Meeting Banner
Abstract #1614

New Bifunctional Chelates with Optimal Water Residence Times for Molecular Imaging

Erik C. Wiener1, Raghvendra Sengar2, Luce Vander Elst3, Marie-Caline Abadjian4, Curtis E. Moore5, Arnold L. Rheingold5, Douglas Grotjahn6

1University of Pittsburgh, Pittsburgh, PA, United States; 2University of Pittsburgh, Johnstown, United States; 3General, Organic and Biomedical Chemistry, University of Mons, Mons, Belgium; 4San Diego State University, United States; 5University of California, San Diego, CA, United States; 6San Diego State University, San Diego, CA, United States

MRI offers the promise of molecular and cellular imaging by using exogenous or endogenous markers. Using exogenous stains requires suitable concentrations at the desired target by delivery of large numbers of paramagnetic or super paramagnetic ions, or a smaller number of more highly efficient agents. This report presents the syntheses of two new bifunctional Gd(III) chelates, with optimal water exchange rates, that can be coupled to other molecules using either click or peptide coupling chemistry. Nuclear magnetic relaxation dispersion experiments demonstrate 100% higher relaxivities then their slower exchange rate controls. Water residence times are measured using 17O NMR.

Abstract PDF

Keywords

acid acids actual agents analog analogs approved argon available biomedical biotin buffer cellular champaign characterization chart chelate chem chemistry circles clearance click clinically closed comparative complex complexes concentrations conserved constrained contrast controls coupled coupling covalently crystallographic cycling delivery derivative derivatives described desired determined distilled dose drug efficiencies efficiency efficient either enormous exchange exchanging exogenous experimental fast field form functionality gadolinium general grade heated highly indicated inductively inner invented ions isomer issues kinetically limited long macromolecular made maintaining majority markers mass measured media modular molecular muller multiplexed nitric nuclear offers open optima optimal organic paramagnetic physiochemical plasma polymeric potential prepared process profiles promise properties property proton ranging rapid reduce reduces relatively report reported require requires residence room rotational rotationally sample samples sensitivity shipped shorter solutions spectra spectrometry sphere spin squares stains studies suitable super synthesis system systems table target temperature theoretical toxicity transferred treatment tubes variable various versatility vial water weeks wiener