Synthesis of Small Peptides and Their Use as Bifunctional Chelating Agents in Diagnostic Radiopharmaceuticals

✍ Scribed by Chongzhi TANG; Longjin LI; Zhen PANG; Zhibin YUAN

• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: English
• Weight: 295 KB
• Volume: 27
• Category: Article
• ISSN: 0256-7660
• DOI: 10.1002/cjoc.200990018

✦ Synopsis

Abstract

Three linear mercaptoacetyl tetrapeptides, MAG3‐Leu‐OH, MAG3‐Phe‐OH and MAG3‐Tyr‐OH, were synthesized via a liquid phase synthetic approach with high yields and high purities without using preparative HPLC technique. The obtained products could be radiolabeled easily with ^99m^Tc under a mild condition and showed high stability in vitro and in vivo conditions. The scintigrams of the tested rabbit after injection of the radiolabeled products via mainline showed a normal biodistribution, which is definitely different from that of ^99m^Tc‐MAG3, indicating different routes of metabolization between these two radiochemicals.