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Synthesis, characterization and biodistribution of a 99m Tc nitrido complex as a potential brain perfusion imaging agent
Author(s) -
Zhang Junbo,
Wang Xuebin,
Lu Gongxu,
Tang Zhigang
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/1099-1344(200006)43:7<693::aid-jlcr354>3.0.co;2-7
Subject(s) - chemistry , biodistribution , dithiocarbamate , ligand (biochemistry) , partition coefficient , technetium , lipophilicity , imaging agent , radiochemistry , chloride , thin layer chromatography , nuclear chemistry , chromatography , stereochemistry , organic chemistry , receptor , in vivo , biochemistry , in vitro , microbiology and biotechnology , biology
The bis(N‐cyclohexyl‐dithiocarbamato) nitrido technetium‐99m complex [ 99m TcN‐(CHDTC) 2 ] (CHDTC:N‐cyclohexyl dithiocarbamato) has been synthesized through a ligand‐exchange reaction. The two‐step procedure involved the initial reaction of 99m TcO − 4 with succinic dihydrazide (SDH) in the presence of stannous chloride as reducing agent and propylenediamine tetraacetic acid (PDTA) as complexant, followed by the addition of sodium N‐cyclohexyl dithiocarbamate dihydrate. The radiochemical purity of the complex was over 90% by thin layer chromatography. It was stable over 6 h at room temperature. Its partition coefficient indicated that it was a good lipophilic complex. Biodistribution in mice demonstrated that the complex accumulated in brain with high uptake and good retention. The brain uptake (ID%/g) was 2.91, 5.88 and 5.91 at 5,30 and 60 min post‐injection respectively. The ratio of brain/blood in mice was high, 2.10 at 1 h post‐injection. The results for the complex suggested that it could be a potential brain perfusion imaging agent. Copyright © 2000 John Wiley & Sons, Ltd.