Clozapine-dihydrochloride-HF-1854-dihydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEClozapinedihydrochlorideCat.No.:HY-14539BCASNo.:2711603-38-0Synonyms:HF1854dihydrochloride分⼦式:C₁₈H₂₁Cl₃N₄分⼦量:399.75作⽤靶点:DopamineReceptor;mAChR;AdrenergicReceptor;5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Clozapine(HF1854)dihydrochloride可⽤于研究精神类疾病。Clozapine对许多神经受体有⾼度的亲和⼒，多巴胺受体的有效拮抗剂，Ki值为75nM。Clozapine抑制毒蕈碱M1受体和⾎素5HT2A受体，Ki值分别为9.5nM和4nM。Clozapine也选择性的毒蕈碱M4受体的激动剂(EC50=11nM)。IC50&Target5-HT2AReceptor5-HT6Receptor5-HT7ReceptormAChR14nM(Ki)9.5nM(Ki)mAChR4α2-adrenergicD2Receptor11nM(EC50)receptor75nM(Ki)51nM(Ki)体外研究Clozapine(HF1854)isaD2receptorantagonistwithaKiof75nM,blockstheserotonin5HT2AreceptorwithaKiof4nM,inhibitsthemuscarinicM1receptorwithaKiof9.5nM,blocksα2-adrenoceptorwithaKivalueof51nM[1].Clozapine(0-1μM;24h)downregulates5-HT6andupregulates5-HT7receptorsinHeLacells[2].ClozapineisafullagonistatthemuscarinicM4receptor(EC50=11nM)expressedinCHOcells[4].体内研究Clozapine(HF1854)(25mg/kg/day;i.p.;21days)showsantipsychoticeffectsinlysergicaciddiethylamide-inducedpsychosismousemodel[3].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Male129S6/Svmice,lysergicaciddiethylamide(LSD)-inducedpsychosismodel[3].Dosage:25mg/kg/day.Administration:Intraperitonealinjection,21days.Result:Decreasedhead-twitchresponse,reduced5-HT2AmRNA,rescuedinductionofc-fos,butnotegr-1andegr-2.户使⽤本产品发表的科研⽂献•NatCommun.2024Sep1;15(1):7603.•MolPsychiatry.2021Jun;26(6):2514-2532.•FEBSJ.2024Aug26.•EurJPharmSci.2023May22;106475.•EurJPharmSci.2021,105889.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SeemanP,etal.Clozapine,afast-off-D2antipsychotic.ACSChemNeurosci.2014Jan15;5(1):24-9.[2].ZhukovskayaNL,etal.Clozapinedownregulates5-hydroxytryptamine6(5-HT6)andupregulates5-HT7receptorsinHeLacells.NeurosciLett.2000Jul21;288(3):236-40.[3].MorenoJL,etal.PersistenteffectsofchronicclozapineonthecellularandbehavioralresponsestoLSDinmice.Psychopharmacology(Berl).2013Jan;225(1):217-26.[4].ZornSH,etal.ClozapineisapotentandselectivemuscarinicM4receptoragonist.EurJPharmacol.1994Nov15;269(3):R1-2.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo