123I标记的2'-碘螺哌隆的制备及使用单光子发射计算机断层扫描（SPECT）对人脑D2多巴胺受体进行成像

Preparation of 123I-labeled 2'-iodospiperone and imaging of D2 dopamine receptors in the human brain using SPECT.

作者信息

Saji H, Iida Y, Magata Y, Yonekura Y, Iwasaki Y, Sasayama S, Konishi J, Nakatsuka I, Shiba K, Yoshitake A

机构信息

Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.

出版信息

Int J Rad Appl Instrum B. 1992 Jul;19(5):523-9. doi: 10.1016/0883-2897(92)90147-q.

DOI:10.1016/0883-2897(92)90147-q

PMID:1399682

Abstract

[123I]2'-ISP was readily prepared using a radioiodine exchange reaction with a radiochemical yield of approx. 50% after HPLC purification. The radiochemical purity of the product was more than 98% and the specific activity was 5.55-11.1 GBq/mumol. Biodistribution studies performed in mice indicated that injection of [123I]2'-ISP with albumin produced a higher gastric uptake and a lower brain uptake than injection of the radioligand in a weakly acidic solution. In addition, toxicity tests performed in mice demonstrated that acute toxic effects would be very unlikely to be encountered if 2'-ISP was used for diagnostic purposes. A preliminary imaging study with [123I]2'-ISP in a healthy human volunteer showed its specific uptake by the basal ganglia, a region of the brain known to have a high density of D2 dopamine receptors.

摘要

[123I]2'-碘代司帕沙星通过放射性碘交换反应很容易制备，经高效液相色谱（HPLC）纯化后，放射化学产率约为50%。产物的放射化学纯度大于98%，比活度为5.55 - 11.1 GBq/μmol。在小鼠身上进行的生物分布研究表明，与在弱酸性溶液中注射放射性配体相比，将[123I]2'-碘代司帕沙星与白蛋白一起注射时，胃摄取量更高，脑摄取量更低。此外，在小鼠身上进行的毒性试验表明，如果将2'-碘代司帕沙星用于诊断目的，极不可能出现急性毒性作用。在一名健康人类志愿者身上用[123I]2'-碘代司帕沙星进行的初步成像研究显示，基底神经节有特异性摄取，基底神经节是大脑中已知D2多巴胺受体密度较高的区域。