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Traceamine1(TA1)receptorantagonist/inverseagonist;exhibitsahigherpotencyatthemouseTA1receptorthantheratandhumanTA1receptors(IC50valuesare27.5,4539and7487nM,respectively).BlockstheTA1receptor-mediatedactivationofaninwardlyrectifyingK+current,whichincreasesthefiringfrequencyofdopamine(DA)neuronsintheventraltegmentalarea.IncreasesDApotencyattheD2receptor.Alsodisplaysinverseagonism,reducingbasalcAMPlevelsinvitro(IC50=19nM).
EPPTBisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight378.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Bradaiaetal(2009)TheselectiveantagonistEPPTBrevealsTAAR1-mediatedregulatorymechanismsindopaminergicneuronsofthemesolimbicsystem.Proc.Natl.Acad.Sci.U.S.A.10620081PMID:19892733
Keywords:EPPTB,supplier,Parkinson"s,disease,trace,amine-associated,receptors,1,TAAR1,antagonists,dopamine,neurons,neurones,TA1,Trace,Amine,1,Receptor,Trace,Amine,1,Receptor,TocrisBioscience
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