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Potentandselectivenociceptin/orphaninFQ(NOP)receptorantagonist(pA2=7.75).DisplaysselectivityforNOPreceptorsoverclassicalopioidreceptors(pKivaluesare8.65,6.60,6.14and<5forNOP,μ-,κ-,andδ-opioidreceptorsrespectively).AttenuatesmotordeficitsinaratmodelofParkinson'sDisease.Activeinvivo.
Trap101isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight434.02.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Trapellaetal(2006)IdentificationofanachiralanalogueofJ-113397aspotentnociceptin/orphaninFQreceptorantagonist.Bioorg.Med.Chem.14692PMID:16202610
Martietal(2008)Thenovelnociceptin/orphaninFQreceptorantagonistTrap-101alleviatesexperimentalparkinsonismthroughinhibitionofthenigro-thalamicpathway:positiveinteractionwithL-DOPA.J.NeuRochem.1071683PMID:19014386
Keywords:Trap101,supplier,Potent,selective,NOP,antagonists,Nociceptin,Receptors,ORL1,OP4,Opioid,Trap101,Parkinsons,disease,antiparkinsons,active,in,vivo,NOP,Receptors,NOP,Receptors,TocrisBioscience
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