OPC-14523-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEOPC-14523hydrochlorideCat.No.:HY-116594ACASNo.:145969-31-9分⼦式:C₂₃H₂₉Cl₂N₃O₂分⼦量:450.4作⽤靶点:SigmaReceptor;5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(185.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2202mL11.1012mL22.2025mL5mM0.4440mL2.2202mL4.4405mL10mM0.2220mL1.1101mL2.2202mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.62mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.62mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性OPC-14523hydrochloride⼀种具有⼝服活性的sigma和5-HT1A受体激动剂，对sigma受体(σ1/2IC50=47/56nM)、5-HT1A受体(IC50=2.3nM)和5-HT转运体(IC50=80nM)具有⾼度亲和⼒。OPC-14523hydrochloride显⽰抗抑郁药样活性。IC50&Target5-HT1AReceptorsigma1sigma22.3nM(IC50)47nM(IC50)56mM(IC50)体外研究OPC-14523hydrochlorideinhibitstheinvitroreuptakeof3H-5-HT(IC50=27nM),butitshowsveryweakinhibitoryactivityon3H-NEand3H-DAreuptake[1].体内研究OPC-14523hydrochloride(0.3-100mg/kg;p.o.;dailyfor0,2,4,7days)producesamarkedantidepressant-likeeffectintheforcedswimmingtest(FST)withratsandmicewithoutaffectingthegenerallocomotoractivity[1].AnimalModel:Wistarstrainofrats(140-245g)[1]Dosage:0.3-100mg/kgAdministration:P.o.;dailyfor0,2,4,7daysResult:Asingledosesof1mg/kgandhigherofOPC-14523reducedimmobilitytimeintheFSTwithanED50valueof27mg/kg.TheED50valueforOPC-14523onday7was18mg/kg.AnimalModel:ICRstrainofmice(25-45g)[1]Dosage:0.3-100mg/kgAdministration:P.o.;dailyfor0,2,4,7daysResult:AsingleoraldoseofOPC-14523producedamarkedreductioninimmobilitytimeduringtheFSTatoraldosesof1mg/kgandhigher,withanED50valueof20mg/kg.ThepotencyofOPC-14523indecreasingimmobilitytimewasgreateraftertreatmentforsevenconsecutivedays,producinganED50valueof2mg/kg.REFERENCES[1].TottoriK,etal.Antidepressant-likeresponsestothecombinedsigmaand5-HT1AreceptoragonistOPC-14523.Neuropharmacology.2001;41(8):976-988.[2].BermackJE,etal.EffectsofthepotentialantidepressantOPC-14523[1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinonemonomethanesulfonate]acombinedsigmaand5-HT1Aligand:modulationofneuronalactivityinthedorsalraphenucleus.JPharmacolExpTher.2004;310(2):578-583.McePdfHeight2/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidated