Osutidine-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOsutidineCat.No.:HY-105101CASNo.:140695-21-2分⼦式:C₁₉H₂₈N₄O₅S₂分⼦量:456.58作⽤靶点:HistamineReceptor作⽤通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Osutidine⼀种选择性组胺H2受体拮抗剂，能有效抑制组胺刺激的胃酸分泌。Osutidine不响卡巴胆碱或⼆丁酰环磷酸腺苷刺激的[¹⁴C]氨⽐林的蓄积。Osutidine具有不可逆抑制作⽤，包括⾮竞争性抑制。Osutidine可⽤于胃粘膜损伤的研究[1][2]。IC50&TargetH2Receptor体外研究Osutidine(T-593)inhibitstheaccumulationof10-4Mhistamine-stimulated[14C]APinisolatedcaninegastricmucosalcellsinaconcentration-dependentmanner,withanIC50of1.85×10-6M[1].Osutidineonlyslightlyinhibitstheaccumulationof[14C]APstimulatedby10-4MdbcAMPinisolatedcaninegastricmucosalcells(maximuminhibitionof20-32%)[1].Osutidineshiftsthehistamineconcentration-responsecurvetotherightandreducesthemaximumresponseinisolatedcaninegastricmucosalcells,withaSchildplotslopeof2.01,indicatingthatH2receptorantagonismisinsurmountableandnon-competitive[1].OsutidinebindstightlytoH2receptorsinisolatedcaninegastricmucosalcellsandisdifficulttoreversebywashing,indicatingthatithasslowdissociationproperties[1].Osutidinehas(-)-S-T-593asitsmainactiveenantiomerresponsibleforH2receptorantagonism,while(+)-R-T-593exhibitsweakactivity[1].体内研究Osutidine(T-593)(6-60mg/kg,i.p.,once)hasasignificantprotectiveeffectonthegastricmucosainSprague-Dawleyrats,significantlyinhibitingethanol-inducedgastricmucosaldamageinadose-dependentmanner[2].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleSprague-Dawleyrats,weighing200-230grams,wereanesthetizedwithsodiumpentobarbital(35mg/kg)and1mlof40%ethanolsolutionwasadministeredviagastrictubetoinduceacutegastricmucosalinjury[2].Dosage:6mg/kg,60mg/kgAdministration:I.p.,onceResult:Significantlyinhibitedethanol-inducedgastricmucosaldamageinadose-dependentmanner.AnimalModel:MaleSprague-Dawleyrats,weighing200-230grams,wereanesthetizedwithsodiumpentobarbital(35mg/kg)and1mlof40%ethanolsolutionwasadministeredviagastrictubetoinduceacutegastricmucosalinjury[2].Dosage:60mg/kgRacemicT-593,60mg/kg(+)-(R)-T-593,60mg/kg(-)-(S)-T-593Administration:I.p.,onceResult:Significantlyinhibitedethanol-inducedgastricdamage,buttheprotectiveeffectoftheracemicmixtureissignificantlystrongerthanthatofitsindividualenantiomer.Directlyimprovedgastricmucosalmicrocirculationandeffectivelyinhibitedgastricacidsecretion,significantlyreducingtheoxygenconsumptionofparietalcells,therebyalleviatingmucosalhypoxia.REFERENCES[1].InoieM,etal.HistamineH2-receptorantagonismofOsutidine,ananti-ulceragent:studiesonaminopyrineaccumulationinisolatedcaninegastricmucosalcells.JpnJPharmacol.1998Nov;78(3):313-22.[2].TsujiS,etal.Effectsofosutidine(T-593)anditsenantiomersongastricmucosalhemodynamicsandmucosalintegrityinanesthetizedrats.Arzneimittelforschung.2001Jan;51(1):46-50.McePdfHeightCaution:Producthasnotbeenfullyv