Flunarizine-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFlunarizineCat.No.:HY-B0358CASNo.:52468-60-7分?式:C??H??F?N?分?量:404.49作?靶點(diǎn):CalciumChannel;SodiumChannel;DopamineReceptor作?通路:MembraneTransporter/IonChannel;NeuronalSignaling;GPCR/GProtein儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Flunarizine?種有效的Na+/Ca2+(T型)通道雙重阻滯劑。FlunarizineD2多巴胺受體拮抗劑。Flunarizine具有抗驚厥和抗偏頭痛活性，以及外周?管擴(kuò)張作?。IC50&TargetD2Receptor體外研究Flunarizineblockssodiumcurrents(INa)andcalciumcurrents(ICa)withIC50valuesof0.94μMand1.77μMinculturedratcorticalneurons,respectively[2].Flunarizine(10and30μM;24h)showscytotoxiceffectstochromaffincells[4].Flunarizine(1-30μM)causesclearcytoprotectionofchromaffincellatconcentrationsof3-10μM[4].CellCytotoxicityAssay[4]CellLine:Chromaffincells[4]Concentration:10and30μMIncubationTime:24hoursResult:Showedatendencytoincreasecelldeathattheconcentrationof10μM,andshowednear100%celllossattheconcentrationof30μM.體內(nèi)研究Flunarizine(intraperitonealinjection;30?mg/kg;once)protectsmicefromlipopolysaccharide-(LPS-)inducedacutelunginjury(ALI)[5].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MaleBALB/cmice(6-8weeksold)withacutelunginjuryinducedbylipopolysaccharide[5]Dosage:30?mg/kgAdministration:Intraperitonealinjection;30?mg/kg;onceResult:SuppressedtheLPS-inducedcellinflux,proteinleakage,andinflammatorycytokinesrelease.Inhibitedthepulmonaryinflammation.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JLeukocBiol.2021Sep17.?JEthnopharmacol.2020May23;254:112727.?SciRep.2018Nov16;8(1):16932.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Hong-SeobSo,etal.ProtectiveeffectofT-typecalciumchannelblockerflunarizineoncisplatin-induceddeathofauditorycells.HearRes.2005Jun;204(1-2):127-39.[2].QingYe,etal.Flunarizineblocksvoltage-gatedNa(+)andCa(2+)currentsinculturedratcorticalneurons:Apossiblelocusofactioninthepreventionofmigraine.NeurosciLett.2011Jan10;487(3):394-9.[3].CeliaMSanti,etal.DifferentialinhibitionofT-typecalciumchannelsbyneuroleptics.JNeurosci.2002Jan15;22(2):396-403.[4].NovalbosJ,etal.EffectsofdotarizineandflunarizineonchromaffincellviabilityandcytosolicCa2+.EurJPharmacol.1999Feb5;366(2-3):309-17.[5].WanL,etal.MibefradilandFlunarizine,TwoT-TypeCalciumChannelInhibitors,ProtectMiceagainstLipopolysaccharide-InducedAcuteLungInjury.MediatorsInflamm.2020Nov10;2020:3691701.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic