Department of Isotope Application Research, National Atomic Research Institute, Taoyuan City, Taiwan
Research Article
Characterization of New Atherosclerosis Imaging Ligands with Aminomethylpyridinyl-Tetraazacyclododecane Group Using Liquid Chromatography and Tandem Mass Spectrometry
Author(s): Weihsi Chen*, Chienchung Hsia, Siaosyun Guan and Chengliang Peng
Macrophage expression C-X-C motif chemokine receptor 4 (CXCR4) plays important role in inflammation and induces atherosclerosis. Two novel similar small molecular CXCR4 antagonists with aminomethylpyridinyl and macrocyclic tetraazadodecanyl groups, known as APD and APO, were designed and synthesized and then used as radio-imaging agents (after chelating with radio isotope of gallium ion) for atherosclerosis diagnosis using an ApoE-/- mouse model. By PET/CT scanning, the imaging performance of 68Ga-APD on atherosclerotic animal model surpasses over 68Ga-APO. The structures of the complexes of the ligands with gallium, impurities in APD and metabolites of APD in serum were analyzed using High-Performance Liquid Chromatography (HPLC) and tandem mass spectrometry. The HPLC method based on a C-18 column (25 cm × 4.6 mm and 5 µm) and mobile phase.. View more»