131I-epidepride的制备与SD大鼠体内分布特性研究

采用双氧水标记法和氯胺 -T法进行13 1I -epidepride标记 ,考察标记物的纯度及稳定性 ,并进行SD大鼠体内分布特性研究。实验结果表明 ,双氧水法和氯胺 -T法标记率分别为 97.4 %和 5 2 .9%。标记物的生理盐水溶液室温放置 4h ,放化纯大于 90 %。大鼠静脉注射13 1I -epide pride的生理盐水溶液后 ,纹状体与小脑比值在注射后 32 0min时高达 2 37:1。13 1I -epidepride进入血液后很快被组织摄取 ,其中以肺的早期摄取最高 (2 .11± 1.0 5 ) %ID·g- 1,各脏器的清除均较快 (T1/2 <4h) ,甲状腺的摄取率随时间的延长而增加。

Preparation of 131I-epidepride and biodistribution study in SD rats

The purpose of this article is to study the preparation and biodistribution in animals of dopamine D2 receptor ligand 131 I-epidepride. Epidepride was 131 I radioiodinated with hydroperoxide or chloramine-T method. The purity and stability of 131 I-epidepride were studied by HPLC and TLC, the dynamic distribution in brain and critical organs of SD rats were studied. The radiolabelling yields of 131 I-epidepride were 97.4% and 52.9% respectively. With no more purification, the hydroperoxide method is better than the chloramine-T method. After 4 hours in room temperature, the radiochemical purity of 131 I-epidepride was still over 90%. The striatum uptake was good, the striatum/cerebellum ratio reached 237:1 at 320min. Among the critical organs,lung had the first and the highest uptake. All organs had quick clearance ( T 1/2 <4h). The radioactivity in thyroid increased with time. The results show that 131 I-epidepride has a high striatum uptake and a high striatum/cerebellum ratio. 131 I-epidepride is a good dopamine D2 receptor agent