MEDICATION DEVELOPMENT FOR COCAINE ABUSERS

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 在过去的报告所述期间取得了重要进展。RTI-336，一种在我们实验室首次测试和表征的化合物，已被批准用于人类第一阶段临床试验。预计它将成为精神刺激剂(可卡因、苯丙胺和甲基苯丙胺)滥用者和成瘾者的药物。在撰写这篇文章时，还没有发现排除进一步研究的毒性影响，还计划在人体上进行更多研究。 PET(正电子发射断层扫描)扫描的使用对于解决药物开发中的问题通常是重要的。在实践中，PET程序仅限于测量蛋白质水平或占有率。从早些时候发表的蛋白质周转和半衰期研究中，有人建议将PET程序扩大到包括动物相关蛋白质的周转测量。与单独测量水平相比，这将提供对各种蛋白质参与的更全面的看法。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Important progress has been made in the past reporting period. RTI-336, a compound first tested and characterized in our laboratory and has been approved for Phase I clinical trials in humans. It is expected to be a medication for psychostimulant (cocaine, amphetamine, and methamphetamine) abusers and addicts. As of this writing, no toxic effects were found that preclude further study, and additional studies are planned in humans. The utilization of PET (positron emission tomography) scanning is often important for addressing problems in medications development. In practice, the PET procedure has been limited to measuring levels of proteins or percentage occupancy. From studies of protein turnover and half-lives published earlier, it has been suggested that PET procedures be expanded to include turnover measurements of relevant proteins in animals. This will provide a more comprehensive view of the involvement of various proteins than is possible by measuring levels alone.