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Synthesis of Complexes of N-vinylpyrrolidone–vinylamine or N-vinylpyrrolidone–allylamine Containing Macrocyclic Polyligand 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetate (DOTA) with Gallium-68 Isotope and Estimation of Their in Vivo Distribution

Russian chemical bulletin(2017)

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摘要
A method for radiolabeling the water-soluble N-vinylpyrrolidone copolymers with N-vinyl- and N-allylamine containing bifunctional chelation unit 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetate by the radioactive isotope gallium-68 (68Ga) was developed. Radiotracers were obtained in the yield about 65%. A method of liquid chromatography for the micropreparative isolation of the metal-polymeric complexes with a radiochemical purity of ~98% was developed. The data on the stability of the complexes in blood serum and the results on the biodistribution of the synthesized complexes in organs and tissues of laboratory animals (rats) with transplantable tumor are presented.
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关键词
radiopharmaceuticals,positron emission tomography (PET),radionuclides,gallium-68,copolymers,chelation unit,biodistribution,liquid chromatography
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