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Neopentyl glycol as a scaffold to provide radiohalogenated theranostic pairs of high in vivo stability
https://repo.qst.go.jp/records/84559
https://repo.qst.go.jp/records/84559287e312e-7336-4052-9cb7-b8925b9a2db0
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-08-25 | |||||
| タイトル | ||||||
| タイトル | Neopentyl glycol as a scaffold to provide radiohalogenated theranostic pairs of high in vivo stability | |||||
| 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 | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Suzuki, Hiroyuki (Chiba Univ.)
× Suzuki, Hiroyuki (Chiba Univ.)× Kaizuka,, Yuta (Chiba Univ.)× Tatsuta,, Maho (Tokyo Inst. Tech.)× Tanaka, Hiroshi (Tokyo Inst. Tech.)× Washiya,, Nana (Chiba Univ.)× Shirakami,, Yoshifumi (Osaka Univ.)× Ooe,, Kazuhiro (Osaka Univ.)× Toyoshima,, Atsushi (Osaka Univ.)× Watabe,, Tadashi (Osaka Univ.)× Teramoto,, Takahiro (Osaka Univ.)× Ichiro, Sasaki× Shigeki, Watanabe× Noriko, Ishioka× Hatazawa,, Jun (Osaka Univ.)× Uehara,, Tomoya (Chiba Univ.)× Arano,, Yasushi (Chiba Univ.)× Hiroyuki, Suzuki× Hiroshi, Tanaka× Ichiro, Sasaki× Shigeki, Watanabe× Noriko, Ishioka |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The high in vivo stability of 2,2-dihydroxymethyl-3-[18F]fluoropropyl-2-nitroimidazole ([18F]DiFA) prompted us to evaluate neopentyl as a scaffold to prepare a radiotheranostic system with radioiodine and astatine.Three DiFA derivatives with one, two, or without a hydroxyl group were synthesized. While all 125I-labeled compounds remained stable against nucleophilic substitution, only a 125I-labeled neopentyl glycol was stable against cytochrome P450 (CYP)-mediated metabolism and showed high stability against in vivo deiodination. 211At-labeled neopentyl glycol also remained stable against both nucleophilic substitution and CYP-mediated metabolism. 211At labeled neopentyl glycol showed the biodistribution profiles similar to those of its radioiodinated counterpart in contrast to the 125I/211At-labeled benzoate pair. The urine analyses confirmed that 211At-labeled neopentyl glycol was excreted in the urine as a glucuronide conjugate with the absence of free [211At]At-. These findings indicate that neopentyl glycol would constitute a promising scaffold to prepare a radiotheranostic system with radioiodine and 211At. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry 巻 64, 号 21, p. 15846-15857, 発行日 2021-11 |
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| 出版者 | ||||||
| 出版者 | ACS | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.1c01147 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01147 | |||||
