Synthesis and evaluation of a trace for peripheral benzodiazepine receptors

被引：0

作者：

Li Bin ^{[1
]}

Li Jian-Feng ^{[2
]}

Fu Lei ^{[3
]}

Sun Xiao-Guang ^{[1
]}

Liu Jian-Jun ^{[1
]}

Huang Gang ^{[1
]}

机构：

[1] Shanghai Jiao Tong Univ, Sch Med, Renji Hosp, Dept Nucl Med, Shanghai 200127, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

[3] Shanghai Jiao Tong Univ, Sch Pharm, Shanghai 200030, Peoples R China

来源：

CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE | 2008年 / 29卷 / 01期

关键词：

peripheral benzodiazepine receptor; radioligand; imidazol [1,2-a] pyridine;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The 2-iodophenyl-imidazo [1,2-a]-pyridines tlirfluoromethyl derivative (ITFZOL) was prepared to study the PBR. The [I-125] analogue was prepared via iododestannylation reaction in radiochemical yields of 75%-85% and a specific activity > 76 GBq/mu mol. After injection of [I-125] ITFZOL into mice through the tall 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 [I-125] ITFZOL to PBR. The biological data reveal that [I-125] ITFZOL is a potential and selective single photo emitting radioligand for PBR.

引用

页码：86 / 89

页数：4