中文摘要：

摘要：目的探讨多巴胺D2受体显像剂131I-nalepride（131I-（s）O-N-[（1-烯丙基-2-吡咯烷基）甲基]-2，3-二甲氧基5-三丁基锡苯甲酰胺）的制备以及在小动物体内的性质，评价其在神经精神疾病诊断应用中的可行性。方法以（s）O-N-[（1-烯丙基-2-吡咯烷基）甲基]-2，3-二甲氧基-5-三丁基锡苯甲酰胺为标记前体，用双氧水法进行131I-nalepride的标记，行ICR小鼠生物分布特性实验，并对SD大鼠进行阻断实验和脑部放射自显影研究。结果131Inalepride标记率和放化纯均大于95％；ICR小鼠生物分布特性研究结果显示131I-nalepride在小鼠纹状体中摄取最多，小鼠尾静脉注射”。Inalepride4h后，纹状体与小脑比值即达111．87，12h后达到最高，为416．97；SD大鼠阻断实验和脑部放射自显影结果显示，在注射131Inalepride后，纹状体与小脑的光密度比值从7．43±0．86降至1．07±0．18，与阻断前比较差异有统计学意义（P〈O．05），说明131I-nalepride与多巴胺D2受体特异性结合很高；131I-nalepride进入血液后迅速被组织摄取，其中以肝、肾的早期摄取最高，肝为（14．82±3．88）%ID／g，肾为（10．28±1．65）％ID／g，各脏器的清除均较快。结论131Inalepride对多巴胺D2受体具有高度亲和性和特异性，可作为多巴胺D2受体的单光子发射计算机断层成像术显像剂并作为工具药筛选、评价其他抗精神病药物对多巴胺D2受体的亲和力。

英文摘要：

Objective To study the preparation of 131I-nalepride and its characters in small animal in vivo,and to evaluate the feasibility for its application in diagnosing neuropsychiatric disease. Methods s-5-（tributyltin）- N E（1-ethyl-2 pyrrolidinyl） meth yl]-2,3-dimethoxy-benzamide was used as the labeled precursor. The hydrogen peroxide method was adopted to labeP31 I-nalepride.The bio-distribution character test in ICR mice was performed. SD rats were performed the blocking experiment and the cerebral au- toradiography. Results The radiolabeled yield and radiochemical purity were over 95 ~. The results of the bio distribution character test showed that the striatum had the highest uptake. The striatum to cerebellum uptake radio（ST/CB） reached 111.87 at 4 h after injection and the maximum ST/CB value of 416.97 at 12 h after injection. Regional brain autoradiography showed that the optical densities were significantly decreased from 7.43±0.86 to 1.07±0.18 after injection of 1311-naleprid（P〈0.05）. These results indi- cated that 1811 nalepride had specific binding to the dopamine D2 receptor. 1311 nalepride was rapidly uptaken by organs after injec- tion. The initial uptake in liver and kidney were higher and the % ID/g values were 14.82±3.88 and 10.28±1.65 receptively. The tracer was cleared out from the organ quite rapidly. Conclusion 131i_nalepride has the high affinity and specificity to dopamine D2 receptor,which could be used as the EPECT imaging agent of dopamine D2 receptors and as a tool drug to screen and evaluate the affinity of other antipsychotic agents to dopamine D2 receptors.