Fluvoxamine-13C-d3-maleate-DU-23000-sup-13-sup-C-d-sub-3-sub-maleate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEFluvoxamine-13C,d3maleateCat.No.: HY-B0103AS2Synonyms: DU-23000-13C,d3maleate分子式: C₁₈₁₃CH₂₂D₃F₃N₂O₆分子量: 438.42作用靶点: SerotoninTransporter;Isotope-LabeledCompounds作用通路: NeuronalSignaling;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Fluvoxamine-13C,d3maleate是13C和氘代标记的Fluvoxaminemaleate(HY-B0103A)。Fluvoxaminemaleate(DU-23000maleate)是5-羟色胺再吸收抑制剂，有抗抑郁活性。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].体内研究Fluvoxaminemaleate(DU-23000maleate)iseffectiveininhibiting5-HTuptakebybloodplateletsandbrainsynaptosomes.Theantagonismbyfluvoxamineofthereserpine-inducedloweringofthepentamethylenetetrazoleconvulsivethresholdcanberegardedasduetoaneffectupon5-HTuptake.Incontrasttotheeffectsofdesmethylimipramineandimipramine,nostimulatoryeffectsarefoundinratswhenrapidlyactingreserpine-likecompoundsaregivenfollowingadoseoffluvoxamine[2].Fluvoxamine(DU-23000)appearstoimprovecombat-relatedPTSDsymptomsbutnotdepressivesymptoms.Thehighattritionrateandlackofaplacebogrouplimitstheconclusionsofourstudy.ControlledstudiesoffluvoxamineinthetreatmentofPTSDarewarranted[3].Fluvoxamine(DU-23000)waslesspotentatdecreasingethanolself-administrationwhenfoodwasavailableconcurrentlyversuswhenethanolwasavailableinisolation[ED50:4.0(2.7-5.9)and5.1(4.3-6.0)].Effectsonfoodweresimilarundereachconditioninwhichfoodwasavailable.Theresultsdemonstratethatthepotencyoffluvoxamineinreducingethanol-maintainedbehaviordependsonwhetherethanolisavailableinisolationorinthecontextofconcurrentlyscheduledfoodreinforcement[4].REFERENCES1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEGinsburg,B.C.,J.W.Pinkston,andR.J.Lamb,Thepotencyoffluvoxaminetoreduceethanolself-administrationdecreaseswithconcurrentavailabilityoffood.BehavPharmacol,2012.23(2):p.134-42.Claassen,V.,etal.,Fluvoxamine,aspecific5-hydroxytryptamineuptakeinhibitor.BrJPharmacol,1977.60(4):p.505-16.Escalona,R.,etal.,Fluvoxaminetreatmentinveteranswithcombat-relatedpost-traumaticstressdisorder.DepressAnxiety,2002.15(1):p.29-33.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp