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首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of I-123-labeled pyridyl benzoxazole derivatives: novel beta-amyloid imaging probes for single-photon emission computed tomography
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Synthesis and biological evaluation of I-123-labeled pyridyl benzoxazole derivatives: novel beta-amyloid imaging probes for single-photon emission computed tomography

机译：I-123标记的吡啶基苯并恶唑衍生物的合成和生物学评估：用于单光子发射计算机断层扫描的新型β-淀粉样蛋白成像探针

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In vivo imaging of beta-amyloid (A beta) plaques by non-invasive techniques such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT) may facilitate early diagnosis and drug discovery for the treatment of Alzheimer's disease (AD). SPECT is known as a more useful modality than PET in terms of routine diagnostic use, but there have been no reports on attractive probes in clinical studies. In this study, we synthesized and evaluated novel I-123-labeled pyridyl benzoxazole (PBOX) derivatives as SPECT probes for imaging A beta plaques in vivo. The PBOX derivatives showed affinity for A beta( 1-42) aggregates in vitro (K-i = 6.9-138 nM). In biodistibution experiments in normal mice, all these derivatives showed high initial uptake into (4.6-6.6% ID g(-1) at 2 min) and rapid clearance (0.3-1.3% ID g(-1) at 60 min) from the brain. Furthermore, [I-125]9 clearly labeled A beta plaques in in vitro autoradiography of postmortem AD brain sections. SPECT/CT study with [I-123]9 displayed higher radioactivity in Tg2576 mice than wild-type mice. In addition, ex vivo autoradiograms of brain sections from Tg2576 mice after the injection of [I-123]9 showed selective binding of Ab plaques. In conclusion, [I-123]9 may be a potential SPECT probe for imaging Ab plaques in AD brain.
机译：通过非侵入性技术（例如正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT））对β-淀粉样蛋白（A beta）斑块进行体内成像可能有助于早期诊断和药物发现，以治疗阿尔茨海默氏病（AD） ）。就常规诊断用途而言，SPECT被认为比PET更有用，但在临床研究中尚无有关引人注目的探针的报道。在这项研究中，我们合成和评估了新型I-123标记的吡啶基苯并恶唑（PBOX）衍生物作为SPECT探针，可在体内对Aβ斑块进行成像。 PBOX衍生物显示出对A beta（1-42）聚集体的亲和力（K-i = 6.9-138 nM）。在正常小鼠的生物分布实验中，所有这些衍生物均显示出较高的初始摄入量（2分钟时为4.6-6.6％ID g（-1））和快速清除（60分钟时为0.3-1.3％ID g（-1））。脑。此外，[I-125] 9在死后AD脑切片的体外放射自显影中清楚地标记了Aβ斑块。用[I-123] 9进行的SPECT / CT研究显示，Tg2576小鼠的放射性高于野生型小鼠。此外，注射[I-123] 9后，来自Tg2576小鼠的脑切片的离体放射自显影显示了抗体斑块的选择性结合。总之，[I-123] 9可能是一种用于在AD脑中成像Ab斑块的潜在SPECT探针。

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