anti-parasitic activities. Riluzole reverses cutaneous hypersensitivity in animal models of thermal pain, increasing response latency. This compound also improves performance of animals in the elevated plus maze, light/dark avoidance test, and open field test. Additionally, riluzole activates transient receptor potential canonical 5 (TRPC5) channels. Riluzole inhibits pteridine reductase 1 (PTR1) in parasites, increasing oxidative stress and resulting in death of Leishmania parasites. In vitro, riluzole increases glucose transport and upregulates translocation of glucose transporters to the plasma membrane. Riluzole may be a non-competitive inhibitor of kainate receptors and NMDA receptors.
References
Richter JM, Schaefer M, Hill K. Riluzole activates TRPC5 channels independently of PLC activity. Br J Pharmacol. 2014 Jan;171(1):158-70. PMID: 24117252.
Daniel B, Green O, Viskind O, et al. Riluzole increases the rate of glucose transport in L6 myotubes and NSC-34 motor neuron-like cells via AMPK pathway activation. Amyotroph Lateral Scler Frontotemporal Degener. 2013 Sep;14(5-6):434-43. PMID: 23834207.
Guerrieri D, Ferrari S, Costi MP, et al. Biochemical effects of riluzole on Leishmania parasites. Exp Parasitol. 2013 Mar;133(3):250-4. PMID: 23206955.
Sugiyama A, Saitoh A, Iwai T, et al. Riluzole produces distinct anxiolytic-like effects in rats without the adverse effects associated with benzodiazepines. Neuropharmacology. 2012 Jun;62(8):2489-98. PMID: 22377384.
Bellingham MC. 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. 2011 Feb;17(1):4-31. PMID: 20236142.
Hama A, Sagen J. Antinociceptive effect of riluzole in rats with neuropathic spinal cord injury pain. J Neurotrauma. 2011 Jan;28(1):127-34. PMID: 20954888.
