Description
Riluzoleisclinicallyusedtotreatsymptomsofamyotrophiclateralsclerosis(ALS).RiluzoleinhibitsNa+,K+,andCa2+currentsandmaydisplayanticonvulsantactivity,inhibitingrhythmicmotordisorders.Riluzolealsoexhibitsantinociceptive,anxiolytic,andanti-parasiticactivities.Riluzolereversescutaneoushypersensitivityinanimalmodelsofthermalpain,increasingresponselatency.Thiscompoundalsoimprovesperformanceofanimalsintheelevatedplusmaze,light/darkavoidancetest,andopenfieldtest.Additionally,riluzoleactivatestransientreceptorpotentialcanonical5(TRPC5)channels.Riluzoleinhibitspteridinereductase1(PTR1)inparasites,increasingoxidativestressandresultingindeathofLeishmaniaparasites.Invitro,riluzoleincreasesglucosetransportandupregulatestranslocationofglucosetransporterstotheplasmamembrane.Riluzolemaybeanon-competitiveinhibitorofkainatereceptorsandNMDAreceptors.
References
RichterJM,SchaeferM,HillK.RiluzoleactivatesTRPC5channelsindependentlyofPLCactivity.BrJPharmacol.2014Jan;171(1):158-70.PMID:24117252.
DanielB,GreenO,ViskindO,etal.RiluzoleincreasestherateofglucosetransportinL6myotubesandNSC-34motorneuron-likecellsviaAMPKpathwayactivation.AmyotrophLateralSclerFrontotemporalDegener.2013Sep;14(5-6):434-43.PMID:23834207.
GuerrieriD,FerrariS,CostiMP,etal.BiochemicaleffectsofriluzoleonLeishmaniaparasites.ExpParasitol.2013Mar;133(3):250-4.PMID:23206955.
SugiyamaA,SaitohA,IwaiT,etal.Riluzoleproducesdistinctanxiolytic-likeeffectsinratswithouttheadverseeffectsassociatedwithbenzodiazepines.Neuropharmacology.2012Jun;62(8):2489-98.PMID:22377384.
BellinghamMC.Areviewoftheneuralmechanismsofactionandclinicalefficiencyofriluzoleintreatingamyotrophiclateralsclerosis:whathavewelearnedinthelastdecade?CNSNeurosciTher.2011Feb;17(1):4-31.PMID:20236142.
HamaA,SagenJ.Antinociceptiveeffectofriluzoleinratswithneuropathicspinalcordinjurypain.JNeurotrauma.2011Jan;28(1):127-34.PMID:20954888.
