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Preparation and biological evaluation of 99m TcN‐labeled pteroyl‐lys derivative as a potential folate receptor imaging agent
Author(s) -
Chen Yuan,
Guo Hongjuan,
Xie Fang,
Lu Jie
Publication year - 2014
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/jlcr.3116
Subject(s) - biodistribution , chemistry , folate receptor , in vivo , in vitro , imaging agent , dithiocarbamate , derivative (finance) , radiochemistry , biochemistry , medicine , microbiology and biotechnology , organic chemistry , cancer , cancer cell , economics , financial economics , biology
In order to develop a novel 99m Tc‐labeled folate receptor (FR) imaging agent, a dithiocarbamate derivative, pteroyl‐lys‐DTC, was synthesized and radiolabeled with 99m Tc through the [ 99m TcN] 2+ intermediate. The radiochemical purity of the corresponding 99m Tc‐complex, 99m TcN‐pteroyl‐lys‐DTC, was over 95% as measured by reversed‐phase HPLC. The 99m TcN complex was stable under physiological conditions. 99m TcN‐pteroyl‐lys‐DTC exhibited specific FR binding in FR‐positive KB cells in vitro . The biodistribution in tumor‐bearing mice showed that the 99m TcN‐labeled radiotracer had good uptake (3.56 ± 0.09%ID/g at 2 h postinjection) in FR‐positive KB tumors, as well as in the kidneys (30.34 ± 3.53%ID/g at 2 h postinjection). After coinjection with excess folic acid, the uptake in tumor and kidneys was significantly blocked. The results indicated that 99m TcN‐pteroyl‐lys‐DTC was able to target the FR‐positive tumor cells and tissues specifically both in vitro and in vivo . Copyright © 2013 John Wiley & Sons, Ltd.