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 某些放射性标记的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能是定位的 作为合成高比活度放射性标记的结果 对该结合部位具有高亲和力的类似物。假肢 基团可以连接到药物或其他受体配体上以达到此目的 对特定放射性同位素的有效和选择性的化学捕获。 开发了茶碱和其他药物的功能化同系物 通过作用于腺苷受体，我们现在正在开发假体群 对于放射性同位素，如18-F、123-I和125-I，要耦合到这些 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 在特定受体上给予高亲和力的结合物的药物，或 不可逆地结合标签的药物(三功能试剂)。我们有 开发了一种含有叠氮基的放射性碘化衍生物，用于 与A2-腺苷受体的共价反应。

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 18-F, 123-I, and 125-I, 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). We have developed a radioiodinated derivative that contains an azido group for covalent reaction with A2-adenosine receptors.