进行帕金森病治疗新药的早期临床药理学研究时，为了评价药物疗效，研究者们通常会使用如VAS评分、数字广度试验、注意力分离试验、血药浓度或脑内药物浓度测定等方法，但这些方法受主观影响大，而且体循环中含有药物并不代表药物可以进入脑内、入脑也不一定与靶点结合。我们以往也使用上述方法来评价新药，在实际操作过程中发现这样不仅耗费大量人力物力，而且准确性差。通过动物实验，我们发现β+电子发射断层人脑纹状体显像技术可以直接检测药物对靶点的占据时间和强度，用这种方法来描述药效更客观、更准确。本课题将β+电子发射断层人脑纹状体显像技术和传统的新药早期临床研究方法结合在一起，通过使用能与脑内纹状体多巴胺受体特异结合的18F-Fallypride作为受体显像剂，来评价试验药物发挥药效时的受体占有率、占有率随时间的变化、以及受体占有率-血药浓度-给药剂量间的相互关系，帮助我们优化给药方案设计、验证临床药理学概念。

Investigators often use some traditional method to evaluate the efficacy of anti-Parkinson's disease drugs in early phase clinical pharmacology research, such as VAS score, digit span test, attention separation test, blood concentration quantitation, brain concentration quantitation, et al. These above methods are subjective, drug in blood does not means that the drug can go through the blood-brain barrier, and drug in brain dose not means that the drug can bind with the receptor. We also use these methods described above in the past to evaluate new drugs and found that not only spend a lot of manpower and resources, but also poor accuracy in actual operation. Based on some animal experiments, we found that the β+ positron emission tomography receptor imaging on human brain striatum could evaluate the efficacy by directly detecting the receptor occupancy ratio and the time, which was more accurate and objective. We plan to integrate the β+ positron emission tomography receptor imaging technology of nuclear medicine and traditional methods for early phase clinical studies of new drugs together, to measure the occupied rate of receptors, the rate of change with time and the relationship within the dose, receptor occupancy rate and concentration by using the 18F-Fallypride as the receptor imaging agents, which could bind with the dopamine D2/D3 receptor specifically. This method could help us to optimize the dosing regimen design and verify the concept of clinical pharmacology.