Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZotepineCat.No.:HY-103093CASNo.:26615-21-4分?式:C??H??ClNOS分?量:331.86作?靶點(diǎn):5-HTReceptor;HistamineReceptor;AdrenergicReceptor;DopamineReceptor作?通路:GPCR/GProtein;NeuronalSignaling;Immunology/Inflammation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)DMSO:25mg/mL(75.33mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0133mL15.0666mL30.1332mL5mM0.6027mL3.0133mL6.0266mL10mM0.3013mL1.5067mL3.0133mL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(chǔ)備液；?旦配成溶液，請分裝保存，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?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.53mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Zotepine，?種抗精神病劑，有效的5-HT2A，5-HT2C，組胺H1，α1-adrenergic和多巴胺D2受體拮抗劑，Kd值分別為2.6nM、3.2nM、3.3nM、7.3nM和8nM。Zotepine在體內(nèi)表現(xiàn)出抗抑郁和抗焦慮作?。體外研究Zotepineshowsmultipleantagonisticprofileswithstrongaffinitiestoα1-adrenergic,α2-adrenergic,DopamineD2,HistamineH1,Muscarinic,5-HT1A,5-HT1D,5-HT2A,and5-HT2Creceptors,withKdsof7.3,180,8,3.3,330,280,80,2.6,3.2nM,respectively[1].體內(nèi)研究Zotepine(1-3mg/kg;asinglei.p.)dose-dependentlyincreasesnoradrenaline,dopamine,GABA,andglutamatereleasewithoutaffecting5-HTlevelsinthemedialprefrontalcortexofrats[2].AnimalModel:MaleSprague-Dawleyrats(250-300g)[1]Dosage:1,3mg/kgAdministration:Asinglei.p.Result:Increasednoradrenaline,dopamine,GABA,andglutamatereleasewithoutaffecting5-HTlevelsinthemedialprefrontalcortex.IncreasedneuronalfiringfrequenciesintheVTA,DRN,LCandMTNinadose-dependentmanner.REFERENCES[1].RichelsonE,et,al.Bindingofantipsychoticdrugstohumanbrainreceptorsfocusonnewergenerationcompounds.LifeSci.2000Nov24;68(1):29-39.[2].YamamuraS,et,al.Effectsofzotepineonextracellularlevelsofmonoamine,GABAandglutamateinratprefrontalcortex.BrJPharmacol.2009Jun;157(4):656-65.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre