Synthesis and evaluation of [sup.111]In-labeled D-glucose as a potential SPECT imaging agent

The purpose of this study was to develop an efficient synthetic method for labeling D-Glucosamine with indium-111 ([sup.111]In), and to investigate the imaging properties of the resulting radiotracer in MDA-MB-468 xenograft models using single-photon emission computed tomography (SPECT). The precursor compound, 2-(4-Isothiocyanato benzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-deoxyglucosone (DOTA-DG), was synthesized from 2-D-Glucosamine. DOTA-DG was labeled with [sup.111]In within 20 min. The labeling efficiency and radiochemical purity of [sup.111]In-DOTA-DG were >95 and >96 % as determined by radio-HPLC. SPECT imaging studies were performed using nude mice bearing MDA-MB-468 mammary tumors after intravenous injection of at a dose of 1.11 MBq (0.1 mL)[sup.111]In-DOTA-DG. Tumors were clearly delineated by SPECT imaging at 120 min after injection. Keywords Indium-111 * 2-D-Glucosamine * Tumor * SPECT imaging