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蚂蚁淘在线 / 品牌中心 / MCE / Medchemexpress/Clozapine N-oxide/HY-17366/10mg

Medchemexpress/Clozapine N-oxide/HY-17366/10mg

价格
￥1580.00
货号：HY-17366-10mM*1mLinDMSO
浏览量：92
品牌：MCE
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商品描述
ClozapineN-oxideisapharmacologicallyinertmetaboliteofClozapine,whichisapotent5-HT1CreceptorantagoNIST.ClozapineN-oxide(CNO)isaDREADD(designerreceptorsexclusivelyactivatedbydesignerdrug)agonist.

CustomerValidation

  • •BiolPsychiatry.2017May1;81(9):737-747.
Description

ClozapineN-oxideisapharmacologicallyinertmetaboliteofClozapine,whichisapotent5-HT1Creceptorantagonist.ClozapineN-oxide(CNO)isaDREADD(designerreceptorsexclusivelyactivatedbydesignerdrug)agonist.

InVivo

Afterasingleintraperitoneal(i.p.)injectionofClozapineN-oxide(1mg/kg)intomice,ClozapineN-oxide(CNO)plasmalevelspeakat15minandareverylowafter2h.AcutelyadministeredCNOcanbemetabolicallyconvertedtoClozapineinotherspeciessuchashumanandguinea-pig.ThemetabolitesthatmayformafterchronicadministrationofCNOtoDREADD-expressingmice(orotherspecies)havenotbeenstudiedsystematically.However,evenifback-transformationtoClozapineoccursafterchronicCNOadministration,itshouldbenotedthatClozapineisamorepotent(by~10-fold)DREADDagonistthanCNOitself.Moreover,confoundingBIOLOGicaleffectsofpotentialCNOmetabolitescanbeeasilyidentifiedbyincludingbothsaline-andCNO-treatedWTanimalsinaparticularDREADDstudy.Despitetheshortplasmahalf-lifeofCNOinmice,thebiologicaleffectsthathavebeendescribedafteracutetreatmentofDREADD-expressingexperimentalanimalsareusuallymuchlonger(6-10h).OnepossibilityisthatCNOtendstoaccumulateintissues,althoughotherscenariosarealsofeasIBLe[1].Usingageneralpharmacokineticmodelfortheinterconversionprocess,themeantotalclearancesofClozapineandClozapineN-oxide(CNO)are28.45L/hrand45.30L/hr,respectively[2].

References

  • [1].WessJ,etal.NoveldesignerreceptorstoprobeGPCRsignalingandphysiology.TrendsPharmacolSci.2013Jul;34(7):385-92.

    [2].ChangWH,etal.ReversiblemetabolismofclozapineandclozapineN-oxideinschizophrenicpatients.ProgNeuropsychopharmacolBiolPsychiatry.1998Jul;22(5):723-39.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.9170mL14.5849mL29.1698mL
5mM0.5834mL2.9170mL5.8340mL
10mM0.2917mL1.4585mL2.9170mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
References

  • [1].WessJ,etal.NoveldesignerreceptorstoprobeGPCRsignalingandphysiology.TrendsPharmacolSci.2013Jul;34(7):385-92.

    [2].ChangWH,etal.ReversiblemetabolismofclozapineandclozapineN-oxideinschizophrenicpatients.ProgNeuropsychopharmacolBiolPsychiatry.1998Jul;22(5):723-39.

MolecularWeight

342.82

Formula

C₁₈H₁₉ClN₄O

CASNo.

34233-69-7

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.98%