多巴胺D_3体显像剂^(125)I-7-OH-PIPAT生物学特性初探  

The preliminary biocharacteristic study of a potential dopamine D_3 receptor imaging agent, ^(125) I-7-OH-PIPAT

作　　者：朱爱芝[1] 薛井泉[1] 柴之芳[1] 

机构地区：[1]中国科学院高能物理研究所,中国科学院核分析技术开放实验室,北京100039

出　　处：《中华核医学杂志》2003年第2期107-109,共3页Chinese Journal of Nuclear Medicine

基　　金：中国科学院知识创新工程资助项目 (U 51 6 3)

摘　　要：目的　研究自行研制的多巴胺D3受体显像剂1 2 5I 7 羟基 2 [N 丙基 N (3′ 碘 2′ 烯丙基 ) ]氨基四氢萘满 (7 OH PIPAT)的生物学特性。方法　用核素示踪法研究1 2 5I 7 OH PIPAT在大鼠体内的生物分布 ,用放射自显影法研究1 2 5I 7 OH PIPAT在大鼠脑组织的键合部位。结果　1 2 5I 7 OH PIPAT在脑中浓集达 1% ;放射自显影结果示 ,1 2 5I 7 OH PIPAT在边缘脑区 ,尤其嗅结节部位有较高浓度结合。结论　1 2 5I 7 OH PIPAT可通过血脑屏障 ,对多巴胺D3受体有亲和性 ,具脑功能显像的潜在活性。Objective To study the biocharacteristics of a potential dopamine D 3 receptor imaging agent, 125 I 7 hydroxy 2 [ N propyl N (3′ iodo 2′ propenyl) amino]tetralin (7 OH PIPAT) which was synthesized in this lab. Methods 125 I 7 OH PIPAT was used as a radioactive tracer to study the biodistribution of 125 I 7 OH PIPAT in rats and in particular, in the brain regions, and autoradiography was used to study the binding sites of 125 I 7 OH PIPAT in rat brain slices. Results The uptake of 125 I 7 OH PIPAT in the whole brain reached to 1%, and autoradiography showed that 125 I 7 OH PIPAT was accumulated at olfactory tubercle and limbic regions of rat brain. Conclusions 125 I 7 OH PIPAT is able to penetrate the brain blood barrier, and has the affinity to dopamine D 3 receptors. It has the potential activity to be a dopamine D 3 receptor imaging agent.

关 键 词：多巴胺D3受体显像剂 ^125I-7-0H-PIPAT 生物学特性 放射自显影法 药代动力学 比学合成 多巴胺 

分 类 号：R817[医药卫生—影像医学与核医学]