Lamotrigine-13C2-15N2-d3-LTG-13C2-15N2-d3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemELamotrigine-13C2,15N2,d3Cat.No.: HY-B0495S6Synonyms: LTG-13C2,15N2,d3;BW430C-13C2,15N2,d3分子式: C₇₁₃C₂H₅D₃Cl₂N₃₁₅N₂分子量: 264.09作用靶点: Autophagy;SodiumChannel;Isotope-LabeledCompounds作用通路: Autophagy;MembraneTransporter/IonChannel;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Lamotrigine-13C2,15N2,d3是15N和氘代标记的Lamotrigine(HY-B0495)。Lamotrigine(BW430C)是一种有效的，具有口服活性的抗惊厥或抗癫痫试剂(anticonvulsantagent)。Lamotrigine选择性地阻断电压门控钠离子通道(Na+channels)，稳定突触前神经元膜，抑制谷氨酸释放。Lamotrigine可用于癫痫、局灶性癫痫等的研究。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].LamotrigineinhibitsVeratrineevokedreleaseofglutamateandaspartatewithED50valuesof21μMforbothaminoacids,butLamotrigineislesspotentintheinhibitionofGABArelease(ED50=44μM.Atconcentrationsupto300μM,LTGhasnoeffectonpatassium-evokedaminoacid[2].?LamotrigineissomefivetimeslesspotentintheinhibitionofVeratrine-evoked[3H]acetylcholinerelease(ED50=100μM)thaninglutamateoraspartaterelease[2].体内研究Lamotrigine(IP,30minbeforepentylenetetrazol;10mg/kg,15mg/kgor20mg/kg)decreasestheseizureintensity?atthehigherdoses,itincreasesthelatencytothefirstpentylenetetrazol-inducedseizure?inallstudieddosescomparedwiththecontrols[3].REFERENCESMJLeach,etal.Pharmacologicalstudiesonlamotrigine,anovelpotentialantiepilepticdrug:II.Neurochemicalstudiesonthemechanismofaction.Epilepsia.Sep-Oct1986;27(5):490-7.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEDamiankaPGetova,etal.Astudyoftheeffectsoflamotrigineonmiceusingtwoconvulsivetests.FoliaMed(Plovdiv).Apr-Jun2011;53(2):57-62.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse