Description
FlupirtinemaleateisanagoNISTatvoltage-gatedKCNQ/Kv7K+channels;openingofthesechannelsonneuronsfacilitatesM-currentgenerationanddecreasesaxonalexcitABIlity.InadditiontoitsmodulationofK+channels,flupirtinemaleatealsoinhibitsNMDAreceptorsandshiftsgatingofGABA-AreceptorstodecreasecirculatingGABAconcentrations.Flupirtinemaleateisaneffectivenon-sedativeanalgesic,showingbenefitinclinicaltrialsofneurosurgicalpatients.Inanimalmodels,thiscompoundalsoattenuatesdevelopmentofandreversesestablishedpulmonaryarterialhypertension,suggestingantihypertensiveactivity.
References
YadavG,ChoupooS,DasSK,etal.EvaluatingtheRoleofFlupirtineforPostcraniotomyPainandCompareitWithDiclofenacSodium:AProspective,Randomized,DoubleBlind,Placebo-controlledStudy.JNeurosurgAnesthesiol.2013Jun11.[Epubaheadofprint].PMID:23764718.
FleckensteinJ,SittlR,AverbeckB,etal.ActivationofaxonalKv7channelsinhumanperipheralnervebyflupirtinebutnotplacebo-therapeuticpotentialforperipheralneuropathies:resultsofarandomisedcontrolledtrial.JTranslMed.2013Feb8;11:34.PMID:23394517.
KlingerF,GeierP,DorostkarMM,etal.ConcomitantfacilitationofGABAAreceptorsandKV7channelsbythenon-opioidanalgesicflupirtine.BrJPharmacol.2012Jul;166(5):1631-42.PMID:22188423.
HarishS,BhuvanaK,BengalorkarGM,etal.Flupirtine:Clinicalpharmacology.JAnaesthesiolClinPharmacol.2012Apr;28(2):172-7.PMID:22557738.
DevulderJ.Flupirtineinpainmanagement:pharmacologicalpropertiesandclinicaluse.CNSDrugs.2010Oct;24(10):867-81.PMID:20839897.
MorecroftI,MurrayA,NilsenM,etal.TreatmentwiththeKv7potassiumchannelactivatorflupirtineisbeneficialintwoindependentmousemodelsofpulmonaryhypertension.BrJPharmacol.2009Aug;157(7):1241-9.PMID:19508393.
