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Synthetic copolymer kit for radionuclide blood-pool imaging

Journal Article · · Journal of Nuclear Medicine
OSTI ID:114872
; ;  [1]
  1. Massachusetts General Hospital, Boston, MA (United States); and others

A synthetic blood pool imaging agent labeled with {sup 99m}Tc is reported. The agent, methoxypolyethylene glycolpoly-L-Iysyl-diethylenetriaminepentaacetate monoamide was synthesized from a covalent graft copolymer of methoxypolyethylene glycol succinate (molecular weight 5.1 kD) with subsequent modification of the product with diethylenetriamineacetyl residues. The polymer was formulated into a kit that contained Sn(II) and sodium acetate for radiolabeling with {sup 99m}Tc. Biodistribution studies were performed in rats. Blood-pool imaging and blood clearance determination was carried out in rabbits and in a rhesus monkey. The {sup 99m}Tc-labeled agent [specific activity greater than 3.7 GBq/mg; radiochemical purity more than 98% by thin-layer and high-performance liquid chromatography (HPLC)] demonstrated remarkable stability in solution (pH 5.5-6.5) with no radioactive products of degradation detectable by HPLC even at 24 hr postlabeling. The agent exhibited prolonged circulation in the blood with a half-life of 31.5 hr in rabbits. Bio-distribution in rats showed a lack of substantial accumulation of the agent in the reticuloendothelial system. Sequential acquisitions were performed in a rhesus monkey. The {sup 99m}Tc-labeled polymer kit was compared with the {sup 99m}Tc-red blood cells (RBCs) labeled in vitro. Both methods produced similar heart-to-lung ratios. The ratios remained essentially unchanged for up to 15 hr postinjection. The {sup 99m}Tc-labeled methaxypolyethylene glycol-poly-L-lysyl-diethylenetriamine pentaacetate monoamide is an attractive alternative to radiolabeled RBCs for blood pool imaging applications. 33 refs., 7 figs.

OSTI ID:
114872
Journal Information:
Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: 11 Vol. 35; ISSN JNMEAQ; ISSN 0161-5505
Country of Publication:
United States
Language:
English

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