@article{oai:kanazawa-u.repo.nii.ac.jp:00028421,
 author = {小川, 数馬 and 川井, 恵一 and 柴, 和弘 and 森, 厚文 and Ogawa, Kazuma and Mukai, Takahiro and Kawai, Keiichi and Takamura, Norito and Hanaoka, Hirofumi and Hashimoto, Kazuyuki and Shiba, Kazuhiro and Mori, Hirofumi and Saji, Hideo},
 issue = {1},
 journal = {European Journal of Nuclear Medicine and Molecular Imaging},
 month = {Jan},
 note = {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., 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},
 pages = {115--121},
 title = {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},
 volume = {36},
 year = {2009}
}