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• W2329623800 abstract "Despite being widely used in the clinical setting for sentinel lymph node detection (SLND), 99mTc-based colloids (e.g., 99mTc-human serum albumin colloids) present a set of properties that are far from ideal. Aiming to design novel compounds with improved biological properties, we describe herein the first class of fully characterized 99mTc(CO)3-mannosylated dextran derivatives with adequate features for SLND. Dextran derivatives, containing the same number of pendant mannose units (13) and a variable number (n) of tridentate chelators (9, n = 1; 10, n = 4, 11, n= 12), have been synthesized and fully characterized. Radiolabeled polymers of the type fac-[99mTc(CO)3(k3-L)] (12, L = 9, 13, L = 10, 14, L = 11) have been obtained quantitatively in high radiochemical purity (≥98%) upon reaction of the dextran derivatives with fac-[99mTc(CO)3(H2O)3]+. The highly stable compounds 13 and 14 were identified by comparing their HPLC chromatograms with the ones obtained for the corresponding rhenium surrogates fac-[Re(CO)3(k3-10)] (13a) and fac-[Re(CO)3(k3-11)] (14a), which have been characterized both at the chemical (NMR and IR spectroscopy, and HPLC) and physical level (DLS, AFM and LDV). Compounds 13a and 14a present a positive zeta potential (+ 7.1 mV, pH 7.4) and a hydrodynamic diameter in the range 8.4−8.7 nm. Scintigraphic imaging and biodistribution studies in Wistar rats have shown good accumulation in the sentinel node at 60 min postinjection (6.71 ± 2.35%, 13; and 7.53 ± 0.69%, 14), with significant retention up to 180 min. A clear delineation of the sentinel lymph node without significant washout to other regions was observed in the scintigraphic images. The popliteal extraction of 94.47 ± 2.45% for 14 at 1 h postinjection, as compared to 61.81 ± 2.4% for 13, indicated that 14 is a very promising compound to be further explored as SLN imaging agent." @default.
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• W2329623800 date "2011-02-23" @default.
• W2329623800 modified "2023-09-24" @default.
• W2329623800 title "Mannosylated Dextran Derivatives Labeled with <i>fac</i>-[M(CO)₃]⁺ (M = ^99mTc, Re) for Specific Targeting of Sentinel Lymph Node" @default.
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• W2329623800 doi "https://doi.org/10.1021/mp100425p" @default.
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