Norbinaltorphimine-dihydrochloride-nor-Binaltorphimine-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENorbinaltorphiminedihydrochlorideCat.No.:HY-100903CASNo.:113158-34-2Synonyms:nor-Binaltorphiminedihydrochloride;nor-BNIdihydrochloride分⼦式:C₄₀H₄₅Cl₂N₃O₆分⼦量:734.71作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(136.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3611mL6.8054mL13.6108mL5mM0.2722mL1.3611mL2.7222mL10mM0.1361mL0.6805mL1.3611mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.40mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.40mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Norbinaltorphiminedihydrochloride⼀种有效的和选择性的κ阿⽚受体(κopioidreceptor)拮抗剂。IC50&Targetκopioidreceptor[1]体外研究NorbinaltorphiminereversiblyantagonizetheeffectsofκagonistswithpA2valuesof10.2-10.4.Norbinaltorphimineismuchlesspotentasanantagonistatμandδreceptors,pA2valuesare7.4-7.6and7.6-7.8,respectively[1].体内研究NorbinaltorphiminehasweakandinconsistenteffectsonTHC-inducedtasteavoidanceinadolescentratsinthatNorbinaltorphiminebothattenuatesandstrengthenstasteavoidancedependentondoseandtrial.Norbinaltorphiminehaslimitedimpactonthefinalone-bottleavoidanceandnoeffectsonthetwo-bottlepreferencetest.Interestingly,NorbinaltorphiminehasnoeffectonTHC-inducedtasteavoidanceinadultratsaswell[2].Norbinaltorphiminepretreatmentsignificantlyattenuatesstress-inducedreinstatementofnicotine-CPP,buthasnoeffectonnicotine-primedreinstatement[3].PROTOCOLAnimalRats[2]Administration[2][3]NorbinaltorphimineisdissolvedinsterileH2Oataconcentrationof15mg/mLandadministeredsubcutaneously(SC)atadoseof15mg/kg.MaleSpragueDawleyratsarerankedaccordingtoaveragewaterconsumptiononallhabituationcyclesandassignedtooneoftwogroups[Norbinaltorphimine(n=42)andVehicle(n=42)],suchthatmeanwaterintakeiscomparableamonggroups.OnPND34(approximately24hpriortoconditioning,seebelow),subjectsassignedtotheNorbinaltorphiminegroupareinjectedwithNorbinaltorphimine(15mg/kg)andsubjectsassignedtotheVehiclegroupareinjectedwiththeNorbinaltorphiminevehicleatanequalvolume[2].Mice[3]Miceareconditionedwith0.5mg/kgnicotine,injectedsubcutaneously(s.c.)for3daysandtestedinthenicotine-conditionedplacepreference(CPP)model.After3daysextinction,Norbinaltorphimine(10mg/kg,s.c.)isadministered16hpriortoaprimingdoseofnicotine(0.1mg/kg,s.c.),andmicearetestedintheCPPmodelfornicotine-inducedreinstatementofCPP.Aseparategroupofmiceissubjectedtoa2-daymodifiedforcedswimtest(FST)paradigmtoinducestressafter3daysextinctionfromCPP.MicearegivenvehicleorNorbinaltorphimine(10mg/kg,s.c.)16hpriortoeachFSTsession[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•FrontImmunol.2021Jul7;12:692286.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•FrontCellNeurosci.2022Jun2;16:894886.•Aging.2021May20;13(10):14355-14371.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BirchPJ,etal.Norbinaltorphimine:antagonistprofileatkappaopioidreceptors.EurJPharmacol.1987Dec15;144(3):405-8.[2].FlaxSM,etal.Effectofnorbinaltorphimineon∆⁹-tetrahydrocannabinol(THC)-inducedtasteavoidanceinadolescentandadultSprague-Dawleyrats.Psychopharmacology(Berl).2015Sep;232(17):3193-201.[3].JacksonKJ,etal.Effectsofthekappaopioidreceptorantagonist,norbinaltorphimine,onstressanddrug-inducedreinstatementofnicotine-conditionedplacepreferenceinmice.Psychopharmacology(Berl).2013Apr;