OPC-14523-hydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEOPC-14523hydrochlorideCat.No.:HY-116594ACASNo.:145969-31-9分?式:C??H??Cl?N?O?分?量:450.4作?靶點:SigmaReceptor;5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(185.01mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2202mL11.1012mL22.2025mL5mM0.4440mL2.2202mL4.4405mL10mM0.2220mL1.1101mL2.2202mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.62mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.62mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.62mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性OPC-14523hydrochloride?種具有?服活性的sigma和5-HT1A受體激動劑，對sigma受體(σ1/2IC50=47/56nM)、5-HT1A受體(IC50=2.3nM)和5-HT轉運體(IC50=80nM)具有?度親和?。OPC-14523hydrochloride顯?抗抑郁藥樣活性。IC50&Target5-HT1AReceptorsigma1sigma22.3nM(IC50)47nM(IC50)56mM(IC50)體外研究OPC-14523hydrochlorideinhibitstheinvitroreuptakeof3H-5-HT(IC50=27nM),butitshowsveryweakinhibitoryactivityon3H-NEand3H-DAreuptake[1].體內研究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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidated