Orphenadrine-racemic-Orphenadrine-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEOrphenadrineCat.No.:HY-157959CASNo.:83-98-7Synonyms:(±)-Orphenadrine分子式:C₁₈H₂₃NO分子量:269.38作用靶点:iGluR;CytochromeP450;Cholinesterase(ChE)作用通路:MembraneTransporter/IonChannel;NeuronalSignaling;MetabolicEnzyme/Protease储存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY生物活性Orphenadrine((±)-Orphenadrine)是一种骨骼肌松弛剂和NMDA拮抗剂，还具有抗帕金森病、抗组胺、抗震颤、抗痉挛和镇痛的作用。Orphenadrine能够抑制剂[3H]MK-801与NMDA受体的苯环己哌啶(PCP)结合位点的结合。Orphenadrine还是抗胆碱能剂和细胞色素P450(CYP)2B诱导剂。Orphenadrine可能发挥促肿瘤作用，导致CAR核易位，导致微粒体活性氧(ROS)的产生和氧化应激。Orphenadrine还发挥神经细胞保护作用，可保护大鼠小脑颗粒细胞(CGC)免受3-NPA诱导的死亡，对NMDA受体过度激活介导的神经退行性疾病有抑制潜力。IC50&TargetNMDAreceptor[1];CYP4502B[2];Cholinesterase(ChE)[3]体外研究Orphenadrine(30-300μM)exhibitsrelativelyfastconcentration-dependentopenchannelblockingkineticswithaKoffof0.013[1].CellViabilityAssay[1]CellLine:NMDAopen-channelConcentration:30,100and300μMIncubationTime:5seconds;with200μMNMDA1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEResult:Nearlycompletelyinhibited[3H]MK-801bindingat100μM.Exhibitedrelativelyfast,concentration-dependentopenchannelblockingkinetics.体内研究Inastudyofthetumor-promotingeffectsofOrphenadrine,maleratswerepretreatedwithasingleintraperitonealinjectionofN-diethylnitrosamine(DEN)for2weeks.Orphenadrine(0,750,1500ppm;po;6wk)accelerateshepatocyteproliferationandinduceslivertumor-promotingactivity[2].Orphenadrine(30mg/kg;po;3d)YesProtectratsfromexposureto3-nitropropionicacid(3-NPA)(30mg/kg;3d),whichcausesneuronaldamageinastrocytes.Markers:[(3)H]-PK11195andIncreasedexpressionlevelsofHSP27[3].AnimalModel:Livertumormodelinmaleratspre-treatedbyN-diethylnitrosamine[2]Dosage:0,750,1500ppmAdministration:PO;for6weeksResult:IncreasedmRNAexpressionlevelsofCyp2b1/2,Mrp2andCyclinD1.Increasedmicrosomalreactiveoxygenspecies(ROS)productionandoxidativestressmarkerssuchasthiobarbituricacid-reactivesubstancesand8-hydroxydeoxyguanosine.REFERENCESKornhuberJ,etal.OrphenadrineisanuncompetitiveN-methyl-D-aspartate(NMDA)receptorantagonist:bindingandpatchclampstudies.JNeuralTransmGenSect.1995;102(3):237-46.PubillD,etal.Orphenadrineprevents3-nitropropionicacid-inducedneurotoxicityinvitroandinvivo.BrJPharmacol.2001Feb;132(3):693-702.MoritaR,etal.LivertumorpromotingeffectoforphenadrineinratsanditspossiblemechanismofactionincludingCARactivationandoxidativestress.JToxicolSci.2013;38(3):403-13.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica