Spiradoline-U-62066-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESpiradolineCat.No.:HY-106756CASNo.:87151-85-7Synonyms:U-62066分⼦式:C₂₂H₃₀Cl₂N₂O₂分⼦量:425.39作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:50mg/mL(117.54mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3508mL11.7539mL23.5078mL5mM0.4702mL2.3508mL4.7016mL10mM0.2351mL1.1754mL2.3508mL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%salineSolubility:≥2.5mg/mL(5.88mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.88mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.88mM);Suspendedsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Spiradoline(U-62066)⼀种芳⼄酰胺，⼀种选择性kappa阿⽚受体(κ-opioidreceptor,KOR)激动剂，在豚⿏中的Ki为8.6nM。Spiradoline对μ和δ受体的Ki值分别为252nM和9400nM。Spiradoline具有强效的利尿，⽌痛，抗⼼律失常，镇咳，神经保护作⽤，并易于穿过⾎脑屏障。IC50&TargetKi:8.6nM(κ-opioidreceptoringuineapig),252nM(μ-receptor)and9400nM(δ-receptor)[2]体外研究Usingthepatch-clampmethodinisolatedratcardiacmyocytes,indicatedthatSpiradoline(15to500μM)producesitsantiarrythmiceffectviablockadeofsodiumchannels(andatthehigherdosesalsoofpotassiumcurrents)inmyocardialtissue.Thus,Spiradolinereducesthepeaksodiumcurrent,increasedthedecayrateofthetransientoutwardpotassiumcurrent,andreducedthesustainedplateaupotassiumamplitude[2].体内研究Spiradoline(U-62066;0.1-0.4mg/kg;subcutaneousinjection;once;Sprague-Dawleyrats)treatmentdose-dependentlyreducessocialbehaviorsinnon-stressedadults,producingsocialavoidanceatthehighestdosetested,whileyoungeranimalsdisplaysreducedsensitivitytothissociallysuppressingeffectofSpiradoline.Instressedanimals,thesociallysuppressingeffectsoftheSpiradolinearebluntedatallages,withjuvenilesandadolescentsexhibitingincreasedsocialpreferenceinresponsetocertaindosesofU-62066[1].AnimalModel:Juvenile,adolescentandadultSprague-Dawleymaleandfemaleratsexposuredtorepeatedrestraint[1]Dosage:0.1mg/kg,0.2mg/kg,0.3mg/kg,and0.4ꢀmg/kgAdministration:Subcutaneousinjection;onceResult:Dose-dependentlyreducedsocialbehaviorsinnon-stressedadults,producingsocialavoidanceatthehighestdosetested.REFERENCES[1].ElenaIVarlinskaya,etal.Stressalterssocialbehaviorandsensitivitytopharmacologicalactivationofkappaopioidreceptorsinanage-specificmannerinSpragueDawleyrats.NeurobiolStress.2018Sep11;9:124-132.[2].M-LGWadenberg.Areviewofthepropertiesofspiradoline:apotentandselectivekappa-opioidreceptoragonist.CNSDrugRev.Summer2003;9(2):187-98.McePdfHeightCaution:Producthasnotbeenfullyvalidat