A novel technique for the preparation of (125)I-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabino-furanosyl) uracil [correction of urail] and its biodistribution pattern in Kunming mice.
In this study, a novel technique for the preparation of (125)I-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) urail (FIAU) was developed, (125)I-FIAU biodistribution profile was detected in Kunming mice and the possibility of using FTAU radio-labeling for reporter gene imaging was explored. 5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) urail (FTAU) was labeled with radioiodine ((125)I). A rotary evaporation method was used to remove excess methanol. The reactant was purified through a Sep-Pak C18 reversal phase column. The radiochemical purity and in vivo stability were determined using silica gel thin layer chromatography (TLC). The biodistribution of (125)I-FIAU in Kunming mice was also detected. The results showed that (125)I-FIAU could be radiolabeled effectively with FTAU, with mean labeling rate being (81±0.38)% (n =5). The mean radiochemical purity of (98.01±0.40)% (n=5) was achieved after a reversal phase Sep-park column purification. (125)I-FIAU was stable when incubated in normal human serum or in saline at 37°C, with a radiochemical purity >96% during a 0.5-24 h time period. Biological experiments exhibited rapid clearance of (125)I-FIAU from the blood pool. (125)I-FIAU was mostly excreted by kidneys. (125)I-FIAU in myocardium dropped conspicuously after 8 h and there was hardly retention at 24 h. We were led to concluded that the new method of radioiodinization of FTAU for the preparation of (125)I-FIAU is easy, highly effective and stable in vivo. The biodistribution of (125)I-FIAU in Kunming mice showed it can serve as an imaging probe for myocardial reporter genes.
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Jia
J
Hu
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Yongxue
Y
Zhang
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Xun
X
Sun
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Duolan
D
Li
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Chongjiao
C
Li
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China.
Chunxia
C
Qin
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China. caoweii@gmail.com.
Wei
W
Cao
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Hubei Province Key Lab of Molecular Imaging, Wuhan, 430022, China. hzslxl@163.com.
Xiaoli
X
Lan
D000818:Animals; D001086:Arabinofuranosyluracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D017930:Genes, Reporter / Q000235:genetics; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D007553:Isotope Labeling; D051379:Mice; D057054:Molecular Imaging / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014298:Trimethyltin Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics*
C580884:(125)I-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabino-furanosyl)uracil; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D014298:Trimethyltin Compounds; D001086:Arabinofuranosyluracil