CARBON ENCAPSULATED RADIONUCLIDE CHELATES

因为它们只寻找并结合特定的细胞， 抗体代表了一种选择性携带 放射性核素到癌细胞。 目前用于连接的技术 放射性核素到单克隆抗体依赖于金属离子螯合物。 这些通常缺乏足够的稳定性，并且放射性核素可能是 通过体内化学过程或通过 将放射性同位素封装在一个封闭的碳球中。 这些 新化合物具有非凡的稳定性，应完全 对体内离子交换过程是惰性的。 最近的实验 证明这些复合物可以很容易地承受核爆炸 核工业用放射性镧系金属产生的衰变能 而不释放放射性衰变产物。 初步的全身毒性研究表明， 体内无毒。 第一阶段将集中在合成，纯化， 并验证这些重要特性。 这将是 通过模型有机金属系统的中子活化完成 含有合适的同位素，然后对 中子俘获和随后衰变产生的产物 流程. 第二阶段将侧重于将新化合物连接到 单克隆抗体和表征所得的缀合物 复杂. 建议的商业应用：预计第一阶段 研究表明，这些新的有机金属化合物 具有非凡的抗释放性， 放射性核素，并将上级传统的螯合物， 将放射性核素与单克隆抗体缀合。阶段成功 II将导致一种新型的放射性标记，可以改善 放射免疫导向药物的性能。

Because they seek out and bind only to specific cells, monoclonal antibodies represent a powerful method for selectively carrying radionuclides to cancerous cells. Current techniques for attaching radionuclides to monoclonal antibodies rely on metal ion chelates. These often lack sufficient stability, and the radionuclide may be released by in vivo chemical processes or by the compounds that encapsulate the radioisotope inside a closed sphere of carbon. These new compounds possess extraordinary stability and should be completely inert to in vivo ion exchange processes. Recent experiments demonstrate that these complexes can easily withstand the nuclear decay energy produced by radioactive lanthanide metals used in nuclear medicine without releasing the radioactive decay products. Preliminary systemic toxicity studies show that they are relatively nontoxic in vivo. Phase I will focus on the synthesis, purification, and verification of these important properties. This will be accomplished by neutron activation of a model organometallic system containing a suitable isotope followed by complete characterization of the products produced by the neutron capture and subsequent decay processes. Phase II will focus on attaching the new compound to a monoclonal antibody and on characterizing the resulting conjugated complex. PROPOSED COMMERCIAL APPLICATION: It is expected that the Phase I research will demonstrate that these new organometallic compounds possess extraordinary resistance against release of the encapsulated radionuclide and will be superior to conventional chelates for conjugating radionuclides to monoclonal antibodies. Success in Phase II will result in a new type of radiolabel that can improve the performance of radioimmunoguided pharmaceuticals.