PROSTHETIC GROUPS FOR RADIOLABELING OF FUNCTIONALIZED DRUGS AND PEPTIDES

用于功能化药物和肽的放射性标记的辅基

• 批准号: 3917487
• 负责人: J JACOBSON
• 金额: --
• 依托单位: NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3917487
• 关键词: adenosine; blood brain barrier; chemical binding; chemical conjugate; drug delivery systems; drug design /synthesis /production; drug receptors; neurotransmitter receptor; positron emission tomography; stable isotope diagnosis; synthetic peptide; theophylline

The use of radioisotopes to label organic compounds for use in diagnostic nuclear medicine is well documented in the literature. It has been found that certain radiolabeled compounds will localize in the brain, heart, or in other target organs or tissues to a sufficient level to allow for imaging thereof. There has been increasing interest in finding compounds which will more effectively cross the blood-brain barrier, thus facilitating more efficacious imaging of the brain. Binding sites for certain drugs in an animal or organ may be localized as a result of the synthesis of high specific activity radiolabeled analogs which have high affinity for that binding site. Prosthetic groups may be attached to a drug or other receptor ligand for the purpose of efficient and selective chemical capture of a particular radioisotope. Having developed functionalized congeners of theophylline and other drugs acting at adenosine receptors, we are now developing prosthetic groups for radioisotopes such as 18F, 123I, and 125I, to be coupled to these functionalized drug molecules. The prosthetic groups contain amino or carboxylic groups which are to be condensed covalently to functionalized drugs to give conjugates of high affinity at a particular receptor. Positron emission tomography (PET) has been used for imaging receptors in the brain and other organs. A prosthetic group for chemical capture of 18F requires rapid and efficient reaction and purification, since the half-life is only 110 minutes.

使用放射性同位素标记有机化合物，用于 诊断核医学在文献中有很好的记载。 已经发现，某些放射性标记的化合物将 定位于大脑、心脏或其他靶器官或组织中 到足以允许其成像的水平。 一直 越来越多的人对寻找化合物感兴趣， 有效地穿过血脑屏障，从而促进更多 大脑的有效成像。 某些药物在动物或器官中的结合位点可能是 由于高比活性的合成而定位 对结合具有高亲和力放射性标记的类似物 绝佳的价钱 假体基团可以连接到药物或其他载体上。 受体配体，用于高效和选择性化学 捕获特定的放射性同位素。 在制定 茶碱和其他作用于 在腺苷受体上，我们现在正在开发辅基， 对于放射性同位素如18F、123I和125I， 这些功能化的药物分子。 辅基含有 氨基或羧基，其共价缩合到 功能化药物，得到高亲和力的缀合物， 特殊受体 正电子发射断层扫描（PET）已用于成像 大脑和其他器官中的受体。 一个假体组， 18F的化学捕获需要快速和有效的反应， 纯化，因为半衰期只有110分钟。