外周苯二氮受体示踪剂的合成和评价

高等学校化学学报

外周苯二氮受体示踪剂的合成和评价

李斌¹, 李剑峰², 傅磊³, 孙晓光¹, 刘建军¹, 黄钢¹

1. 上海交通大学医学院, 仁济医院核医学科, 上海 200127;
2. 中国科学院上海生命科学院上海药物研究所, 上海 201203;
3. 上海交通大学药学院, 上海 200030

收稿日期:2007-04-23 修回日期:1900-01-01 出版日期:2008-01-10 发布日期:2008-01-10
通讯作者: 黄钢

Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors

LI Bin¹, LI Jian-Feng², FU Lei³, SUN Xiao-Guang¹, LIU Jian-Jun¹, HUANG Gang¹*

1. Department of Nuclear Medicine, Renji Hospital, Medical School of Shanghai Jiaotong University, Shanghai 200127, China;
2. Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China;
3. School of Pharmacy, Shanghai Jiaotong University, Shanghai 200030, China

Received:2007-04-23 Revised:1900-01-01 Online:2008-01-10 Published:2008-01-10
Contact: HUANG Gang

摘要/Abstract

摘要： 合成了用作外周苯二氮受体潜在的选择性配体的N,N-二乙基-2-(4-碘苯基)-6-三氟甲基-咪唑并[1,2-a]吡啶-3-乙酰胺(ITFZOL). 其放射性标记物[¹²⁵I]ITFZOL通过碘脱锡化反应制备, 放化得率75%~85%, 比活度大于76 GBq/μmol. 小鼠尾静脉注射[¹²⁵I]ITFZIOL后, 放射性集中分布于肾上腺、肺、肾、心、嗅球和小脑等外周苯二氮受体高密度区域. 预先给与外周苯二氮受体选择性配体PK11195明显减少外周苯二氮受体高密度区域放射性分布, 提示[¹²⁵I]ITFZOL对外周苯二氮受体具有较高的特异亲和性. 生物活性数据表明, [¹²⁵I]ITFZO是一种潜在的选择性外周苯二氮受体单光子放射性配体.

关键词: 外周苯二氮受体, 放射性配体, 咪唑并吡啶

Abstract: The 2-iodophenyl-imidazo[1,2-a]-pyridines tirfluoromethyl derivative(ITFZOL) was prepared to study the PBR. The [¹²⁵I] analogue was prepared via iododestannylation reaction in radiochemical yields of 75%—85% and a specific activity>76 GBq/μmol. After injection of [¹²⁵I] ITFZOL into mice through the tail vein, high accumulations of radioactivity were found in PBR-rich tissues such as adrenal, lung, kidney, heart, olfactory bulb and cerebellum. Per-administration of PBR-selective PK11195 displayed a significant reduction of radioactivity, suggesting a high specific binding of [¹²⁵I] ITFZOL to PBR. The biological data reveal that [¹²⁵I] ITFZOL is a potential and selective single photo emitting radioligand for PBR.

Key words: Peripheral benzodiazepine receptor, Radioligand, Imidazol[1,2-a]pyridine

中图分类号:

O626
O657

TrendMD:

李斌,李剑峰,傅磊,孙晓光,刘建军,黄钢 . 外周苯二氮受体示踪剂的合成和评价. 高等学校化学学报, doi: .

LI Bin¹, LI Jian-Feng², FU Lei³, SUN Xiao-Guang¹, LIU Jian-Jun¹, HUANG Gang¹*. Synthesis and Evaluation of a Trace for Peripheral Benzodiazepine Receptors. Chem. J. Chinese Universities, doi: .