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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/盐酸氯丙嗪/HY-B0407A/10mM*1mL二甲基亚砜
商品详细Medchemexpress/盐酸氯丙嗪/HY-B0407A/10mM*1mL二甲基亚砜
Medchemexpress/盐酸氯丙嗪/HY-B0407A/10mM*1mL二甲基亚砜
Medchemexpress/盐酸氯丙嗪/HY-B0407A/10mM*1mL二甲基亚砜
商品编号： HY-B0407A-1g
品牌： MedChemExp
市场价： ¥1200.00
美元价： 720.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
ChlorpromazineHydrochlorideisanantagoNISTofthedopamineD2receptors,5-HT2Areceptors,potassiumchannel,sodiumchannel,withKiof363nMand8.3nMfordopamineD2receptorandSEROtonin5-HT2Areceptor,respectively.
Description

ChlorpromazineHydrochlorideisanantagonistofthedopamineD2receptors,5-HT2Areceptors,potassiumchannel,sodiumchannel,withKiof363nMand8.3nMfordopamineD2receptorandserotonin5-HT2Areceptor,respectively.

IC50&Target

Ki:363nM(dopamineD2receptor),8.3nM(5-HT2Areceptor)[4]

InVitro

Chlorpromazine(3,10,20,40,and60μM)decreasesthepeakcurrentsofhNav1.7inaconcentration-dependentmanner,withIC50of25.9μMwithaHillcoefficientof2.3.Chlorpromazine(25μM)producesstronguse-dependentinhibitionofthehNav1.7current.ChlorpromazineblocksthehNav1.7channel,independentofcalmodulin[1].ChlorpromazineblocksHERGpotassiumchannelswithanIC50valueof21.6μMandaHillcoefficientof1.11.Chlorpromazine(1,10,100μM)blocksHERGpotassiumchannelsexpressedinXenopuslaevisoocytesinaconcentration-dependentmanner.ChlorpromazineblocksHERGpotassiumchannelsintheactivatedstate[5].

InVivo

Chlorpromazine(2mg/kg,i.p.)-inducedneurobehaviouralabnormalities(NAs)arecharacterizedbysignificantincreaseincatalepticbehaviourandloaredspontaneousactivityreactiontimeinmice[2].Chlorpromazine(1or5mg/kg,i,p.)preventsketamine(KET)fromincreasingaveragespectralpowerofdeltaandgamma-highbandsonthe5thand10thdaysoftreatmentinrats[3].

ClinicalTrial
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References

  • [1].LeeSJ,etal.Mechanismofinhibitionbychlorpromazineofthehumanpainthresholdsodiumchannel,Nav1.7.NeurosciLett.2017Feb3;639:1-7.

    [2].KaleOE,etal.Amlodipine,anL-typecalciumchannelblocker,protectsagainstchlorpromazine-inducedneurobehaviouraldeficitsinmice.FundamClinPharmacol.2017Jan19.

    [3].SampaioLR,etal.Electroencephalographicstudyofchlorpromazinealoneorcombinedwithalpha-lipoicacidinamodelofschizophreniainducedbyketamineinrats.JPsychiatrRes.2017Mar;86:73-82.

    [4].SuzukiH,etal.Comparisonoftheanti-dopamineD₂andanti-serotonin5-HT(2A)activitiesofchlorpromazine,bromperidol,haloperidolandsecond-generationantipsychoticsparentcompoundsandmetabolitesthereof.JPsychopharmacol.2013Apr;27(4):396-400

    [5].Thomas,D.,etal.TheantipsychoticdrugchlorpromazineinhibitsHERGpotassiumchannels.BrJPharmacol,2003.139(3):p.567-74.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.8143mL14.0714mL28.1429mL
5mM0.5629mL2.8143mL5.6286mL
10mM0.2814mL1.4071mL2.8143mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdministration
[2]

Chlorpromazineisformulatedinsaline.

Adultmice(8-10weeksold)weighing18-25garedividedintofivegroupsofsixmicepergroup.Thetreatmentscheduleisasfollows:Group1,control(NormalSaline:NS,10mL/kgi.p.);Group2,chlorpromazine(CPZ,2mg/kgi.p.);Group3,bromocriptine(BMC,2.5mg/kgs.c.);Group4:amlodipine(AML,1mg/kgs.c.);Group5,BMC(2.5mg/kgs.c.)+AML(1mg/kg).AnimaltreatedwithBMCorAMLortheircombinationalsoreceivechlorpromazine30minlater(i.p.).Animalsaresubjectedtovarioustestsincludingmetalbartestforcatalepsyandspontaneousactivitywheelformotorassessmentandagilityandelevatedplusmaze,hole-board,Y-maze,open-fieldtestsforlocomotoryactivity,andexploratorybehaviourrespectively.Animalsareeuthanizedeighteenhourslaterbycervicaldislocation.Thebrainisdissected,rinsedinbuffer(pH7.6)andhomogenizedwithTeflonandusedforassessmentoflipidperoxidation,reducedglutathione,superoxidedismutaseandcatalase.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LeeSJ,etal.Mechanismofinhibitionbychlorpromazineofthehumanpainthresholdsodiumchannel,Nav1.7.NeurosciLett.2017Feb3;639:1-7.

    [2].KaleOE,etal.Amlodipine,anL-typecalciumchannelblocker,protectsagainstchlorpromazine-inducedneurobehaviouraldeficitsinmice.FundamClinPharmacol.2017Jan19.

    [3].SampaioLR,etal.Electroencephalographicstudyofchlorpromazinealoneorcombinedwithalpha-lipoicacidinamodelofschizophreniainducedbyketamineinrats.JPsychiatrRes.2017Mar;86:73-82.

    [4].SuzukiH,etal.Comparisonoftheanti-dopamineD₂andanti-serotonin5-HT(2A)activitiesofchlorpromazine,bromperidol,haloperidolandsecond-generationantipsychoticsparentcompoundsandmetabolitesthereof.JPsychopharmacol.2013Apr;27(4):396-400

    [5].Thomas,D.,etal.TheantipsychoticdrugchlorpromazineinhibitsHERGpotassiumchannels.BrJPharmacol,2003.139(3):p.567-74.

MolecularWeight

355.33

Formula

C₁₇H₂₀Cl₂N₂S

CASNo.

69-09-0

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥60mg/mL

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

Purity:99.85%