Brompheniramine-racemic-Brompheniramine-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBrompheniramineCat.No.:HY-B0480ACASNo.:86-22-6Synonyms:(±)-Brompheniramine分?式:C??H??BrN?分?量:319.24作?靶點(diǎn):HistamineReceptor;mAChR;PotassiumChannel;SodiumChannel;CalciumChannel作?通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling;MembraneTransporter/IonChannel儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Brompheniramine((±)-Brompheniramine)?種有效的?服有效的烷胺類抗組胺藥。Brompheniramine?種選擇性組胺H1受體(histamineH1receptor)拮抗劑，Kd為6.06nM。Brompheniramine可阻斷hERG通道(hERGchannels)、鈣離?通道(calciumchannels)和鈉離?通道(sodiumchannels)，IC50分別為0.90μM、16.12μM和21.26μM。Brompheniramine具有抗膽堿能、抗抑郁以及?醉作?，可?于過敏性?炎和緩解疼痛的研究。體外研究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].體內(nèi)研究Brompheniramine(0.3-3?μM;SC,singledosage)inducescutaneousanalgesiainrats[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MaleSprague-Dawleyrats[1]Dosage:0.3,0.6,1.1,1.5and3.0?μMAdministration:SC,singledosageResult:Provokedcutaneousanalgesiainadose-dependentmanner,withanEC50valueof0.66μM,andinducedprolongedanalgesicduration.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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