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Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of 186Re-MAG3-conjugated bisphosphonate (186Re-MAG3-HBP), an agent for treatment of painful bone metastases
https://doi.org/10.24517/00028408
https://doi.org/10.24517/00028408a894ab2b-d82a-4da8-97a2-764033f09754
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
ME-PR-OGAWA-K-115.pdf (303.9 kB)
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| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||||
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| 公開日 | 2017-10-05 | |||||||||||||
| タイトル | ||||||||||||||
| タイトル | Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of 186Re-MAG3-conjugated bisphosphonate (186Re-MAG3-HBP), an agent for treatment of painful bone metastases | |||||||||||||
| 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 | 10.24517/00028408 | |||||||||||||
| ID登録タイプ | JaLC | |||||||||||||
| 著者 |
Ogawa, Kazuma
× Ogawa, Kazuma× Mukai, Takahiro× Kawai, Keiichi× Takamura, Norito× Hanaoka, Hirofumi× Hashimoto, Kazuyuki× Shiba, Kazuhiro× Mori, Hirofumi× Saji, Hideo |
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| 著者別表示 |
小川, 数馬
× 小川, 数馬
× 川井, 恵一
× 柴, 和弘
× 森, 厚文
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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 / 金沢大学学際科学実験センターアイソトープ総合研究施設 | |||||||||||||
| 書誌情報 |
European Journal of Nuclear Medicine and Molecular Imaging 巻 36, 号 1, p. 115-121, 発行日 2009-01-01 |
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| 収録物識別子タイプ | ISSN | |||||||||||||
| 収録物識別子 | 1619-7070 | |||||||||||||
| NCID | ||||||||||||||
| 収録物識別子タイプ | NCID | |||||||||||||
| 収録物識別子 | AA1161516X | |||||||||||||
| DOI | ||||||||||||||
| 関連タイプ | isVersionOf | |||||||||||||
| 識別子タイプ | DOI | |||||||||||||
| 関連識別子 | 10.1007/s00259-008-0925-8 | |||||||||||||
| 出版者 | ||||||||||||||
| 出版者 | Springer Verlag (Germany) | |||||||||||||
| 抄録 | ||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||
| 内容記述 | Purpose: We have developed a 186Re-mercaptoacetylglycylglycylglycine complex-conjugated bisphosphonate (186Re-MAG3-HBP) for the treatment of painful bone metastases. We assumed competitive inhibitors of protein binding to be useful for procuring a favorable biodistribution of 186Re-MAG3-HBP for the palliation of bone pain because it has been reported that the concurrent administration of 99mTc-MAG3 and drugs with high affinity for serum protein produced competitive displacement at specific binding sites and enhanced total clearance and tissue distribution. Methods: The displacement effects of several protein-binding inhibitors on the protein binding of 186Re-MAG3-HBP were investigated. Biodistribution experiments were performed by intravenously administering 186Re-MAG3-HBP into rats with ceftriaxone as a competitive protein-binding inhibitor or saline. Results: The protein binding of 186Re-MAG3-HBP in rat serum, human serum, and a human serum albumin solution was significantly decreased by the addition of ceftriaxone, which has high affinity for binding site I on serum albumin. In the biodistribution experiments, pretreatment with ceftriaxone enhanced the clearance of the radioactivity of 186Re-MAG3-HBP in blood and nontarget tissues but had no effect on accumulation in bone. Conclusions: The findings suggested that the use of protein-binding competitive inhibitors would be effective in improving the pharmacokinetics of radiopharmaceuticals with high affinity for serum protein. © 2008 Springer-Verlag. | |||||||||||||
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| 出版タイプ | AM | |||||||||||||
| 出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||||||||||
