| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2017-10-05 |
| タイトル |
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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 |
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言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| ID登録 |
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ID登録 |
10.24517/00028408 |
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ID登録タイプ |
JaLC |
| 著者 |
Ogawa, Kazuma
Mukai, Takahiro
Kawai, Keiichi
Takamura, Norito
Hanaoka, Hirofumi
Hashimoto, Kazuyuki
Shiba, Kazuhiro
Mori, Hirofumi
Saji, Hideo
|
| 著者別表示 |
小川, 数馬
川井, 恵一
柴, 和弘
森, 厚文
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| 提供者所属 |
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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 |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
1619-7070 |
| NCID |
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収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA1161516X |
| DOI |
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関連タイプ |
isVersionOf |
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識別子タイプ |
DOI |
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関連識別子 |
10.1007/s00259-008-0925-8 |
| 出版者 |
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出版者 |
Springer Verlag (Germany) |
| 抄録 |
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内容記述タイプ |
Abstract |
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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 |
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出版タイプ |
AM |
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出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
ME-PR-OGAWA-K-115.pdf (303.9 kB)
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