Synthesis and biological evaluation of (99m)Tc-DMP-NGA as a novel hepatic asialoglycoprotein receptor imaging agent.
A novel bifunctional coupling agents-biomolecular compound DMP-NGA was prepared by coupling the SATP with galactosyl-neoglycoalbumin (NGA). The DMP-NGA was labeled with technetium-99m, and the radiochemical purity in excess of 98% after purified with HPLC. In vivo biodistribution showed that (99m)Tc-DMP-NGA had very high initial liver uptake with good retention. The liver accumulated 99.35+/-9.77%, 74.25+/-3.03%, 52.47+/-7.58% of the injected dose per gram at 5, 30 and 120min after injection, respectively. It had relative higher initial liver uptake and much lower blood uptake than that of (99m)Tc-GSA. The liver/blood ratio reached 83.4 at 30min post-injection, while the ratio of liver/kidney was 14.4. The uptakes in other organs in the abdomen were also slightly low. In addition, the hepatic uptake of (99m)Tc-DMP-NGA was blocked by preinjecting free GSA as blocking agent. The result indicates that (99m)Tc-DMP-NGA has specific binding to ASGP receptor. Images acquired with Kodak In-Vivo Imaging System FX Pro showed significant difference before and after inhibition. The promising biological properties of (99m)Tc-DMP-NGA afford potential applications in liver receptor imaging for assessment of hepatocyte function.
Yang
Wenjiang
W
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Mou
Tiantian
T
Zhang
Xianzhong
X
Wang
Xuebin
X
D000418:Albumins / Q000138:chemical synthesis*; D000818:Animals; D037263:Asialoglycoprotein Receptor / Q000032:analysis*; D008099:Liver / Q000378:metabolism*; D051379:Mice; D015609:Organotechnetium Compounds / Q000097:blood / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000378:metabolism; D014018:Tissue Distribution
D000418:Albumins; D037263:Asialoglycoprotein Receptor; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C546840:technetium 99m dimercaptopropionyl-neogalactosylalbumin