Guanfacine-15N3-13C2-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEGuanfacine-15N3,13C2Cat.No.:HY-17416AS1分子式:C₇₁₃C₂H₉Cl₂₁₅N₃O分子量:251.06作用靶点:AdrenergicReceptor;Isotope-LabeledCompounds作用通路:GPCR/GProtein;NeuronalSignaling;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Guanfacine-15N3,13C2是15N和13C标记的Guanfacine(HY-17416A)。Guanfacine是一种去甲肾上腺素能α2A激动剂，具有口服活性，对α2A受体亚型具有高度选择性。Guanfacine具有产生低血压和镇静作用。Guanfacine可用于研究多种PFC认知障碍，包括妥瑞氏综合征和注意力缺陷多动障碍(ADHD)。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Guanfacineincreasesthedelay-relatedneuronalfiringneededforworkingmemoryondIPFCneuronsatthecellularlevel[2][4].GuanfacineimprovesPFCcognitivefunctionbyinhibitingtheproductionofCAMP,closingHCNchannels,andstrengtheningthePFCnetworks[2][4].体内研究GuanfacineenhancesPFCworkingmemoryfunctioninagedmonkeysandimprovesimpulsecontrolinmonkeysperformingadelayeddiscountingtask[2][4].GuanfacineimprovescognitiveperformancewheninfuseddirectlyintotheratormonkeyPFC[2][4].Guanfacineblocks2AreceptorsinthemonkeydIPFCmarkedlyimpairsworkingmemory,behavioralinhibitionandgreatlyreducespersistentneuronalfiring[2][4].REFERENCESAmyFTArnsten,etal.Guanfacineforthetreatmentofcognitivedisorders:acenturyofdiscoveriesatYale.YaleJBiolMed.2012Mar;85(1):45-58.Epub2012Mar29.P.A.VanZwieten,etal.Thepharmacologyofcentrallyactingantihypertensivedrugs.BrJClinPharmacol.1983;15(Suppl4):1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE455S–462S.MinWang,etal.Alpha2A-adrenoceptorsstrengthenworkingmemorynetworksbyinhibitingcAMP-HCNchannelsignalinginprefrontalcortex.Cell.2007Apr20;129(2):397-410.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse