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- W57884612 abstract "1233 Objectives: This study was aimed to develop 68Ga-N6-carboxymethyl-N3,N9-bis[[2,2-bis(phosphono)-2-hydroxy]ethyl]-3,6,9-triazaundecanedioic acid (DTPA-BP) for the detection of bone metastases by PET. Methods: DTPA-BP was synthesized by reacting tris(trimethylsilyl)phosphite with DTPA anhydride in THF. After solvent evaporation and methanolic hydrolysis, the product was purified from a sephadex-packed column. 68GaCL3 was eluted from a 68Ge/68Ga generator (Eckert & Ziegler, Berlin, Germany). DTPA-BP was labeled with 68Ga(III) using acetate buffer (PH 5). First, the biodistribution of 68Ga-DTPA-BP and 99mTc-MDP (reference standard) was studied in normal female F-344 rats at 0.5-2hrs by tissue sampling and gamma spectrometry. Then, the osteolytic bone metastases model was created by injecting PC-3 human prostate cancer cells into the left tibia of male SCID mice. PET-imaging of 68Ga-DTPA and 68Ga-DTPA-BP was performed in a microPET R4 (Siemens) at 0.5-2h post iv injection (150uCi/mouse). The specific activity of 68Ga-DTPA-BP was 75 Ci/mol. Results: The total synthesis yield of DTPA-BP was 10-15%. To achieve 80-90% radiochemical purity of 68Ga -DTPA-BP, the physical amount DTPA-BP was >1mM. The biodistribution of 68Ga-DTPA-BP in normal rats at 0.5-2 hrs post-injection revealed increased bone-to-blood (3.4+ 0.80 to 5.3+0.24) and bone-to-muscle (13.6+3.46 to 21.8+11.50) ratios. The uptake of 68Ga-DTPA-BP and 99mTc-MDP in bones at 0.5 hr was 2.2+0.45 and 3.9+0.31 %ID/g, respectively. PET with 68Ga-DTPA-BP was able to detect osteolytic bone metastases, but not with 68Ga-DTPA. Conclusions: 68Ga-DTPA-BP can detect osteolytic bone metastases. Further characterization of this novel tracer in different tumor models is underway." @default.
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- W57884612 date "2008-05-01" @default.
- W57884612 modified "2023-09-27" @default.
- W57884612 title "Synthesis, biodistribution, and imaging of 68Ga-DTPA-BP in normal and bone metastasis rodent models" @default.
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