Evaluation of Radioiodinated 1-[2-(3,4-Dimethoxyphenyl)ethyl]-4-(2-iodophenylpropyl)piperazine as a Tumor Diagnostic Agent with Functional Sigma Receptor Imaging by Single Photon Emission Computed Tomography(Pharmacology)
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概要
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Radioiodinated 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(2-iodophenylpropyl)piperazine (o-BON) and 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-iodophenylpropyl)piperazine (m-BON) were evaluated as single photon emission computed tomography (SPECT) radiopharmaceuticals for tumor imaging by visualization of sigma receptors. In vivo biodistribution studies of [^<125>I]o-BON and [^<125>I]m-BON in tumor-bearing mice showed a high tumor uptake and prolonged retention of radiolabeled compounds in the tumor. In contrast with these factors, the blood and muscle accumulations were low, which resulted in a good tumor-to-blood ratio and tumor-to-muscle ratio. In peripheral organs, [^<125>I]o-BON showed rapid clearance in comparison with [^<125>I]m-BON. Selective interactions of [^<125>I]o-BON and [^<125>I]m-BON with sigma receptors on tumor cell membranes were confirmed by pretreatment experiments with various sigma and other receptor ligands. [^<125>I]o-BON possesses higher specific binding toward sigma receptors than does [^<125>I]m-BON; thus, [^<125>I]o-BON was chosen for further evaluations. High uptake of [^<125>I]o-BON was observed in various tumors, and a good linear correlation (R^2=0.70) was found between accumulation of [^<125>I]o-BON and the sigma receptor expression level. Furthermore, the accumulation of [^<125>I]o-BON in tumors reflected their proliferation rate. These results suggest that it is feasible to use radioiodinated o-BON as a marker for measuring the proliferative status associated with sigma receptor expression.
- 公益社団法人日本薬学会の論文
- 2008-05-01
著者
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Mori Tetsuya
Osaka University Of Pharmaceutical Sciences
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Hirata Masahiko
Osaka University Of Pharmaceutical Sciences
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UMEDA Takuya
Osaka University of Pharmaceutical Sciences
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ABE Takeshi
Osaka University of Pharmaceutical Sciences
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YAMAMOTO Tomoya
Osaka University of Pharmaceutical Sciences
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OHMOMO Yoshiro
Osaka University of Pharmaceutical Sciences
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