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2β-甲氧羰基-3β-(3'-[(123)I]碘苯基)托烷([(123)I]YP256)作为一种血清素转运体放射性示踪剂的合成、放射性标记及狒狒单光子发射计算机断层显像成像

Synthesis, radiolabeling and baboon SPECT imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl)tropane ([(123)I]YP256) as a serotonin transporter radiotracer.

作者信息

Bois Frederic, Baldwin Ronald M, Amici Louis, Al-Tikriti Mohammed S, Kula Nora, Baldessarini Ross, Innis Robert B, Staley Julie K, Tamagnan Gilles D

机构信息

Yale University, School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA.

出版信息

Nucl Med Biol. 2008 Jan;35(1):53-9. doi: 10.1016/j.nucmedbio.2007.09.002.

DOI:10.1016/j.nucmedbio.2007.09.002
PMID:18158943
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2276982/
Abstract

To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson's disease, Alzheimer's disease and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl) tropane (YP256, 6). The radiolabeling was performed by iododestannylation using sodium [(123)I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.

摘要

为开发一种潜在的单光子发射计算机断层扫描（SPECT）探针，以评估血清素能系统（5-HTT）的完整性，该系统功能障碍与帕金森病、阿尔茨海默病和抑郁症等多种疾病相关，我们报告了2β-甲氧羰基-3β-（3'-[（123）I]碘苯基）托烷（YP256，6）的合成、放射性标记及在狒狒体内的成像。放射性标记通过使用[（123）I]碘化钠和过氧乙酸进行碘去锡化反应来完成。尽管该配体在体外对5-HTT的选择性高于多巴胺转运体，但在狒狒体内进行的SPECT成像并未显示出其在脑内有选择性的5-HTT蓄积。

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