使用18F-“点击”化学法对αvβ6特异性肽进行放射性标记的体内正电子发射断层扫描（PET）成像：与相应的4-[18F]氟苯甲酰基肽和2-[18F]氟丙酰基肽的评估与比较。
In vivo positron emission tomography (PET) imaging with an alphavbeta6 specific peptide radiolabeled using 18F-"click" chemistry: evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F]fluoropropionyl-peptides.
作者信息
Hausner Sven H, Marik Jan, Gagnon M Karen J, Sutcliffe Julie L
机构信息
Department of Biomedical Engineering, University of California Davis, Davis, California 95616, USA.
出版信息
J Med Chem. 2008 Oct 9;51(19):5901-4. doi: 10.1021/jm800608s. Epub 2008 Sep 12.
Abstract
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [(18)F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase (18)F-"click" radiolabeling and solid-phase radiolabeling using 4-[(18)F]fluorobenzoic and 2-[(18)F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
摘要
许多放射性标记的肽已被用于多种细胞表面受体的体内成像。对于使用[（18）F]氟的PET应用，肽通过辅基方法进行放射性标记。我们之前开发了使用4- [（18）F]氟苯甲酸和2- [（18）F]氟丙酸的溶液相（18）F-“点击”放射性标记和固相放射性标记。在这里，我们比较了三种不同的放射性标记方法，并报告了对PET成像和药代动力学的影响。辅基确实有影响；观察到具有明显不同极性的代谢物。
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