PDF(Pubmed)
Abstract：
Positron emission tomography (PET) is a noninvasive molecular imaging method extensively applied in the detection and treatment of various diseases. Hypoxia is a common phenomenon found in most solid tumors. Nitroimidazole is a group of bioreducible pharmacophores that selectively accumulate in hypoxic regions of the body. Over the past few decades, many scientists have reported the use of radiopharmaceuticals containing nitroimidazole for the detection of hypoxic tumors. Gallium-68, a positron-emitting radioisotope, has a favorable half-life time of 68 min and can be conveniently produced by 68Ge/68Ga generators. Recently, there has been significant progress in the preparation of novel 68Ga-labeled complexes bearing nitroimidazole moieties for the diagnosis of hypoxia. This review provides a comprehensive overview of the current status of developing 68Ga-labeled radiopharmaceuticals with nitroimidazole moieties, their pharmacokinetics, and in vitro and in vivo studies, as well as PET imaging studies for hypoxic tumors.
摘要：
正电子发射断层扫描（PET）是一种无创的分子成像方法，广泛应用于各种疾病的检测和治疗。缺氧是大多数实体瘤中常见的现象。硝基咪唑是一组可生物还原的药效团,其选择性地积累在身体的缺氧区域中。在过去的几十年里，许多科学家报道了使用含有硝基咪唑的放射性药物来检测缺氧肿瘤。镓-68，一种发射正电子的放射性同位素，具有68min的有利半衰期,并且可以通过68Ge/68Ga发生器方便地生产。最近,在制备带有硝基咪唑部分的新型68Ga标记复合物以诊断缺氧方面取得了重大进展。这篇综述全面概述了具有硝基咪唑部分的68Ga标记的放射性药物的开发现状，他们的药代动力学，以及体外和体内研究，以及缺氧肿瘤的PET成像研究。
