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LC/MS/MS approach to determine in vivo receptor occupancy of CNS drugs at GABAA and D2 receptors in rat brain

机译:LC / MS / MS方法,以确定大鼠GABAA和D2受体在GABAA和D2受体中的体内受体占用

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Radiolabeled tracer is not required. This will result in: (1) Radiolabeling fewer new compounds; (2) Less radioactive waste generated for RO studies. Direct measurement of tracer and pretreatment drug: (1)Capable of measuring both parent tracer and metabolite(s); (2) Exposure and occupancy analyzed on the same platform Rapid means of screening PET candidates; (3) Using criteria for a trace-dose in vivo tool compound for CNS (high affinity, selectivity, brain permeability); Possibility of analyzing more than one drug or target: (1) Practical use of multiple tracers in the same animal; (2) Not limited to existing PET ligands.
机译:不需要放射性标记的示踪剂。这将导致:(1)放射性标记更少的新化合物; (2)对RO研究产生的放射性废物较少。直接测量示踪剂和预处理药物:(1)能够测量母体示踪剂和代谢物; (2)在同一平台上分析的曝光和占用快速筛选宠物候选人的方法; (3)使用用于CNS的体内工具化合物的痕量剂量标准(高亲和力,选择性,脑渗透率);分析多种药物或目标的可能性:(1)在同一动物中的​​多个示踪剂的实际应用; (2)不限于现有的宠物配体。

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