Iloperidone-d3-hydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEIloperidone-d3hydrochlorideCat.No.:HY-17410S1分子式:C₂₄H₂₅D₃ClFN₂O₄分子量:465.96作用靶点:DopamineReceptor;5-HTReceptor;Isotope-LabeledCompounds作用通路:GPCR/GProtein;NeuronalSignaling;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Iloperidone-d3hydrochloride是氘代标记的Iloperidone(HY-17410)。Iloperidone(HP873)是一种D2/5-HT2受体拮抗剂，可作用于精神分裂症的非典型抗精神病药。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].IloperidonedisplayshigheraffinityforthedopamineD3receptor(Ki=7.1nM)thanforthedopamineD4receptor(Ki=25nM).Iloperidonedisplayshighaffinityforthe5-HT6and5-HT7receptors(Ki=42.7and21.6nM,respectively),andisfoundtohavehigheraffinityforthe5-HT2A(Ki=5.6nM)thanforthe5-HT2Creceptor(Ki=42.8nM)[2].体内研究Iloperidoneiseliminatedslowly,withameant1/2of13.5to14.0hours.CoadministrationwithfooddidnotsignificantlyaffectAUC,tmax,orCmax.Theseresultsindicatethattherateofiloperidone'sabsorptionisdecreased,buttheoverallbioavailabilityisunchanged,whenthedrugistakenwithfood.Orthostatichypotension,dizziness,andsomnolencewerethemostcommonlyreportedadverseevents[3].REFERENCESKongsamut,S.,etal.,Iloperidonebindingtohumanandratdopamineand5-HTreceptors.EurJPharmacol,1996.317(2-3):p.417-23.Sainati,S.M.,etal.,Safety,tolerability,andeffectoffoodonthepharmacokineticsofiloperidone(HP873),apotentialatypicalantipsychotic.JClinPharmacol,1995.35(7):p.713-20.Albers,L.J.,A.Musenga,andM.A.Raggi,Iloperidone:anewbenzisoxazoleatypicalantipsychoticdrug.Isitnovelenoughtoimpactthecrowdedatypicalantipsychoticmarket?ExpertOpinInvestigDrugs,2008.17(1):p.61-75.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemERussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch