新型双功能螯合剂DOTA及其衍生物在金属核素标记中的应用进展

Application of new bifunctional chelator DOTA and its derivatives in the metal radionuclide labeled compounds

DOTA及其衍生物是应用最为广泛的新型双功能螯合剂之一。DOTA及其衍生物不仅具有成熟的合成工艺路线，还具有良好的配位和螯合能力，DOTA-多肽分子探针作为MRI对比剂、核素靶向显像剂和放射性药物在生物医学领域被广泛应用。笔者对DOTA双功能螯合剂的种类、DOTA-多肽标记前体的合成和DOTA一多肽金属配合物的应用进行综述。

DOTA and its derivatives are most widely used novel bifunctional chelators. They have not only mature synthesis route, but also good coordination and chelating ability. Therefore, DOTA metal complexes of DOTA-peptide conjugates are increasingly used as MRI contrast agents, radionuclide targeted imaging agents and therapeutic radiopharmaceuticals in the biomedical field. This review covers the bifunctional derivatives of DOTA, the synthesis of DOTA-peptide conjugates, and the applications of DOTA-pep-tide conjugate metal complexes.