Avizafone-dihydrobromide-Pro-diazepam-dihydrobromide-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAvizafonedihydrobromideCat.No.:HY-W702001CASNo.:60067-15-4Synonyms:Pro-diazepamdihydrobromide分⼦式:C₂₂H₂₉Br₂ClN₄O₃分⼦量:592.75作⽤靶点:DrugIntermediate作⽤通路:Others储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)BIOLOGICALACTIVITY⽣物活性Avizafone(Pro-diazepam)dihydrobromide地西泮的前体药物，具有抗惊厥作⽤。Avizafonedihydrobromide可⽤作神经毒剂中毒的解毒剂。在体内，Avizafonedihydrobromide可被氨肽酶迅速⽔解，⽣成赖氨酸和地西泮。Avizafonedihydrobromide的研究领域包括神经系统疾病，例如癫痫。体内研究Avizafonedihydrobromide(3.5mg/kg;i.m.;singledose)preventsseizures,reducesclinicalsigns,eliminates24-hourmortality,andmitigatesbrainlesionsinCharlesRiverguineapigs(somanpoisoned)(witha24-hourmortalityrateof0%)[2].AnimalModel:Guineapigs(300-350g)[2]Dosage:3.5mg/kgAdministration:i.m.;singledoseResult:Reducedclinicalsignseveritytoscore1vs.3incontrols,achieved0%24-hourmortality,preventedseizuresin0/8animals,reducednecrosisto3/8animalsvs.4/4incontrols,eliminatedperivascularcuffsandedema,preventedseizuresin0/8animalsvs.4/8withdiazepam,eliminatedbrainlesions,andshowednosignificantrespiratoryparametermodifications.REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].LallementG,etal.Comparedefficacyofdiazepamoravizafonetopreventsoman-inducedelectroencephalographicdisturbancesandneuropathologyinprimates:relationshiptoplasmaticbenzodiazepinepharmacokinetics.ArchToxicol.2000Oct;74(8):480-6.[2].TaysseL,etal.Protectionagainstsoman-inducedneuropathologyandrespiratoryfailure:acomparisonoftheefficacyofdiazepamandavizafoneinguineapig.Toxicology.2006;225(1):25-35.[3].ClairP,etal.Stabilitystudyofanewantidotedrugcombination(Atropine-HI-6-Prodiazepam)fortreatmentoforganophosphatepoisoning.EurJPharmSci.2000Jan;9(3):259-63.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4