PROSTHETIC GROUPS FOR RADIOLABELING OF FUNCTIONALIZED DRUGS AND PEPTIDES

使用放射性同位素标记用于诊断的有机化合物 核医学在文献中有很好的记录。它已经找到了 某些放射性标记化合物会定位在大脑、心脏或 在其他靶器官或组织中达到足够的水平以允许 对其进行成像。人们对寻找化合物越来越感兴趣。 它会更有效地穿过血脑屏障，从而 有助于更有效地对大脑进行成像。 某些药物在动物或器官中的结合部位可定位为 高比活度放射性标记类似物的合成结果 它们对该结合部位具有高亲和力。假肢团体可能是 依附于药物或其他受体配基以达到有效的目的 以及对特定放射性同位素的选择性化学捕获。拥有 开发茶碱和其他作用药物的官能化同系物 在腺苷受体方面，我们现在正在为 放射性同位素，如18F、123I和125I，与这些 功能化的药物分子。假体基团含有氨基或 需要共价缩合到官能化的羧基 在特定受体上给出高亲和力的结合物的药物。 正电子发射断层扫描(PET)已被用于对受体进行成像 大脑和其他器官。一种化学捕获18F的假体基团 需要快速高效的反应和提纯；因为半衰期 只有110分钟。

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.