PROSTHETIC GROUPS FOR RADIOLABELING OF FUNCTIONALIZED DRUGS AND PEPTIDES

放射性同位素标记用于诊断的有机化合物的用途 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在大脑，心脏，或 在其他靶器官或组织中达到足够的水平， 其成像。 人们对寻找化合物的兴趣越来越大 它将更有效地穿过血脑屏障， 促进对大脑的更有效成像。 某些药物在动物或器官中的结合位点可以定位为 合成高比活度放射性标记类似物的结果 其对该结合位点具有高亲和力。 假体组可能是 连接到药物或其他受体配体上，用于有效的 和选择性化学捕获特定的放射性同位素。 具有 开发了茶碱和其他药物的功能化同系物， 在腺苷受体，我们现在正在开发辅基， 放射性同位素如18F、123 I和125 I，以与这些化合物偶联。 功能化药物分子。 辅基含有氨基或 待共价缩合至官能化的羧基， 在特定受体上产生高亲和力缀合物的药物，或 不可逆地结合标签的药物（三功能试剂）。 正电子 发射断层扫描（PET）已被用于对大脑中的受体进行成像 和其他器官。 用于化学捕获18F的辅基需要 快速有效的反应和纯化;由于半衰期仅为 110分钟 我们正在利用这种方法来成像胰岛素受体， vivo.

The use of radioistopes to label organic compounds for use in diagnostic nuclear medicine as 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, or drugs that bind the label irreversibly (trifunctional reagents). 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. We are utilizing this approach to image insulin receptors in vivo.