Preparation of Radiolabeled Materials

合同包括两个主要活动：合成和与存储库相关的活动。后者包括放射性标记化合物的冷冻储存、分析、提纯和运输。年度预算的约70%用于合成，其余部分用于支付维持与储存库有关的活动的费用，包括冷藏设施(零下70摄氏度)、无线电安全和无线电废物处理。现在储存的115种化合物的估计价值超过100万美元。 选择用于合成的化合物既涉及合成产物，也涉及天然产物，涵盖了广泛的化学结构和复杂性。重点将放在高比活性的~3H标记化合物和~(14)C标记化合物的合成上。根据NEXT计划、生物评估委员会(BEC)和NIH RAID计划的程序请求，启动新的放射性标记合成。 放射性标记化合物主要用于支持临床前药理学、毒理学和作用机制研究。这些研究对成功的药物开发至关重要，因为它们帮助研究人员确定重要的性质，例如母体化合物在体内的命运。此外，放射性标记剂被用来识别代谢物，选择最佳给药途径，并监测化合物的生物处置。

The contract encompasses two major activities: synthesis and repository-related activities. The latter includes deep freeze storage, analysis, purification and shipping of radiolabeled compounds. About 70% of the annual budget is utilized for synthesis and the remainder is required to cover expenses incurred to maintain the repository-related activities including the deep freeze storage facility (-70 degrees Celsius) radio-safety and radio-waste disposal. The estimated value of the stored compounds now number 115 exceeds $1,000,000. The compounds selected for syntheses involve both synthetics and natural products and cover a wide variety of chemical structures and complexity. The major focus will be on the synthesis of 3H-labeled compounds of high specific activity as well as 14C-labeled compounds. New radiolabeled syntheses are initiated upon program request derived from NExT program, Biological Evaluation Committee (BEC) and also from NIH RAID program. The radiolabeled compounds are used primarily to support preclinical pharmacology, toxicology, and mechanism of action studies. These studies are critical for successful drug development since they help the investigators define important properties, such as the in vivo fate of the parent compound. Furthermore, radiolabeled agents are used to identify metabolites, select the optimal route of drug administration, and monitor the biological disposition of compounds.