Brompheniramine-racemic-Brompheniramine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBrompheniramineCat.No.:HY-B0480ACASNo.:86-22-6Synonyms:(±)-Brompheniramine分⼦式:C₁₆H₁₉BrN₂分⼦量:319.24作⽤靶点:HistamineReceptor;mAChR;PotassiumChannel;SodiumChannel;CalciumChannel作⽤通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling;MembraneTransporter/IonChannel储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Brompheniramine((±)-Brompheniramine)⼀种有效的⼝服有效的烷胺类抗组胺药。Brompheniramine⼀种选择性组胺H1受体(histamineH1receptor)拮抗剂，Kd为6.06nM。Brompheniramine可阻断hERG通道(hERGchannels)、钙离⼦通道(calciumchannels)和钠离⼦通道(sodiumchannels)，IC50分别为0.90μM、16.12μM和21.26μM。Brompheniramine具有抗胆碱能、抗抑郁以及⿇醉作⽤，可⽤于过敏性⿐炎和缓解疼痛的研究。体外研究Brompheniramine(0.1-100μM)blockshERGK+channelsexpressedinCHOcellsinaconcentration-dependentmannerwithanIC50of0.90±0.14μM,andreducedpeaktailcurrentamplitudemeasuredat-60mV(cellsaredepolarizedfor2sto+20mVfromaholdingpotentialof-80mVfollowedbya3srepolarizationbackto-60mV)[3].Brompheniramine(1,10and100μM)significantlyshortenstheAPD50anddepressestheplateauphaseontheactionpotentialinguineapigpapillarymuscle,aswellasslightlyprolongstheAPD90inguineapigpapillarymuscleat10and100μM[3].Brompheniramine(0.1-100μM)inhibittheamplitudeoftheCa2+channelcurrentsinratventricularmyocytesby14.1±1.1,31.1±5.8,38.0±3.8and90.2±3.7%at0.1,1,10and100μM,respectively[3].Brompheniramineblocksmuscariniccholinergicreceptorsinhumanchinesehamsterovary(CHO)cells[4].体内研究Brompheniramine(0.3-3ꢀμM;SC,singledosage)inducescutaneousanalgesiainrats[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleSprague-Dawleyrats[1]Dosage:0.3,0.6,1.1,1.5and3.0ꢀμMAdministration:SC,singledosageResult:Provokedcutaneousanalgesiainadose-dependentmanner,withanEC50valueof0.66μM,andinducedprolongedanalgesicduration.户使⽤本产品发表的科研⽂献•Biomaterials.2021,120742.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Chong-ChiChiu,etal.Subcutaneousbrompheniramineforcutaneousanalgesiainrats.EurJPharmacol.2019Oct5;860:172544.[2].BCusack,etal.Bindingofantidepressantstohumanbrainreceptors:focusonnewergenerationcompounds.Psychopharmacology(Berl).1994May;114(4):559-65.[3].ShinWH,KimKS,KimEJ.Electrophysiologicaleffectsofbrompheniramineoncardiacionchannelsandactionpotential.PharmacolRes.2006Dec;54(6):414-20.[4].YasudaSU,YasudaRP.Affinitiesofbrompheniramine,chlorpheniramine,andterfenadineatthefivehumanmuscariniccholinergicreceptorsubtypes.Pharmacotherapy.1999Apr;19(4):447-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical