RWJ52353-hydrochloride-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemERWJ52353hydrochlorideCat.No.:HY-103216ACASNo.:245744-13-2分子式:C₁₁H₁₁ClN₂S分子量:238.74作用靶点:AdrenergicReceptor作用通路:GPCR/GProtein;NeuronalSignaling储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性RWJ-52353hydrochloride是口服有效、高选择性的α2D肾上腺素能受体的激动剂(Ki:1.5nM)，具有潜在镇痛作用。RWJ-52353hydrochloride在大鼠和小鼠的腹部测试实验中均表现出镇痛活性，并改善小鼠在热板实验和甩尾实验中的焦躁情况。RWJ-52353hydrochloride还调节有机阳离子转运蛋白(OCT)亚型，抑制rOCT1和rOCT2的IC50s分别为100μM和20μM；同时激活rOCT3，影响细胞中[3H]-1-甲基-4-苯基吡啶鎓([3H]MPP)转运。IC50&TargetKi:1.5nM(α2DAR),254nM(α2AAR),621nM(α2BAR),443nM(α1AR)[1]IC50:100μM(rOCT1),20μM(rOCT2)[2]体内研究RWJ-52353(30mg/kg;po;singledose)hydrochloridehasaninhibitoryeffectontheinducedabdominalpainmodelinmice,withaninhibitionrateof100%[1].RWJ-52353TheED50sinthemouseabdominalpainmodelare15.1mg/kg(po)and11.6mg/kg(po)respectively[1].RWJ-52353canalsoreducetheriskofmiceinthehotplatetest(48°C)andshakingThedegreeofpaininthetailexperiment,ED50sare25.9mg/kg(po)and100.2mg/kg(po)respectively[1].REFERENCESRossTM,etal.α2Adrenoceptoragonistsaspotentialanalgesicagents.2.Discoveryof4-(4-imidazo)-1,3-dimethyl-6,7-dihydrothianaphtheneasahigh-affinityligandfortheα2Dadrenergicreceptor[J].Journalofmedicinalchemistry,2000,43(7):1423-1426.AmphouxA,etal.Inhibitoryandfacilitoryactionsofisocyaninederivativesathumanandratorganiccationtransporters1,2and3:acomparisontohumanalpha1-andalpha2-adrenoceptorsubtypes.EurJPharmacol.2010May25;634(1-3):1-9.McePdfHeight1/1 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792