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: 3875624
• 负责人: K 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/3875624
• 关键词: adenosine; aminoacid; blood brain barrier; carboxylate; chemical binding; chemical conjugate; drug delivery systems; drug design /synthesis /production; drug receptors; drug vehicle; neurotransmitter receptor; positron emission tomography; radiopharmacology; 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 organi 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 核医学在文献中有详细记载。已经找到了 某些放射性标记化合物将定位于大脑、心脏或 在其他靶器官或组织中达到足够的水平，以允许 其成像。人们对寻找化合物越来越感兴趣 这将更有效地穿过血脑屏障，从而 促进更有效的大脑成像。 动物或器官中某些药物的结合位点可能定位为 高比活性放射性标记类似物的合成结果 其对该结合位点具有高亲和力。假肢组可能是 附着在药物或其他受体配体上以有效 以及特定放射性同位素的选择性化学捕获。拥有 开发了茶碱和其他作用药物的功能化同系物 在腺苷受体方面，我们现在正在开发假体基团 放射性同位素，如 18F、123I 和 125I，与这些物质偶联 功能化药物分子。辅基含有氨基或 共价缩合成官能化的羧基 药物对特定受体产生高亲和力的缀合物。 正电子发射断层扫描 (PET) 已用于对受体进行成像 大脑和其他器官。用于化学捕获 18F 的辅基 需要快速、高效的反应和纯化；自从半衰期以来 只有110分钟。