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Uehara, Tomoya*; Jin, Z. L.*; Ogawa, Kazuma*; Akizawa, Hiromichi*; Hashimoto, Kazuyuki; Nakayama, Morio*; Arano, Yasushi*
Nuclear Medicine and Biology, 34(1), p.79 - 87, 2007/01
Times Cited Count:24 Percentile:56.53(Radiology, Nuclear Medicine & Medical Imaging)In this study, a key factor affecting the pharmacokinetics of a chelate-conjugated BP was investigated to estimate the validity and the applicability of molecular design. Chemically inert and well-characterized [Re]CpTR-Gly was conjugated with 3-amino-1-hydroxypropylidene-1,1-bisphosphonate and purified by HPLC to prepare [Re]CpTR-Gly-APD. Plasma stability, plasma protein binding, hydroxyapatite (HA) binding and the pharmacokinetics of [Re]CpTR-Gly-APD were compared with those of Re 1-hydroxyethylidene-1,1-diphosphonate (HEDP). The HPLC-purified [Re]CpTR-Gly-APD showed higher plasma stability, higher HA binding, higher bone accumulation and lower plasma protein binding than did Re -HEDP. Although Re -HEDP possessed HA binding and bone accumulation similar to those of [Re]CpTR-Gly-APD, the specific activity of Re -labeled BPs was found to play a crucial role in bone accumulation and blood clearance. Thus, the molecular design of chelate-conjugated BP would be useful for the development of bone-seeking radiopharmaceuticals with a variety of radionuclides by selecting chelating molecules that provide high specific activities.
Uehara, Tomoya*; Koike, Miho*; Nakata, Hideo*; Miyamoto, Shigehiko*; Motoishi, Shoji; Hashimoto, Kazuyuki; Oku, Naoto*; Nakayama, Morio*; Arano, Yasushi*
Nuclear Medicine and Biology, 30(3), p.327 - 334, 2003/04
Times Cited Count:20 Percentile:50.08(Radiology, Nuclear Medicine & Medical Imaging)no abstracts in English