Quinpirole-Hydrochloride-minus-LY-171555-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEQuinpiroleHydrochlorideCat.No.:HY-B1752ACASNo.:85798-08-9Synonyms:(-)-LY171555分?式:C??H??ClN?分?量:255.79作?靶點(diǎn):DopamineReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:50mg/mL(195.47mM;Needultrasonic)DMSO:27.78mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.9095mL19.5473mL39.0946mL5mM0.7819mL3.9095mL7.8189mL10mM0.3909mL1.9547mL3.9095mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(8.13mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.13mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.13mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(390.95mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性QuinpiroleHydrochloride((-)-LY171555)具有?親和?的dopamineD2/D3受體的激動(dòng)劑。IC50&TargetDopamineD2/D3receptor[1].體內(nèi)研究DAcontentisleftbrainbiasedacrossgroups,andalthoughthisasymmetryappearsgreaterinsalinecontrolsthanalldrug-treatedgroups,thereisnotasignificantinteractionbetweenSideandGroup.Wheneachsideisconsideredseparatelyitcanbeseenthatintheleftbrainstructure,DAlevelsprogressivelydecreasewithchronicquinpiroletreatment,withtheQQratsdifferingsignificantlyfromsalinecontrols.Incontrast,rightcorticalDAlevelsareonlyalteredsignificantly(increased)byacuteQuinpirole.ItcanbefoundthatDOPAClevelsarealsoleftbrainbiasedacrossgroups.However,nosignificantGrouporinteractioneffectsarefound.RatsreceivingacuteQuinpiroleshowaselectiveincreaseinDAcontentanddecreaseinturnoverratio,relativetoeithersalinecontrolsortheQSgroup.Sensitized(QQ)ratshowever,haveelevatedDOPAClevelsincomparisontotheacutequinpirolegroup.Instriatumaswell,allthreemeasuresofDAfunctiondifferedsignificantlyacrossgroups(DA,F3,33=6.27,P=0.0020;DOPAC,F3,33=7.98,P=0.0004;turnoverratio,F3,33=16.85,P[1].PROTOCOLAnimalRat[1]Administration[1]36maleLong-Evansratsareinjecteddailyfor12dayswitheithersalineorQuinpirole(Hydrochloride)(quinpiroleHCl:0.5mg/kg,s.c.,n=18/condition),andplacedimmediatelyinOmnitechactivitymonitors(60×60×40cm)for90min.Onthefinaltestday,halftheratsineachchronicconditionreceivedsalineandhalfQuinpirole(n=9/group).Thefourgroupsthereforerepresentedsalinecontrols(SS),acuteQuinpirole(SQ),sensitizedQuinpirole(nodrug)(QS)andsensitizedQuinpirole(drug)(QQ).30minafterthefinalinjection,eachratisremovedfromtheactivitymonitorstoanearbyroomandkilledimmediatelybydecapitation.Thistimepointischosentodissociatethebehaviouraleffectsofquinpirolebetweengroups,sinceacutequinpiroleproducesinhibitionofactivityatthistime,whilechronicquinpiroleisassociatedwithpronouncedhyperlocomotionat30min[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?BrJPharmacol.2021Apr26.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SullivanRM,etal.Effectsofquinpiroleoncentraldopaminesystemsinsensitizedandnon-sensitizedrats.Neuroscience.1998Apr;83(3):781-9.McePdfHeig