Sameridine-NIH-10908-free-base-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESameridineCat.No.:HY-105525CASNo.:143257-97-0Synonyms:NIH10908freebase分⼦式:C₂₁H₃₄N₂O分⼦量:330.51作⽤靶点:OpioidReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Sameridine(NIH-10908)μ-阿⽚受体的弱部分激动剂。鞘内注射Sameridine可产⽣局部⿇醉和镇痛作⽤。低剂量Sameridine对呼吸抑制作⽤极⼩，但⾼剂量可抑制呼吸反应。Sameridine可⽤于镇痛作⽤的研究[1][2]。IC50&TargetμOpioidReceptor/MOR体内研究Sameridine(5-10mg/mL(10μL),intrathecalinjection,twicedaily,fivedaysaweek,fortwoweeks)didnotinducesignificantneurotoxicityinaratmodelafterintrathecalinjection[3].AnimalModel:MaleSprague-Dawleyrats(weighing320-420g)[1].Dosage:5mg/mL(10μL),10mg/mL(10μL)Administration:Intrathecalinjection,twicedaily,fivedaysaweek,fortwoweeks.Result:Nopermanentmotorimpairmentwasobservedinanygroup.ThedorsalhornneuronsintheL1segmentofthespinalcordshowednormalmorphology,andnosignsofneurotoxicitywerefound,suchasedema,organelledamage,necrosis,ormicroglia.REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].MulroyMF,etal.Sameridineissafeandeffectiveforspinalanesthesia:acomparativedose-rangingstudywithlidocaineforinguinalherniarepair.AnesthAnalg.1999Apr;88(4):815-21.[2].OsterlundA,etal.Theeffectsonrestingventilationofintravenousinfusionsofmorphineorsameridine,anovelmoleculewithbothlocalanestheticandopioidproperties.AnesthAnalg.1999Jan;88(1):160-5.[3].KarlstenR,etal.Sameridine--intrathecalinjectionintherat.Morphometricandmorphologicanalysisafterchronicadministrationandeffectsonspinalcordbloodflow.ActaAnaesthesiolScand.1999May;43(5):573-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-