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Magnetic resonance imaging (MRI) is a noninvasive medical imaging technique based on a phenomenon of nuclear physics discovered in the 1930s, in which matter exposed to magnetic fields and radio waves was found to emit radio signals. In 1970, a physician and researcher named Raymond Damadian noticed that malignant (cancerous) tissue gave off different signals than normal body tissue. He applied for a patent for the first MRI scanning device in clinical use by the early 1980s. The early MRI...
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自组装基高放松性向MRI对比剂 自组装基高放松性向MRI对比剂

Andrew M O'Brien1, Griffin C Pileski1, Matthew P Henry1

  • 1School of Chemistry and Materials Science, Rochester Institute of Technology, Rochester, NY-14623.

ChemMedChem
|June 3, 2024
PubMed
概括

具有Gd-DOTA的自组合基MRI对比剂通过Fmoc-基相互作用显著增强放松性 (r1). 这种自组装策略为开发有针对性,高放松度的药物来改进MRI提供了一种多功能方法.

关键词:
这就是为什么MRI是MRI.癌症 癌症 癌症 癌症 癌症这是一种类.自动组装的自动组装机定位目标 定位目标 定位目标

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科学领域:

  • 生物医学工程 生物医学工程
  • 材料科学 材料科学 材料科学
  • 放射化学 放射化学是指辐射化学.

背景情况:

  • 磁共振成像 (MRI) 的对比剂通过改变水质子的放松时间来提高图像质量.
  • 加多-DOTA (Gd-DOTA) 酸盐是常见的MRI对比剂,但它们的放松性可能是有限的.
  • 基于的药物的自我组装提供了一种扩大放松性的策略.

研究的目的:

  • 为了研究自我组装对基于的MRI对比剂的放松性 (r1) 的影响.
  • 探索序列,离子强度和生物介质对药剂性能的影响.
  • 使用自组装方法开发有针对性的高放松度MRI对比剂.

主要方法:

  • 合成各种包含Fmoc和Gd-DOTA的二和三.
  • 在不同条件下 (离子强度,缓冲区,血清) 评估放松度 (r1) 和临界聚合度 (CAC).
  • 通过将PSMA结合连体 (DCL) 与基架结合,设计和合成向剂.

主要成果:

  • 含有的Fmoc-三的自我组装显著增加了r1值,从3.5-7.4增加到13.2-16.9mM-1s-1每Gd.
  • 发现临界聚合度 (CACs) 取决于度,在缓冲剂中为0.22-2.59mM,在胎儿牛血清 (FBS) 中为<25μM.
  • 向药物表现出高的r1值 (13.5-14.8mM-1s-1在缓冲区,11.2-11.9mM-1s-1在FBS) 与低的CAC在FBS.

结论:

  • 自组装是一种有效的策略,可以显著提高基于Gd-DOTA的MRI对比剂的放松性.
  • 开发的基于的药物在FBS.等生物相关介质中保持高放松性和低CAC.
  • 这项工作提供了一个广泛适用的途径,通过后期结合来创建有针对性的,高放松度的MRI对比剂.