nAChR-IN-1-2-2-6-6-Tetramethylpiperidin-4-yl-heptanoate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEnAChR-IN-1Cat.No.:HY-151129CASNo.:849461-90-1Synonyms:2,2,6,6-Tetramethylpiperidin-4-ylheptanoate分?式:C??H??NO?分?量:269.42作?靶點(diǎn):nAChR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性nAChR-IN-1(2,2,6,6-Tetramethylpiperidin-4-ylheptanoate)?種四甲哌啶庚酸酯，選擇性的煙堿型?酰膽堿受體(nAChR)抑制劑，抑制缺乏α5、α6或β3亞的煙堿型?酰膽堿受體。nAChR-IN-1具有預(yù)防神經(jīng)損傷的作?，可?于煙堿型?酰膽堿受體功能障或神經(jīng)紊亂的研究。體外研究nAChR-IN-1(100nM)inhibitsnAChRwithinhibitionrateof90%inXenovusoocytes,andsuppressesAChRsubtypes(mousemuscle-type(α1β1εδ)nAChR,threedifferentpairwisecombinationsofratneuronalalphaandbetasubunits(α3β4,α4β2,andα3β2),andα7homomericneuronalnAChR)withIC50s(area)of390,1.2,110,75,440,460,430,2.7,1.0,1.4,and18.3nM,respectively,basedonthedecreaseinthenetchargeoftheAChresponse[1].體內(nèi)研究nAChR-IN-1(20mg/kg;s.c.;singledose)improvesnicotine-inducedhypomotilityandhypothermiainatime-dependentmannerinmice[1].AnimalModel:Nicotine-inducedmicemodel[1]Dosage:20mg/kgAdministration:Subcutaneousinjection;singledose;15minutespriortotheinjectionofnicotine(1.5mg/kg)Result:Increasedlocomotoractivityinmice,evenifnicotine-induceddecrease.Showednoeffectonbodytemperature.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Tail-flickandhot-platemodelinmice[1]Dosage:0,0.1,1,5mg/kgAdministration:Subcutaneousinjection;singledoseResult:Blockedtheantinociceptiveeffectofnicotineinthehot-plate.Time-dependentlyblockednicotine-inducedantinociception.REFERENCES[1].PapkeRL,et,al.Compositionsetmethodesd'inhibitionselectivedesrecepteursnicotiniquesdel'acetylcholine.WO2005032479A2McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82