Procaterol-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEProcaterolCat.No.:HY-114732CASNo.:72332-33-3分子式:C??H??N?O?分子量:290.36作用靶點(diǎn):AdrenergicReceptor作用通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Procaterol是一種可口服的選擇性β2adrenergicreceptor激動(dòng)劑。Procaterol可通過環(huán)磷酸腺苷依賴性機(jī)制直接抑制嗜酸性粒細(xì)胞遷移和BEAS-2B細(xì)胞釋放嗜酸性粒細(xì)胞趨化活性因子。Procaterol對(duì)大鼠的支氣管擴(kuò)張作用和代謝作用存在較大的劑量差，可用于運(yùn)動(dòng)員哮喘研究[1]。IC50&Targetβ2adrenoceptor體外研究Procaterol(10-1000ng/mL,12,24,48h,BEAS-2B)directlyinhibitseosinophilmigrationandthereleaseofeosinophilchemotacticfactorfromBEAS-2BcellsthroughacyclicAMP-dependentmechanism[3].Procaterol(10-1000ng/mL,12,24,48h,BEAS-2B)Dose-dependentinhibitionofRANTESreleaseinresponsetoIL-1bandTNF-ainBEAS-2Bcellmonolayers,andenhancementofGM-CSFmRNAexpressioninresponsetoIL-1b[3].Procaterol(0.1μM,72h,Humantrachealsurfaceepithelialcells)reducerhinovirustitersandRNA,cytokineconcentrations,susceptibilitytorhinovirusinfection,andtheexpressionofintercellularadhesionmolecule-1(ICAM-1),thereceptorfortype14rhinovirus,andthenumberofacidicendosomesinthecellsfromwhichrhinovirusRNAentersintothecytoplasm[4].Procaterol(10nM,onetime,Lungepithelialcells)increasedciliarybendamplitude(CBA)andciliarybeatingfrequency(CBF)inadosedependentmannerviacAMP[5].CellMigrationAssay[3]CellLine:eosinophilConcentration:10,100,1000ng/mL1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:24hResult:Attenuatedtheeosinophilmigratoryresponseinadose-dependent.體內(nèi)研究Procaterol(0.03-1mg/kg,inhalation3timesaday,14days)hasnosignificantchangesinweightorbodyweightgaininratgastrocnemiusmuscle[1].Procaterol(1mg/kg,inhalation3timesaday,14days)significantlyincreasesweightofthelevatoranimusclewithanaboliceffects[1].Procaterol(1mg/kg,inhalation3timesaday,14days)increasesventralprostateweightisassociatedwithdrugstimulationofb2adrenergicreceptorsintissues[1].Procaterol(0.03-1mg/kg,inhalation3timesaday,14days)differentdosebetweenbronchodilatorandanaboliceffects>30-fold,[1].Procaterol(0.1,1,10mg/kg,orally,beforeovalbumin(HY-W250978)(OVA)inhalation)inhalerdoesnotenhanceairwayhyperresponsiveness,airwaywallinflammation,orairwaywallthickening,anddecreaseseosinophilnumber[2].AnimalModel:Six-week-oldratswerecastratedonDay–5,exceptforanormalgroupof6rats[1]Dosage:0.03,0.1,0.3,1mg/mLAdministration:in-halation3timesaday(09:00,12:00,16:00)for14daysfromDay0toDay13.Result:Nosignificantchangedinweightorbodyweightgaininratgastrocnemiusmuscle.Significantlyincreasedtheweightofthelevatoranimuscle.Increasdinventralprostateweight.AnimalModel:Miceimmunizedwithovalbumin(HY-W250978)(OVA,inhalationof20mg/mLOVAfor10minuteseveryotherday,total7times)+alum[2]Dosage:0.1,1,10mg/kgAdministration:orally,beforeovalbumin(HY-W250978)(OVA)inhalationResult:Inhalationdidnotenhanceairwayhyperresponsiveness,airwaywallinflammation,orairwaywallthickeningafterOVAinhalation.ReducedthenumberofeosinophilsinBALFmice.REFERENCESIkezonoK,etal.Bronchodilatingeffectandanaboliceffectofinhaledprocaterol.IntJSportsMed.2008Nov;29(11):888-94.TashimoH,etal.Effectofprocaterol,abeta(2)selectiveadrenergicreceptoragonist,onairwayinflammationandhyperresponsiveness.AllergolInt.2007Sep;56(3):241-7.KoyamaS,etal.ProcaterolinhibitsIL-1beta-andTNF-alpha-mediatedepithelialcelleosinophilchemotacticactivity.EurRespirJ.19992/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEOct;14(4):767-75.YamayaM,etal.Procaterolinhibitsrhinovirusinfectioninprimaryculturesofhumantrachealepithelialcells.EurJPharmacol.2011Jan10;650(1):431-44.Komatani-TamiyaN,etal.Procaterol-stimulatedincreasesinciliarybendamplitudeandciliarybeatfrequencyinmousebronchioles.CellPhysiolBiochem.2012;29(3-4):511-22.M