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KMID : 1145520150010010031
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Journal of Radiopharmaceuticals and Molecular Probes
2015 Volume.1 No. 1 p.31 ~ p.37
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Preparation and characterization of Ga-68-deferoxamine to test the feasibility as a bifunctional chelating agent or a renal imaging radiopharmaceutical
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Kim Young-Ju
Lee Yun-Sang
Jeong Jae-Min
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Abstract
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Chelating agents 1,4,7-triazacyclononanetriacetic acid (NOTA), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and 30-amino-3,14,25-trihydroxy-3,9,14,20,25-penta-azatriacontane-2,10,13, 21,24-pentaone (desferrioxamine, DFO) were labeled with 68Ga and tested in vitro properties to check the feasibility of using DFO as a bifunctional chelating agent or renal imaging agent. The chelating agents of concentration 2 μM were labeled with 68Ga in 0.1 M HCl at pH 1.7-10.3 at room temperature and 80℃ and the optimal pH for labeling each chelating agent was found. And then, the chelating agents were labeled with 68Ga in various concentration of chelating agents at optimal pH. The labeled chelating agents were subject to stability test in human serum and to binding studies to human red blood cell (RBC) and plasma protein. The optimal pH’s of NOTA, DOTA and DFO for 68Ga-labeling were 4.4, 3.6 and 5.6, respectively. DFO (10 μM) showed high labeling efficiency (>97%) at pH 5.6. All the labeled chelating agents showed high stability in human serum. 68Ga-DFO showed low RBC binding but significant amount was bound to plasma protein. The results demonstrated that 68Ga-DFO can be used as a bifunctional chelating agent but not as a renal imaging agent.
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KEYWORD
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68Ga, Deferoxamine, NOTA, DOTA, Labeling efficiency
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