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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/卡麦角林（同义词：FCE-21336）/HY-15296/10mM*1mL二甲基亚砜
商品详细Medchemexpress/卡麦角林（同义词：FCE-21336）/HY-15296/10mM*1mL二甲基亚砜
Medchemexpress/卡麦角林（同义词：FCE-21336）/HY-15296/10mM*1mL二甲基亚砜
Medchemexpress/卡麦角林（同义词：FCE-21336）/HY-15296/10mM*1mL二甲基亚砜
商品编号： HY-15296-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥2120.00
美元价： 1272.00
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
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商品介绍
Cabergolineisanergotderived-dopamineD2-likereceptoragoNISTthathashighaffinityforD2,D3,and5-HT2Breceptors(Ki=0.7,1.5,and1.2,respectively).
Description

Cabergolineisanergotderived-dopamineD2-likereceptoragonistthathashighaffinityforD2,D3,and5-HT2Breceptors(Ki=0.7,1.5,and1.2,respectively).

IC50&Target

Ki:0.7(DopamineD2receptor),1.5(DopamineD3receptor),1.2(5-HT2Breceptor)[1]

InVitro

CabergolineactsasapotentagonistofD2,D3and5-HT2Breceptors.PretreatmentwithCabergolineinhibitsH2O2-inducedneuronalcelldeathinadose-dependentmanner.Inthefollowingexperiments,10µMofCabergolineisusedtoinvestigateitsneuroprotectiveeffects.MAP2stainingrevealsthatCabergolinesignificantlysuppressesthelossofneuronscausedbyH2O2incubation.ThedetectionofapoptoticnuclearcondensationsuggestedthatCabergolinepreventsapoptoticcelldeathfollowingH2O2exposure[1].

InVivo

Cabergolinehasalongereliminationhalf-life(63to109h)comparedwithotherD2-likereceptoragonists,bothalong-lastingclinicaleffectfollowingsingle-doseadministration,andanimprovementinthequalityoflifeofpatientswithchronicdiseasesareexpected[1].Themostsignificantreductioninrapideyemovement(REM)sleepboutnumberoccurredduringthelightphase,inwhichCabergoline-injectedfemalehandledmicehas67.3%lessREMsleepbouts(F(1,11)=12.892,P=0.004)thanCabergoline-injectedfemalesthatarerestrained,althoughthegreatestnumberinreductionofREMsleepboutsoccurrduringthedarkphase(82.3%fewerREMsleepbouts;F(1,11)=3.667,P=0.082).Inmalemice,CabergolinereducesbaselineProlactin(PRL)levels(98.5%;F(1,6)=13.192,P=0.011)from5.8±1.3to0.08ng/mLwithin2hoursofinjection.Aftera7-dayrecoveryperiod,PRLlevelsreturntovaluesthatarenotdifferentfrombaseline(5.0±0.60ng/mL;F(1,6)=0.715,P=0.43)[2].

References

  • [1].OdakaH,etal.Cabergoline,dopamineD2receptoragonist,preventsneuronalcelldeathunderoxidativestressviareducingexcitotoxicity.PLoSOne.2014Jun10;9(6):e99271.

    [2].JeffersonF,etal.Adopaminereceptord2-typeagonistattenuatestheABIlityofstresstoaltersleepinmice.Endocrinology.2014Nov;155(11):4411-21.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.2143mL11.0717mL22.1435mL
5mM0.4429mL2.2143mL4.4287mL
10mM0.2214mL1.1072mL2.2143mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

CabergolineisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[1].

Primarycorticalneuronsareprepared.Cabergoline(10µM;exceptforexperimentsofdose-dependency)isappliedtocorticalcellsatDIV6-7.After24-hourCabergolinetreatment(exceptforexaminationofpretreatmenttime-dependencyofCabergoline),H2O2(50µM;exceptforthedose-dependencyofH2O2)isadded.Allinhibitorsandantagonists,includingspiperone,U0126,SB203580,SP600125,AP5,andnifedipineareapplied20minbeforeCabergolineorH2O2addition.L-glutamateisaddedatDIV7-8forcelldeathinduction.CellsurvivalrateismeasuredbyMTTassay.Aftertheindicatedtreatmentwithdrugsiscompleted,culturemediumisreplacedwith200µLfreshmediumcontaining40µlMTTsolution(2.5mg/mL,dilutedinPBS)andcellsareincubatedat37°Cfor1.5-2.5hours.Then,200µLlysisbuffercontainingisopropylalcoholisappliedtoeachwellandmixedbypipetting.Eachsampleismovedtoa96-wellplateanditsabsorbanceat570nmismeasuredusinganiMarkMicroplateleader.Cellsurvivalrateisquantitatedbyabsorbancemeasurement,becauseMTT(yellow)isdeoxidizedtoformazan(violet)inproportiontomitochondrialactivity[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2]

Cabergolineisdissolvedin100%pharmasolveandthendilutedwith20%β-cyclodextrininwatertoyieldafinalconcentrationof0.15-0.5mg/mL[2].

Mice[2]
FemaleandmaleC57BL/6Jmiceareused.Cabergolineisdissolvedin100%pharmasolveandthendilutedwith20%β-cyclodextrininwatertoyieldafinalconcentrationof0.15-0.5mg/mLCabergoline.Micereceiveda0.3-mg/kgipinjectionofCabergolineorvehicle.Alldrugsarepreparedwithin48hoursofexperimentandstoredat4°C.Solutionsareallowedtoreachatroomtemperaturebeforeinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].OdakaH,etal.Cabergoline,dopamineD2receptoragonist,preventsneuronalcelldeathunderoxidativestressviareducingexcitotoxicity.PLoSOne.2014Jun10;9(6):e99271.

    [2].JeffersonF,etal.Adopaminereceptord2-typeagonistattenuatestheabilityofstresstoaltersleepinmice.Endocrinology.2014Nov;155(11):4411-21.

MolecularWeight

451.6

Formula

C₂₆H₃₇N₅O₂

CASNo.

81409-90-7

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥33mg/mL

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

Purity:99.47%