Mu-opioid-receptor-antagonist-9-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMuopioidreceptorantagonist9Cat.No.:HY-179282CASNo.:3058600-77-1分⼦式:C₂₁H₂₇ClN₂O₂分⼦量:374.9作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Muopioidreceptorantagonist9⼀种强效、选择性强且可穿透⾎脑屏障的μ-阿⽚受体(MOR)拮抗剂，其Ki为77.3nM。Muopioidreceptorantagonist9对κ-阿⽚受体(KOR)和δ-阿⽚受体(DOR)具有选择性。Muopioidreceptorantagonist9能有效阻断精神活性物质的镇痛作⽤。Muopioidreceptorantagonist9可以逆转精神活性物质诱导的⼩⿏呼吸抑制。Muopioidreceptorantagonist9可⽤于阿⽚类药物使⽤障碍(OUD)的研究[1]。IC50&TargetμOpioidReceptor/MORκOpioidReceptor/KORδOpioidReceptor/DOR77.3nM(Ki)681nM(Ki)4182nM(Ki)体外研究Muopioidreceptorantagonist9(compound53)(15min)inhibitscalciumfluxinducedbyDAMGO(HY-P0210)andpsychoactivesubstancesinmMOR-CHOcellswithIC50valuesof33.6and4.51μM,respectively[1].体内研究Muopioidreceptorantagonist9(1-10mg/kg;s.c.;singledose)blockstheantinociceptiveeffectsofMorphineandfentanylinthewarmwatertailimmersionpainmodelinmice[1].Muopioidreceptorantagonist9(1-32mg/kg;s.c.;singledoseat20minpost-fentanyl)demonstratesapotentreversaleffectonfentanyl-inducedrespiratorydepressioninthewhole-bodyplethysmographystudyinmice[1].AnimalModel:MaleSwissWebstermice(6-8-week-old)subcutaneousinjectedwithpsychoactivesubstances[1]Dosage:1,2,4,5,10mg/kg1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:s.c.;singledoseResult:Blockedtheantinociceptionofmorphineatadoseof10mg/kg.showedAD50sof2.02mg/kg(95%CL)against10mg/kgmorphine,and4.02mg/kg(95%CL)against0.1mg/kgfentanyl.AnimalModel:MaleSwissWebstermice(6-8-week-old)subcutaneousinjectedwithpsychoactivesubstances[1]Dosage:1,3.2,10,32mg/kgAdministration:s.c.;singledoseat20minpost-fentanylResult:Demonstratedapotentreversaleffectonfentanyl-inducedrespiratorydepressionatboth10and32mg/kgdoses.Increasedbothrespiratoryfrequencyandtidalvolume.Showedbeneficialeffectwithinashorttimeframe,appearing10minpostadministrationforthe32mg/kgdoseand15minpostadministrationforthe10mg/kgdose.REFERENCES[1].SilteAA,etal.Design,Syntheses,andPharmacologicalEvaluationsofCoreRingExpandedFentanylAnaloguesasPotentialCounteractingAgentsAgainstFentanylInducedRespiratoryDepression.JMedChem.2025;68(21):22170-22195.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications