TMU4142-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETMU4142Cat.No.:HY-179579分⼦式:C₂₃H₃₁N₃O₄分⼦量:413.51作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性TMU4142⼀种具有⾼GoA活性的选择性5-HT1a激动剂。TMU4142的Gi3活性较弱，能够在不显著激活DRN区5-HT1A⾃⾝受体的情况下快速产⽣抗抑郁样效应或抑制⾎素能神经元放电。TMU4142在抑郁⼩⿏模型中显⽰出快速起效抗抑郁效果。TMU4142可⽤于抗抑郁研究[1]。IC50&Target5-HT1AReceptor5-HT1AReceptor体外研究TMU4142agonistGoAsignalingpathwayandweakactivityattheGi3pathway,showsnodiscernibleactivityattheβ-arrestin-2pathwayassociatedwiththe5-HT1Areceptor,demonstratesahigherpotencyatthe5-HT1Areceptorwhilereducingactivityatβ-adrenergicreceptors[1].体内研究TMU414(0.3or1.5mg/kg,i.p.)hasGoA-biasedwithminimalGi3activity,selectivelyactivatestheGoAsignalingpathway(primarilylocalizedpostsynapticallyandantidepressantresponses)whileavoidingtheGi3-mediatedfeedbackofpresynapticautoreceptors,preserves5-HTsynthesisandreleaseintheDRNinchronicrestraintstress-induceddepressionmodelinC57BL/6mice[1].AnimalModel:Chronicrestraintstress(CRS)-induceddepressionmodelinmaleC57BL/6Jmice(8-12weeks)[1]Dosage:0.3or1.5mg/kgAdministration:i.p.,onceResult:SignificantlyreducedtheimmobilitytimeofCRSmiceintheforcedswimtest(FST)30minpost-injectionindicatinganantidepressant-likeeffect.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEReversedCRS-induceddepressive-likebehaviorsinmiceat1.5mg/kg.Elicitedsignificantantidepressant-likeeffectsExertedantidepressant-likeeffectsinCRSmicethrough5-HTARꢀRactivation,asdemonstratedbytheblockadeoftheimmobility-reducingeffectsintheFSTandtailsuspensiontest(TST)bytheantagonistWAY100635(Y-10349).AbolishedthereductioninimmobilitytimeinboththeFSTandTSTindicatedthattheantidepressant-likeeffectsaremediatedthroughtheactivationof5-HTAR.Significantlyreducedthelatencytofeedinmiceasearlyas1hafterdrugadministrationwithoutaffectingthehomecagefoodintake.HasacuteeffectintheNSFtestwasblockedbyway-100635,suggestingthatitsactionismediatedthrough5-HT1aRactivation.DidnotalterDRN5-HTlevelsinCRSmice.REFERENCES[1].WangC,etal.Pathway-selective5-HT1ARagonistasarapidantidepressantstrategy.Cell.2025Dec11;188(25):7222-7237.e24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For