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Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for $$alpha$$ radionuclide therapy

小川 数馬*; 水野 覚瑛*; 鷲山 幸信*; 柴 和弘*; 高橋 成人*; 小阪 孝史*; 渡辺 茂樹; 篠原 厚*; 小谷 明*

Nuclear Medicine and Biology, 42(11), p.875 - 879, 2015/11

 被引用回数:21 パーセンタイル:70.63(Radiology, Nuclear Medicine & Medical Imaging)

Sigma receptors are overexpressed in a variety of human tumors, making them potential targets for radionuclide receptor therapy. We have previously synthesized and evaluated $$^{131}$$I-labeled (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-[$$^{131}$$I]pIV], which has a high affinity for sigma receptors. Therefore, (+)-[$$^{131}$$I]pIV significantly inhibited tumor cell proliferation in tumor-bearing mice. In the present study, we report the synthesis and the in vitro and in vivo characterization of (+)-[$$^{211}$$At]pAtV, an $$^{211}$$At-labeled sigma receptor ligand, that has potential use in $$alpha$$-radionuclide receptor therapy. The lipophilicity of (+)-[$$^{211}$$At]pAtV was similar to that of (+)-[$$^{125}$$I]-pIV. Uptake of DU-145, prostate cancer cell lines, and the biodistribution patterns in DU-145 tumor-bearing mice at 1 h post-injection were also similar between (+)-[$$^{211}$$At]pAtV and (+)-[$$^{125}$$I]-pIV. Namely, (+)-[$$^{211}$$At]pAtV demonstrated high uptake and retention in tumor via binding to sigma receptors.


Preparation and biological evaluation of 3-[$$^{76}$$Br]bromo-$$alpha$$-methyl-L-tyrosine, a novel tyrosine analog for positron emission tomography imaging of tumors

大島 康宏; 花岡 宏史*; 渡邉 茂樹; 須郷 由美; 渡辺 智; 富永 英之*; 織内 昇*; 遠藤 啓吾*; 石岡 典子

Nuclear Medicine and Biology, 38(6), p.857 - 865, 2011/08

 被引用回数:14 パーセンタイル:48.55(Radiology, Nuclear Medicine & Medical Imaging)

3-[$$^{18}$$F]fluoro-$$alpha$$-methyl-L-tyrosine ([$$^{18}$$F]FAMT) is a useful amino acid tracer for positron emission tomography (PET) imaging of malignant tumors. FAMT analogs labeled with $$^{76}$$Br, a positron emitter with a long half-life ($$t$$$$_{1/2}$$=16.1 h), could be widely used as tracers for tumor imaging. In this study, 3-[$$^{76}$$Br]bromo-$$alpha$$-methyl-L-tyrosine ([$$^{76}$$Br]BAMT) was designed, and its usefulness was evaluated as a novel PET tracer for imaging malignant tumors. In this study, both [$$^{76}$$Br]BAMT and [$$^{77}$$Br]BAMT were prepared. [$$^{77}$$Br]BAMT was stable in vitro, but was catabolized after administration in mice. Cellular accumulation and retention of [$$^{77}$$Br]BAMT using LS180 colon adenocarcinoma cells were significantly higher than those of [$$^{18}$$F]FAMT. In biodistribution studies using LS180 tumor-bearing mice, the tumor accumulation of [$$^{77}$$Br]BAMT was higher than that of [$$^{18}$$F]FAMT. However, some level of debromination was seen, and this debromination caused more retention of radioactivity in the blood and organs than was seen with [$$^{18}$$F]FAMT. PET imaging with [$$^{76}$$Br]BAMT enabled clear visualization of the tumor. In conclusion, although an improvement in stability is still needed, $$^{76}$$Br-labeled FAMT analogs could potentially serve as PET tracers for the imaging of malignant tumors.


Chelating ion-exchange methods for the preparation of no-carrier-added $$^{64}$$Cu

渡邉 茂樹; 渡辺 智; Liang, J. X.; 花岡 宏史*; 遠藤 啓吾*; 石岡 典子

Nuclear Medicine and Biology, 36(6), p.587 - 590, 2009/09

 被引用回数:6 パーセンタイル:23.29(Radiology, Nuclear Medicine & Medical Imaging)

We have developed a production method for no-carrier-added copper-64 ($$^{64}$$Cu) by using chelating resin bearing iminodiacetic acid groups. We optimized the condition for selective separation of radioactive copper by using chelating resin from nickel and cobalt. Radioactive copper was separated completely using 0.1 M and 2 M HCl solution. In production of no-carrier-added $$^{64}$$Cu, the average 87% of $$^{64}$$Cu was isolated from the $$^{64}$$NiO target with high radionuclide purity ($$>$$ 99%). In order to investigate the quality of the obtained $$^{64}$$Cu, metallic impurities contained in the $$^{64}$$Cu solution were analyzed by means of inductive coupled-plasma mass spectroscopy (ICP-MS) and optical emission spectroscopy (ICP-OES). It was observed that extremely low amounts of metal ion were contained in the $$^{64}$$Cu. The $$^{64}$$Cu solution showed high specific activity (average: 594.7 GBq/$$mu$$mol). In this study, the chelating exchange method yielded high-quality of $$^{64}$$Cu sufficient for the synthesis of $$^{64}$$Cu-labeled radiopharmaceuticals and medical applications.


Assessment of $$^{186}$$Re chelate-conjugated bisphosphonate for the development of new radiopharmaceuticals for bones

上原 知也*; Jin, Z. L.*; 小川 数馬*; 秋澤 宏行*; 橋本 和幸; 中山 守雄*; 荒野 泰*

Nuclear Medicine and Biology, 34(1), p.79 - 87, 2007/01

 被引用回数:23 パーセンタイル:57.57(Radiology, Nuclear Medicine & Medical Imaging)



Rhemium-186-monoaminemonoamidedithiol-conjugated bisphosphonate derivatives for bone pain palliation

小川 数馬*; 向 高弘*; 荒野 泰*; 大高 章*; 上田 真史*; 上原 知也*; 間賀田 泰寛*; 橋本 和幸; 佐治 英郎*

Nuclear Medicine and Biology, 33(4), p.513 - 520, 2006/05

 被引用回数:54 パーセンタイル:80.81(Radiology, Nuclear Medicine & Medical Imaging)



In vivo recognition of Cyclopentadienyltricarbonylrhenium (CpTR) derivatives

上原 知也*; 小池 美穂*; 中田 英夫*; 宮本 重彦*; 本石 章司; 橋本 和幸; 奥 直人*; 中山 守雄*; 荒野 泰*

Nuclear Medicine and Biology, 30(3), p.327 - 334, 2003/04

 被引用回数:20 パーセンタイル:50.74(Radiology, Nuclear Medicine & Medical Imaging)


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