PrNMI-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPrNMICat.No.:HY-123917CASNo.:1541244-33-0分⼦式:C₂₉H₃₁NO分⼦量:409.56作⽤靶点:CannabinoidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PrNMI⼀种有效的、具有⼝服活性的外周限制性⼤⿇素1受体(CB1R)激动剂。PrNMI可抑制化疗引起的周神经病变疼痛症状，并且还可作为癌症引起的⾻痛的镇痛剂[1][2]。IC50&TargetCB1体外研究PrNMI(1nM-1μM;24hours)showsnoeffectsonviabilityof66.1breasttumorcellsinvitro[2].CellViabilityAssay[2]CellLine:66.1breastcancercellConcentration:1nM,10nM,100nM,and1μMIncubationTime:24hoursResult:Showednoeffectsonviabilityof66.1breasttumorcellsinvitro.体内研究PrNMI(0.25mg/kg;Intraplantaripsilateraladministration;i.p.)causessignificantlygreatersuppressioninmechanicalbutnotcoldallodyniaontheipsilateralpawcomparedtocontralateralpaworsystemicadministrationat2hpost-PrNMI[1].PrNMI(3.0mg/kg;i.g.;48hours)dose-dependentlysuppressesCIPNsymptomsinbothmaleandfemaleratsandisequallyeffectiveinmaleandfemaleratsafteroraladministration[1].PrNMI(1mg/kg;p.o.;48hours)exhibitsanti-allodyniceffectsinCIPNmediatedmainlybyCB1Rs[1].PrNMI(1mg/kg;p.o.;dailyfortwoweeks)showsnosignificanttolerancetosuppressionofbothmechanical1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEandcoldallodyniaduringthetwo-weektestingperiod[1].PrNMI(0.1,0.3,and0.6mg/kg;i.p.)resultsinasignificant,time-relatedreductionofflinchingbutnotguardinginadose-dependentmanner.Thissuppressionofflinchingstarts1-hourpost-injectionandpersistsforatleast5hours[2].AnimalModel:Chemotherapy-inducedperipheralneuropathy(CIPN)ratmodel(Cisplatin;i.p.;daily3mg/kgfor4weeks)[1]Dosage:0.25mg/kgAdministration:Intraplantaripsilateraladministration;i.p.Result:At2hpost-PrNMI,mechanicalbutnotcoldallodyniasuppressionwassignificantlygreaterontheipsilateralpawcomparedtocontralateralpaworsystemicadministration.AnimalModel:Chemotherapy-inducedperipheralneuropathy(CIPN)ratmodel(i.p.;daily3mg/kgfor4weeks)[1]Dosage:1mg/kgAdministration:p.o.;dailyfortwoweeksResult:SuppressedmechanicalandcoldallodyniaCIPNsymptoms.AnimalModel:18–20gfemaleBALB/cAnNHsdmice(bearingmurinemammarytumorline,66.1;CIBPmodel)[2]Dosage:0.1,0.3,and0.6mg/kgAdministration:i.p.Result:Resultedinasignificant,time-relatedreductionofflinchingbutnotguardinginadose-dependentmanner.Thissuppressionofflinchingstarted1-hourpost-injectionandpersistedforatleast5hours.REFERENCES[1].MulpuriY,etal.Syntheticperipherally-restrictedcannabinoidsuppresseschemotherapy-inducedperipheralneuropathypainsymptomsbyCB1receptoractivation.Neuropharmacology.2018;139:85-97.[2].ZhangH,etal.Peripherallyrestrictedcannabinoid1receptoragonistasanovelanalgesicincancer-inducedbonepain.Pain.2018;159(9):1814-1823.McePdfHeightCaution:Producthasnotbeenfullyvalidated