用于正电子发射断层扫描（PET）的基质金属蛋白酶（MMP）抑制剂CGS 27023A的新型18F标记衍生物：放射性合成及初步小动物PET研究
A new 18F-labelled derivative of the MMP inhibitor CGS 27023A for PET: radiosynthesis and initial small-animal PET studies.
作者信息
Wagner Stefan, Breyholz Hans-Jörg, Höltke Carsten, Faust Andreas, Schober Otmar, Schäfers Michael, Kopka Klaus
机构信息
Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Str. 33, D-48149 Münster, Germany.
出版信息
Appl Radiat Isot. 2009 Apr;67(4):606-10. doi: 10.1016/j.apradiso.2008.12.009. Epub 2008 Dec 24.
The CGS 27023A derivative (R)-2-(N-((6-fluoropyridin-3-yl)methyl)-4-methoxyphenyl-sulphonamido)-N-hydroxy-3-methylbutanamide 1a was identified as a very potent matrix metalloproteinase inhibitor. Here, we describe a one-step radiosynthesis of the target compound [(18)F]1a. The syntheses of [(18)F]1a resulted in a radiochemical yield of 12.1+/-5.9% (decay-corrected), a radiochemical purity of 98.8+/-0.6%, and a specific activity of 39+/-27 GBq/micromol at the end of synthesis within 160+/-18 min from the end of radionuclide production (n=5). Initial small-animal PET studies in wild-type mice (C57/BL6) showed no unfavourable tissue accumulation of [(18)F]1a.
CGS 27023A的衍生物（R）-2-（N-（（6-氟吡啶-3-基）甲基）-4-甲氧基苯基磺酰胺基）-N-羟基-3-甲基丁酰胺1a被鉴定为一种非常有效的基质金属蛋白酶抑制剂。在此，我们描述了目标化合物[(18)F]1a的一步放射性合成。[(18)F]1a的合成放射化学产率为12.1±5.9%（衰变校正），放射化学纯度为98.8±0.6%，在放射性核素生产结束后160±18分钟内合成结束时比活度为39±27 GBq/μmol（n=5）。在野生型小鼠（C57/BL6）中进行的初步小动物PET研究表明，[(18)F]1a在组织中没有不良蓄积。
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