title: Synthesis and evaluation of (99m)Tc-2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose as a potential tumor imaging agent.
abstract: The 2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose (CPADG) was synthesized and radiolabeled with (99m)TcO4(-) to obtain the (99m)Tc-CPADG complex in high yield. It was stable over 6 h in saline at room temperature and in serum at 37 °C. The partition coefficient and electrophoresis results indicated that the complex was hydrophilic and cationic. In vitro cell studies showed there was an increase in the uptake of (99m)Tc-CPADG as a function of incubation time and (99m)Tc-CPADG was possibly transported via the glucose transporters. The biodistribution of (99m)Tc-CPADG in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 1.91 and 5.05 at 4h post-injection. Single photon emission computed tomography (SPECT) image studies showed there was an obvious accumulation in tumor sites, suggesting (99m)Tc-CPADG would be a promising candidate for tumor imaging.
authors.affiliation: Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Zhu
authors.affiliation: Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Song
authors.affiliation: Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Xuebin
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Nuclear Medicine, Beijing Friendship Hospital of Capital Medical University, Beijing, China.
authors.forename: Jigang
authors.initials: J
authors.lastname: Yang
authors.affiliation: Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China. Electronic address: zhjunbo@bnu.edu.cn.
authors.forename: Junbo
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000818:Animals; D005947:Glucose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D015394:Molecular Structure; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics; D012510:Sarcoma 180 / Q000175:diagnosis*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: C000595762:(99m)Tc-2-((3-carboxy-1-oxopropyl)amino)-2-deoxy-D-glucose; D015609:Organotechnetium Compounds; D005947:Glucose
keywords: Glucose; Imaging; SPECT; Technetium-99m; Tumor