[en] Radiolabeling of biologically active molecules with fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺ unit has been of primary interest in recent years. Therefore, we herein report ligands L¹-L⁴ (L¹=histidine, L²=nitrilotriacetic acid, L³=2-picolylamine-N,N-diacetic acid, L⁴=bis(2-pyridymethy)amine) that have been evaluated by radiochemical reactions with fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺. These reactions yielded the radioactive complexes of fac-[¹⁸⁸Re(CO)₃L] (L = L¹-L⁴, ¹⁸⁸Re tricarbonyl complexes 1-4), which were identified by HPLC. Complexes 1-4, with log P_o/w values ranging from -2.23 to 2.18, were obtained with yields of ≥95% using ligand concentrations within 10^-6-10^-4M range. Thus, specific activities of 220 GBq/μmol could be achieved. Challenge studies with cysteine and histidine revealed high stability for all of these radioactive complexes, and biodistribution studies in mice indicated a fast rate of blood clearance and high rate of total radioactivity excretion occurring primarily through the renal-urinary pathway. In summary, the ligands L¹-L⁴ are potent chelators for the future functionalization of biomolecules labeling with fac-[¹⁸⁸Re(CO)₃(H₂O)₃]⁺. (author)

[en] The aim of this study was to develop a radiopharmaceutical for the imaging of CXCR4-expressing tumors in vivo. For ¹²⁵I-labeling, ¹²⁵I-SIB was synthesized and conjugated with the ε-NH₂ group of Ac-TZ14011, a specific CXCR4 antagonist. The specific radioactivity of the product was 5 GBq/μmol and the radiochemical purity (RCP) was 96% (n = 3). After 6 h, the RCP of the product in PBS was 93%. The MCF-7 cell uptake of Ac-TZ14011 was rapid and high. Primary biodistribution studies indicated that ¹²⁵I-IB-Ac-TZ14011 was mainly excreted via the kidney, and further evaluation in mice with induced tumors was necessary. (author)