@article{oai:kanazawa-u.repo.nii.ac.jp:00058965,
 author = {小川, 数馬 and 絹谷, 清剛 and 柴, 和弘 and 森, 厚文 and Ogawa, Kazuma and Mukai, Takahiro and Asano, Daigo and Kawashima, Hidekazu and Kinuya, Seigo and Shiba, Kazuhiro and Hashimoto, Kazuyuki and Mori, Hirofumi and Saji, Hideo},
 issue = {1},
 journal = {Journal of Nuclear Medicine},
 month = {Jan},
 note = {Previously, based on the concept of bifunctional radiopharmaceuticals, we developed a highly stable 186Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate, [[[[(4-hydroxy-4,4-diphosphonobutyl) carbamoylmethyl]carbamoylmethyl] carbamoylmethyl]carbamoylmethanethiolate] oxorhenium(V) (186Re-MAG3-HBP), for the treatment of painful bone metastases. This agent showed a superior biodistribution as a bone-seeking agent in normal mice when compared with 186Re-1-hydroxyethylidene-1,1- diphosphonate (186Re-HEDP). In this study, we evaluated the therapeutic effects of 186Re-MAG3-HBP using an animal model of bone metastasis. Methods: The model was prepared by injecting syngeneic MRMT-1 mammary tumor cells into the left tibia of female Sprague-Dawley rats. 186Re-MAG3-HBP (55.5, 111, or 222 MBq/kg) or 186Re-HEDP (55.5 MBq/kg) was then administered intravenously 21 d later. To evaluate the therapeutic effects and side effects, tumor size and peripheral blood cell counts were determined. Palliation of bone pain was evaluated by a von Frey filament test. Results: In the rats treated with 186Re-HEDP, tumor growth was comparable with that in untreated rats. In contrast, when 186Re-MAG3-HBP was administered, tumor growth was significantly inhibited. Allodynia induced by bone metastasis was attenuated by treatment with 186Re-MAG3-HBP or 186Re-HEDP, but 186Re-MAG3- HBP tended to be more effective. Conclusion: These results indicate that 186Re-MAG3-HBP could be useful as a therapeutic agent for the palliation of metastatic bone pain. Copyright © 2006 by the Society of Nuclear Medicine, Inc., 金沢大学疾患モデル総合研究センター},
 pages = {122--127},
 title = {Therapeutic effects of a 186re-complex-conjugated bisphosphonate for the palliation of metastatic bone pain in an animal model},
 volume = {48},
 year = {2007}
}