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Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent
https://doi.org/10.24517/00065249
https://doi.org/10.24517/00065249a3c37ed3-27a7-431f-bdd2-427c605b94c7
| 名前 / ファイル | ライセンス | アクション |
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ME-PR-SHIBA-K-2-54.pdf (1.1 MB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||||||
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| 公開日 | 2022-02-03 | |||||||||||||||
| タイトル | ||||||||||||||||
| タイトル | Development and evaluation of a novel radioiodinated vesamicol analog as a sigma receptor imaging agent | |||||||||||||||
| 言語 | ||||||||||||||||
| 言語 | eng | |||||||||||||||
| 資源タイプ | ||||||||||||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||||||||
| 資源タイプ | journal article | |||||||||||||||
| ID登録 | ||||||||||||||||
| ID登録 | 10.24517/00065249 | |||||||||||||||
| ID登録タイプ | JaLC | |||||||||||||||
| 著者 |
Ogawa, Kazuma
× Ogawa, Kazuma× Kanbara, Hiroya× Shiba, Kazuhiro× Kitamura, Yoji× Kozaka, Takashi× Kiwada, Tatsuo× Odani, Akira |
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| 著者別表示 |
小川, 数馬
× 小川, 数馬
× 柴, 和弘
× 北村, 暘二
× 小阪, 孝史
× 小谷, 明
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| 提供者所属 | ||||||||||||||||
| 内容記述タイプ | Other | |||||||||||||||
| 内容記述 | 金沢大学疾患モデル総合研究センター | |||||||||||||||
| 書誌情報 |
EJNMMI Research 巻 2, 号 1, p. 54, 発行日 2012-09-28 |
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| ISSN | ||||||||||||||||
| 収録物識別子タイプ | ISSN | |||||||||||||||
| 収録物識別子 | 2191-219X | |||||||||||||||
| DOI | ||||||||||||||||
| 関連タイプ | isIdenticalTo | |||||||||||||||
| 識別子タイプ | DOI | |||||||||||||||
| 関連識別子 | 10.1186/2191-219X-2-54 | |||||||||||||||
| 出版者 | ||||||||||||||||
| 出版者 | Springer Verlag | |||||||||||||||
| 抄録 | ||||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||||
| 内容記述 | Background Sigma receptors are highly expressed in human tumors and should be appropriate targets for developing tumor imaging agents. Previously, we synthesized a vesamicol analog, (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol ((+)-p IV), with a high affinity for sigma receptors and prepared radioiodinated (+)-p IV. As a result, (+)-[125I]p IV showed high tumor uptake in biodistribution experiments. However, the accumulation of radioactivity in normal tissues, such as the liver, was high. We supposed that some parts of the accumulation of (+)-p IV in the liver should be because of its high lipophilicity, and prepared and evaluated a more hydrophilic radiolabeled vesamicol analog, (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-iodophenol ((+)-IV-OH). Methods (+)-[125I]IV-OH was prepared by the chloramine T method from the precursor. The partition coefficient of (+)-[125I]IV-OH was measured. Biodistribution experiments were performed by intravenous administration of a mixed solution of (+)-[125I]IV-OH and (+)-[131I]p IV into DU-145 tumor-bearing mice. Blocking studies were performed by intravenous injection of (+)-[125I]IV-OH mixed with an excess amount of ligand into DU-145 tumor-bearing mice. Results The hydrophilicity of (+)-[125I]IV-OH was much higher than that of (+)-[125I]p IV. In biodistribution experiments, (+)-[125I]IV-OH and (+)-[131I]p IV showed high uptake in tumor tissues at 10-min post-injection. Although (+)-[131I]p IV tended to be retained in most tissues, (+)-[125I]IV-OH was cleared from most tissues. In the liver, the radioactivity level of (+)-[125I]IV-OH was significantly lower at all time points compared to those of (+)-[131I]p IV. In the blocking studies, co-injection of an excess amount of sigma ligands resulted in significant decreases of tumor/blood uptake ratios after injection of (+)-[125I]IV-OH. Conclusions The results indicate that radioiodinated (+)-IV-OH holds a potential as a sigma receptor imaging agent. |
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| 権利 | ||||||||||||||||
| 権利情報 | Copyright © 2012 Ogawa et al.; licensee Springer. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. | |||||||||||||||
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| 出版タイプ | VoR | |||||||||||||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||||||
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| 識別子タイプ | URI | |||||||||||||||
| 関連識別子 | http://www.ejnmmires.com/ | |||||||||||||||
| 関連名称 | http://www.ejnmmires.com/ | |||||||||||||||
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| 識別子タイプ | URI | |||||||||||||||
| 関連識別子 | https://ejnmmires.springeropen.com/articles/10.1186/2191-219X-2-54 | |||||||||||||||
| 関連名称 | https://ejnmmires.springeropen.com/articles/10.1186/2191-219X-2-54 | |||||||||||||||
