6533b821fe1ef96bd127baa2

RESEARCH PRODUCT

Heparin–polynitroxides: Synthesis and preliminary evaluation as cardiovascular EPR/MR imaging probes and extracellular space-targeted antioxidants

Stefan A. L. WeberMaxim TerekhovThomas MünzelValery G. GolubevVasily D. SenLaura M. SchreiberAndrei L. KleschyovDariush HinderbergerKerstin MünnemannKarl J. Lackner

subject

Nitroxide mediated radical polymerizationmedicine.drug_mechanism_of_actionFactor Xa InhibitorUronic acidAntioxidantslaw.inventionchemistry.chemical_compoundSuperoxideslawDrug DiscoverymedicineExtracellularHumansElectron paramagnetic resonancePharmacologyHeparinSuperoxideOrganic ChemistryElectron Spin Resonance SpectroscopyAnticoagulantsHexosaminesGeneral MedicineHeparinMagnetic Resonance ImagingExtracellular MatrixUronic AcidschemistryBiochemistryMolecular ProbesFactor XaNitrogen OxidesPartial Thromboplastin TimeEndothelium VascularFactor Xa Inhibitorsmedicine.drugMacromolecule

description

We report here the synthesis of heparin-polynitroxide derivatives (HPNs) in which nitroxide moieties are linked either to uronic acid or glycosamine residues of the heparin macromolecule. HPNs have low anticoagulant activity, possess superoxide scavenging properties, bind to the vascular endothelium/extra-cellular matrix and can be detected by EPR and MRI techniques. As the vascular wall-targeted redox-active paramagnetic compounds, HPNs may have both diagnostic (molecular MRI) and therapeutic (ecSOD mimics) applications.

https://doi.org/10.1016/j.ejmech.2012.09.028