Imaging of peripheral-type benzodiazepine receptor in tumor: in vitro binding and in vivo biodistribution of N

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• 作者：Tomoteru Yamasaki ; Katsushi Kumata ; Kazuhiko Yanamoto ; Akiko Hatori ; Makoto Takei ; Yukio Nakamura ; Sachiko Koike ; Koichi Ando ; Kazutoshi Suzuki ; Ming-Rong Zhang
• 关键词：Tumor imaging ; [¹¹C]DAC ; PBR ; PET ; NFSa
• 刊名：Nuclear Medicine and Biology
• 出版年：2009
• 出版时间：October 2009
• 年：2009
• 卷：36
• 期：7
• 页码：801-809
• 全文大小：1001 K

文摘

Introduction

The aim of this study was to evaluate N-benzyl-N-[¹¹C]methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide ([¹¹C]DAC) as a novel peripheral-type benzodiazepine receptor (PBR) ligand for tumor imaging.

Methods

[¹¹C]DAC was synthesized by the reaction of a desmethyl precursor with [¹¹C]CH₃I. In vitro uptake of [¹¹C]DAC was examined in PBR-expressing C6 glioma and intact murine fibrosarcoma (NFSa) cells. In vivo distribution of [¹¹C]DAC was determined using NFSa-bearing mice and small-animal positron emission tomography (PET).

Results

[¹¹C]DAC showed specific binding to PBR in C6 glioma cells, a standard cell line with high PBR expression. Specific binding of [¹¹C]DAC was also confirmed in NFSa cells, a target tumor cell line in this study. Results of PET experiments using NFSa-bearing mice, showed that [¹¹C]DAC was taken up specifically into the tumor, and pretreatment with PK11195 abolished the uptake.

Conclusions

[¹¹C]DAC was taken up into PBR-expressing NFSa. [¹¹C]DAC is a promising PET ligand that can be used for imaging PBR in tumor-bearing mice.