TRITIUM LABELING-MECHANISMS AND METHODS

氚标记机制和方法

• 批准号: 3171383
• 负责人: CHIN-TZU PENG
• 金额: $ 10.31万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
• 依托单位国家: 美国
• 财政年份: 1982
• 资助国家: 美国
• 起止时间: 1982-07-01 至 1988-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3171383
• 关键词: chemical synthesis; halogenation; microwave radiation; nuclear magnetic resonance spectroscopy; radiobiology; radiopharmacology; radiotracer

The objective of the proposed ressearch is to study the conditions under which tritium labeled compounds such as unsaturates, polypeptides, proteins, and biomolecules, can be obtained with high specific activity and minimum degradation. The use of energy transfer agents, catalytic surfaces and graded tritium energies to increase the selectivity of tritium labeling by active sp]ecies of tritium will be studied. The short duration of exposure, mild conditions, minimum radiation degradation and high specific activity can be obtained make excitation labeling the method of choice for complex molecules and biomelecules. Adsorbed or chemisorbed tritium on supported metal catalysts will be used for tritium labeling. Adsorbed tritium is the mildest tritium exchange agent and can label compounds with hydrogen sensitive groups without causing their reduction of substitution. The method can be improved to increase the amount of tritium adsorbed or chemisorbed on the catalyst so that curie amount of tritium is available for tritation of biological molecules. The use of surfaces to complex and stabilize the peptide bond and the N- and C-terminal residues in peptide molecules to minimize degradation will be investigated and, particularly, the reactions of protected and non-protected small peptides with tritium to determine how polypeptides such as interferons and insulin can be routinely labeled with high specific activity. The dehalogenation reactions, i.e., T-for-I and T-for-Br reactions are particularly useful for introducing tritium into specific positions in a molecule in the absence of hydrogen transfer catalyst and will be investigated. Dehalogenation in the presence of metal catalyst may result in tritium exchange and is undesirable. Tritium NMR spectroscopy of some of these labeled compounds will be performed by Dr. Yang of Lawrence Berkeley Laboratory.

拟议的Ressearch的目的是研究 哪个标记化合物，例如不饱和，多肽， 蛋白质和生物分子可以以高特异性活性和 最小降解。 使用能量传输剂，催化表面和分级tri剂量 通过主动sp] ecies提高tritium标记的选择性的能量 将研究Tritium。 暴露时间短，温和 条件，最小辐射降解和高比活性可以是 获得了兴奋标记复合物选择方法 分子和生物粒子。 将使用在支撑的金属催化剂上吸附或化学吸附的tribed Tritium 用于Tritium标签。 吸附的tritium是最温和的trip交流 代理和可以用氢敏感组标记化合物，而无需 导致他们减少替代。 该方法可以改进到 增加在催化剂上吸附或化学吸附剂的量 居里的tri量可用于生物学的术 分子。 使用表面复合和稳定肽键和n- 和肽分子中的C末端残基，以最大程度地减少降解 被调查，特别是受保护和 未受保护的小肽，用tritium确定多肽如何 例如干扰素和胰岛素可以用高特异性标记 活动。 脱征反应，即t-for-i和t-for-br反应是 对于将tritium引入特定位置特别有用 在没有氢转移催化剂的情况下分子，将是 调查。 在存在金属催化剂的情况下可能会导致去al alogenation 在Tritium Exchange中，是不可取的。 其中一些标记化合物的NMR nmr光谱将是 由劳伦斯·伯克利实验室的杨博士进行。