Bergström K A, Kuikka J T, Ahonen A, Vanninen E
Department of Clinical Physiology and Nuclear Medicine, Kuopio University Hospital, Finland.
J Nucl Biol Med (1991). 1994 Dec;38(4 Suppl 1):128-31.
beta-CIT (2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane) is a new ligand that has a high affinity to dopamine and serotonin re-uptake sites. [123I] beta-CIT was prepared by reacting the corresponding trimethylstannyl precursor with no-carrier-added 123I. Iodogen was used as an oxidizing agent. The labeling mixture was purified by filtration through a mini-column. The purity of the product was confirmed by analytical HPLC. The total radiochemical yield was 67 +/- 5%. The radiochemical purity was > 95% and the specific activity was > 107 GBq/mol (> 2900 Ci/mmol). The final product was confirmed to be free of endotoxins before intravenous administration. Two healthy male volunteers were injected iv with 120-160 MBq of [123I] beta-CIT and scanned with a 3-head gamma-camera (Siemens MultiSPECT3). Dynamic SPECT scans were performed for up to 2 hours. There was a high accumulation of radioactivity in the striatum and in the thalamus, and some in the medial prefrontal area. Thus, we have developed an easy method to prepare [123I] beta-CIT with a high specific radioactivity and in a sufficient radiochemical yield. Specific [123I] beta-CIT binding in striatal and thalamic regions was demonstrated in humans. [123I] beta-CIT is a potential marker of the dopamine and serotonin transporters and can be used to study the pathophysiology of Parkinson's disease, as well as neuropsychiatric disorders.
β-CIT（2β-羧甲氧基-3β-（4-碘苯基）托烷）是一种对多巴胺和5-羟色胺再摄取位点具有高亲和力的新型配体。[123I]β-CIT通过使相应的三甲基锡前体与无载体添加的123I反应制备。碘珠用作氧化剂。标记混合物通过微型柱过滤进行纯化。产物的纯度通过分析型高效液相色谱法确认。总放射化学产率为67±5%。放射化学纯度>95%，比活度>107GBq/mol（>2900Ci/mmol）。最终产物在静脉给药前被确认为无内毒素。两名健康男性志愿者静脉注射120 - 160MBq的[123I]β-CIT，并用三头γ相机（西门子MultiSPECT3）进行扫描。进行动态单光子发射计算机断层扫描长达2小时。纹状体和丘脑中放射性高度聚集，内侧前额叶区域也有一些聚集。因此，我们开发了一种简便方法来制备具有高比放射性且放射化学产率充足的[123I]β-CIT。在人体中证实了[123I]β-CIT在纹状体和丘脑区域的特异性结合。[123I]β-CIT是多巴胺和5-羟色胺转运体的潜在标志物，可用于研究帕金森病以及神经精神疾病的病理生理学。
