| Description | Cabergolineisanergotderived-dopamineD2-likereceptoragonistthathashighaffinityforD2,D3,and5-HT2Breceptors(Ki=0.7,1.5,and1.2,respectively). |
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| 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 |
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| PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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| 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] | ||||||||||||||||
| References |
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| MolecularWeight | 451.6 | ||||||||||||
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| Formula | C₂₆H₃₇N₅O₂ | ||||||||||||
| CASNo. | 81409-90-7 | ||||||||||||
| Storage |
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| Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
| Solvent&Solubility | DMSO:≥33mg/mL *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> Purity:99.47% |
