Isradipine-d7-PN-200-110-d-sub-7-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEIsradipine-d7Cat.No.:HY-B0233S2Synonyms:PN200-110-d7分子式:C₁₉H₁₄D₇N₃O₅分子量:378.43作用靶点:CalciumChannel;Autophagy;Isotope-LabeledCompounds作用通路:MembraneTransporter/IonChannel;NeuronalSignaling;Autophagy;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Isradipine-d7是氘代标记的Isradipine(HY-B0233)。Isradipine(PN200-110)是一个具有口服活性的L型钙通道阻滞剂。Isradipine是一种强效外周血管扩张剂，是一种二氢吡啶钙拮抗剂，对心脏和外周循环有选择性作用。Isradipine是一种潜在可行的帕金森病神经保护剂[1][2][3]。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Isradipinehasmuchhigher(＞40fold)affinityforCav1.3channelsaswellasgoodbrainbioavailability.IsradipinehasnearlyequalpotencyatCav1.2andCav1.3channels[2].体内研究Isradipine(0.1~3mg/kg;p.o.)makessodiumexcretionincreaseinadose-dependentmanner[4].Isradipinepre-treatmentreduces6-hydroxydopamineinducedneurotoxicityatthestriatallevel.Protectiveeffectofisradipineatthestriatallevelisdose-dependentasshownfrom6mice.Isradipinepre-treatmentincreasesthenumberofsurvivingSNcDAcellsafter6-hydroxydopamineinduceddegeneration.IsradipineiscapableofprotectingstriataldopaminergicterminalsandSNcdopaminergiccellbodiesagainstaslow,progressiveinsultcreatedbyintrastriatalinjectionof6-hydroxydopamine[2].REFERENCESIlijicE,etal.TheL-typechannelantagonistisradipineisneuroprotectiveinamousemodelofParkinson'sdisease.NeurobiolDis.2011;43(2):364-371.CampbellCA,etal.Effectsofisradipine,anL-typecalciumchannelblockeronpermanentandtransientfocalcerebralischemiain1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEspontaneouslyhypertensiverats.ExpNeurol.1997;148(1):45-50.HofRP,etal.SelectiveeffectsofPN200-110(isradipine)ontheperipheralcirculationandtheheart.AmJCardiol.1987;59(3):30B-36B.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear