RS-102221-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERS-102221Cat.No.:HY-101365CASNo.:185376-97-0分⼦式:C₂₇H₃₁F₃N₄O₇S分⼦量:612.62作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性RS-102221⼀种选择性5-HT2C受体拮抗剂(Ki=10nM)。RS-102221对5-HT2C受体的选择性5-HT2A和5-HT2B受体的近100倍。RS-102221能够促进新⽣神经细胞分化。RS-102221增加了⼤⿏的⾷物摄⼊量和体重增加。IC50&Target5-HT2CReceptor5-HT2AReceptor5-HT2BReceptor10nM(Ki)体外研究RS-102221(0.3-300nM;24h)promotesthedifferentiationofadulthippocampalneuralprecursorcells(ahNPCs)andsignificantlyincreasesthepercentageofMAP-2+cells[1].CellDifferentiationAssay[1]CellLine:Mouseadulthippocampalneuralprogenitorcells(ahNPCs)Concentration:0.3,1,10,30,100,and300nMIncubationTime:24hoursResult:SignificantlyincreasesthepercentageofMAP-2+cellsat10nM.体内研究RS-102221(2mg/kg;i.p.;oncedailyfor14d)increasesfood-intakeandweight-gaininrats[2].RS-102221(2mg/kg;i.p.;singledose),combinedwiththe3,4-Methylenedioxy-N-methamphetamine(MDMAor'ecstasy'),suppressestheMDMA-inducedhypophagiaforthefirst1hperiod,andalsosuppressesMDMA-inducedhyperlocomotioninmice[3].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemERS-102221(2mg/kg;i.p.;singledose)canreduceanxietyandreducetheamplitudeofstartlereflexinmiceinlightanddarktest[4].REFERENCES[1].BortolottoV,etal.ProneurogenicEffectsofTrazodoneinMurineandHumanNeuralProgenitorCells.ACSChemNeurosci.2017Sep20;8(9):2027-2038.[2].BonhausDW,etal.RS-102221:anovelhighaffinityandselective,5-HT2Creceptorantagonist.Neuropharmacology.1997Apr-May;36(4-5):621-9.[3].SalzerI,etal.Controlofsensoryneuronexcitabilitybyserotonininvolves5HT2CreceptorsandCa(2+)-activatedchloridechannels.Neuropharmacology.2016Nov;110(PtA):277-286.[4].ConductierG,etal.3,4-N-methlenedioxymethamphetamine-inducedhypophagiaismaintainedin5-HT1Breceptorknockoutmice,butsuppressedbythe5-HT2CreceptorantagonistRS102221.Neuropsychopharmacology.2005Jun;30(6):1056-63.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse