Quinpirole-Hydrochloride-minus-LY-171555-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEQuinpiroleHydrochlorideCat.No.:HY-B1752ACASNo.:85798-08-9Synonyms:(-)-LY171555分⼦式:C₁₃H₂₂ClN₃分⼦量:255.79作⽤靶点:DopamineReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:50mg/mL(195.47mM;Needultrasonic)DMSO:27.78mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9095mL19.5473mL39.0946mL5mM0.7819mL3.9095mL7.8189mL10mM0.3909mL1.9547mL3.9095mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(8.13mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.13mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.13mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:100mg/mL(390.95mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性QuinpiroleHydrochloride((-)-LY171555)具有⾼亲和⼒的dopamineD2/D3受体的激动剂。IC50&TargetDopamineD2/D3receptor[1].体内研究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.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•BrJPharmacol.2021Apr26.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SullivanRM,etal.Effectsofquinpiroleoncentraldopaminesystemsinsensitizedandnon-sensitizedrats.Neuroscience.1998Apr;83(3):781-9.McePdfHeig