title: Synthesis, characterization and biodistribution of new fatty acids conjugates bearing N,N,N-donors incorporated [99mTc/Re(CO)3]+.
abstract: [(99m)Tc(CO)(3)](+)-6-[N-(2-dipicolyl)amino]hexanoic acid (1a) and [(99m)Tc(CO)(3)](+)-11-[N-(2-dipicolyl)amino]undecanoic acid (1b) were prepared by incorporating [(99m)Tc-(CO)(3)](+) into 6-[N-(2-dipicolyl)amino]hexanoic acid and 11-[N-(2-dipicolyl)amino]undecanoic acid, respectively. The overall radiochemical yield of 1a and 1b was from 79.7% to 91.3% and radiochemical purity after HPLC purification was more than 94%. The resulting complexes were found to be chemically stable when incubated in SD rat serum for 3 h at 37 °C. Tissue distribution studies in normal mice showed that high initial uptake of Tc-99m complexes were observed, followed by slow clearance from the heart. The maximum heart-to-blood ratio of 1a was 1.46 at 60 min, but 1b showed a poor heart-to-blood ratio. By estimating the tissue distribution and the computing result of the molar volume and the solvation free energy of Tc-99m chelating groups, a small-size and monocationic Tc-99m core is very important to enhance the myocardial accumulation and low liver uptake for the fatty acid tracers.
authors: Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors: Huahui
authors: H
authors: Zeng
authors: Lingzhou
authors: L
authors: Zhao
authors: Shiyuan
authors: S
authors: Hu
authors: Yongjuan
authors: Y
authors: Liu
authors: Haijing
authors: H
authors: Yu
authors: Na
authors: N
authors: Chen
authors: Huabei
authors: H
authors: Zhang
mesh_terms: D000818:Animals; D002248:Carbon Monoxide / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D012211:Rhenium / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: D005227:Fatty Acids; D015609:Organotechnetium Compounds; D012211:Rhenium; D002248:Carbon Monoxide