Renzapride-BRL-24924-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERenzaprideCat.No.:HY-14147CASNo.:112727-80-7Synonyms:BRL24924分⼦式:C₁₆H₂₂ClN₃O₂分⼦量:323.82作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Renzapride(BRL24924)，⼀种取代苯甲酰胺，5-HT4受体激动剂，也5HT2b和5HT3受体拮抗剂[1]。Renzapride(BRL24924)可以⽤于便秘型肠易激综合征(C-IBS)的研究[2]。IC50&Target5-HT4Receptor115nM(Ki)体外研究Renzapridereplacesspecificbindingof[H3]GR113808(aselective5-HTreceptorantagonist)toclonedhuman5-HT4receptorswithaKivalueof115nM[3].体内研究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—您⾝边的抑制剂⼤师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: