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Preparation and biological evaluation of 99mTcN-4-(cyclohexylpiperazin-1-yl)-dithioformate as a potential sigma receptor imaging agent

✍ Scribed by Jie Lu; Dejing Kong; Hongmei Jia; Winnie Deuther-Conrad; Peter Brust; Xuebin Wang

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
127 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The goal of this study is to develop a novel ^99m^Tc‐labeled σ receptor imaging agent. Potassium 4‐(cyclohexylpiperazin‐1‐yl)‐dithioformate, 2, and the corresponding rhenium complex, ReN‐2, were synthesized and characterized. ReN‐2 possessed moderate affinity toward σ~1~ (K~i~ = 1.94 ± 0.60 µmol/L) and σ~2~ (K~i~ = 2.83 ± 1.39 µmol/L) receptors. The radiolabeled complex ^99m^TcN‐2 was prepared in high yield (> 95%) through the [^99m^TcN] precursor and characterized by HPLC. ^99m^TcN‐2 was found to be a lipophilic and neutral complex with good stability. The biodistribution in tumor‐bearing mice showed that ^99m^TcN‐2 had good tumor uptake (2.12 ± 0.01 %ID/g at 2 h p.i.) and moderate brain uptake (0.27 ± 0.05 %ID/g at 2 h p.i.). After blocking with haloperidol, the uptakes by tumor and brain were lower than control. The results indicated that the complex has specific binding to the σ receptors in vivo. Further structural modifications of this complex are needed to obtain ^99m^Tc‐based σ receptor imaging agents with high affinity and subtype selectivity. Copyright © 2007 John Wiley & Sons, Ltd.

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