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基于锝-99m的小分子放射性药物和针对炎症与感染的放射性示踪剂。

Technetium-99m based small molecule radiopharmaceuticals and radiotracers targeting inflammation and infection.

作者信息

Kniess Torsten, Laube Markus, Wüst Frank, Pietzsch Jens

机构信息

Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, 01328 Dresden, Germany.

出版信息

Dalton Trans. 2017 Oct 31;46(42):14435-14451. doi: 10.1039/c7dt01735a.

DOI:10.1039/c7dt01735a
PMID:28829079
Abstract

In nuclear medicine, the detection of inflamed and infected lesions is of growing interest. Extensive efforts have been made to develop radiopharmaceuticals specific for inflammation or for discriminating sterile inflammation from infection. Tc is the worldwide most widely used radioisotope for SPECT imaging. The scope of this review article is to give an overview on the development of Tc-labelled small molecule radiotracers targeting inflammatory lesions and infections, ranging from their radiopharmacological evaluation to examples of their clinical applications. A systematic overview of Tc-citrate, Tc-antibiotics and antifungal agents as well as Tc-labelled antimicrobial peptides is provided. Additionally, the class of Tc-labelled cyclooxygenase-2 inhibitors is discussed, since cyclooxygenases are known to play a key role in inflammatory diseases and also in malignant neoplastic diseases. In a short perspective, newer developments in the field of inflammation imaging covering Tc-labelled bacteriophages and chemotactic peptides are highlighted.

摘要

在核医学中,对炎症和感染性病变的检测越来越受到关注。人们已经做出了广泛的努力来开发针对炎症或区分无菌性炎症与感染的放射性药物。锝是全球用于单光子发射计算机断层扫描(SPECT)成像最广泛的放射性同位素。这篇综述文章的范围是概述锝标记的小分子放射性示踪剂在靶向炎症性病变和感染方面的发展,从它们的放射药理学评估到临床应用实例。本文提供了锝 - 柠檬酸盐、锝 - 抗生素和抗真菌剂以及锝标记的抗菌肽的系统概述。此外,还讨论了锝标记的环氧化酶 - 2抑制剂类别,因为已知环氧化酶在炎症性疾病以及恶性肿瘤疾病中都起着关键作用。从简短的视角来看,还强调了炎症成像领域中涵盖锝标记噬菌体和趋化肽的新进展。

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