Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERenzaprideCat.No.:HY-14147CASNo.:112727-80-7Synonyms:BRL24924分?式:C??H??ClN?O?分?量:323.82作?靶點:5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Renzapride(BRL24924)，?種取代苯甲酰胺，5-HT4受體激動劑，也5HT2b和5HT3受體拮抗劑[1]。Renzapride(BRL24924)可以?于便秘型腸易激綜合征(C-IBS)的研究[2]。IC50&Target5-HT4Receptor115nM(Ki)體外研究Renzapridereplacesspecificbindingof[H3]GR113808(aselective5-HTreceptorantagonist)toclonedhuman5-HT4receptorswithaKivalueof115nM[3].體內研究Renzapride(BRL24924)(100μgi.v.)resultsinapartialreverseofboththedelayedsolidandliquidmealsemptying[2].Renzapride(BRL24924)(0.5-1mg/kg)significantlyincreasestherateofemptyingofa51Cr-labeledliquidmealfromthemurinestomach[4].AnimalModel:Dog(simulatinggastroparesis)[2]Dosage:100μg/kgAdministration:i.v.Result:Resultsinapartialreverseofboththedelayedsolidandliquidmealsemptying.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Mice(30-45g)[2]Dosage:0.5-1mg/kgAdministration:p.o.Result:Significantlyincreasetherateofemptyingofa51Cr-labeledliquidmealfromthemurinestomach.REFERENCES[1].CamilleriM,etal.Effectofrenzaprideontransitinconstipation-predominantirritablebowelsyndrome.ClinGastroenterolHepatol.2004;2(10):895-904.[2].ScarpelliniE,etal.Renzapride:anewdrugforthetreatmentofconstipationintheirritablebowelsyndrome.ExpertOpinInvestigDrugs.2008;17(11):1663-1670.[3].NagakuraY,etal.Pharmacologicalpropertiesofanovelgastrointestinalprokineticbenzamideselectiveforhuman5-HT4receptorversushuman5-HT3receptor.PharmacolRes.1999;39(5):375-382.[4].MaweGM,etal.Blockadeof5-HT-mediatedentericslowEPSPsbyBRL24924:gastrokineticeffects.AmJPhysiol.1989;257(3Pt1):G386-G396.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: