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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 |
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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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ISSN | ||||||
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. | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa |