正电子心肌灌注显像剂的临床应用及研究进展

Research Progress and Clinical Application of Cardiac Positron Emission Tomography Perfusion Tracers

  • 摘要: 随着正电子发射型断层显像仪(PET)及PET/CT在国内外的逐步推广应用,正电子心肌灌注显像剂的研究也备受关注,PET应用的心肌灌注显像剂有82Rb、13NH3和H215O,但半衰期均较短(t1/2<10 min),或需要82Sr/82Rb发生器或加速器等原因限制其应用。近来长半衰期核素18F标记的新型灌注类显像剂成为研究热点,报道较多的一类显像剂是以心肌细胞线粒体复合物-I(MC-I)为靶点,该类显像在动物体内外试验中均表现出良好的显像性能:心肌摄取快,血流灌注相关性好,滞留时间长。其中又以18F-BMS747158-02最为突出,除具备上述特性外,还体现出心室放射性摄取均匀,体内生物分布理想的特点,有望成为较理想的正电子心肌灌注显像剂。

     

    Abstract: Since the worldwide popularization of positron emission tomography (PET) and PET/CT,myocardial perfusion PET tracers have been gathering more and more attention. Currently, three tracers are used for the assessment of myocardial perfusion with cardiac PET: 82Rb, 13NH3 and H215O. However, their usage is limited by a short physical half-life (t1/2<10 min),and requires onsite generator or cyclotron. Therefore, new myocardial perfusion PET tracers labeled with 18F are becoming a hot research topic due to its sufficient half-life. Presently, several 18F labelled compounds designed to target mitochondrial complex I (MC-I) have been reported in myocardial perfusion assessing. Most of them showed great myocardial extraction, good linearity of uptake versus flow, and excellent retention in the myocardium for the desired imaging window in vitro and vivo. Among them, 18F-BMS747158-02 was the most promising one with rapid kinetics, uniform myocardial distribution, and favorable organ biodistribution. It has the potential of becoming an ideal tracer for cardiac positron emission tomographic imaging.

     

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