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Synthesis of Small Peptides and Their Use as Bifunctional Chelating Agents in Diagnostic Radiopharmaceuticals
Author(s) -
TANG Chongzhi,
LI Longjin,
PANG Zhen,
YUAN Zhibin
Publication year - 2009
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.200990018
Subject(s) - chemistry , biodistribution , bifunctional , in vivo , in vitro , high performance liquid chromatography , combinatorial chemistry , chelation , chromatography , radiochemistry , stereochemistry , organic chemistry , biochemistry , microbiology and biotechnology , biology , catalysis
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.