Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENorbinaltorphiminedihydrochlorideCat.No.:HY-100903CASNo.:113158-34-2Synonyms:nor-Binaltorphiminedihydrochloride;nor-BNIdihydrochloride分?式:C??H??Cl?N?O?分?量:734.71作?靶點(diǎn):OpioidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(136.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.3611mL6.8054mL13.6108mL5mM0.2722mL1.3611mL2.7222mL10mM0.1361mL0.6805mL1.3611mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.40mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性Norbinaltorphiminedihydrochloride?種有效的和選擇性的κ阿?受體(κopioidreceptor)拮抗劑。IC50&Targetκopioidreceptor[1]體外研究NorbinaltorphiminereversiblyantagonizetheeffectsofκagonistswithpA2valuesof10.2-10.4.Norbinaltorphimineismuchlesspotentasanantagonistatμandδreceptors,pA2valuesare7.4-7.6and7.6-7.8,respectively[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?FrontImmunol.2021Jul7;12:692286.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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??-tetrahydrocannabinol(THC)-inducedtasteavoidanceinadolescentandadultSprague-Dawleyrats.Psychopharmacology(Berl).2015Sep;232(17):3193-201.[3].JacksonKJ,etal.Effectsofthekappaopioidreceptorantagonist,norbinaltorphimine,onstressanddrug-inducedreinstatementofnicotine-conditionedplacepreferenceinmice.Psychopharmacology(Berl).2013Apr;