68Ga-Labeling of RGD peptides and biodistribution

International Journal of Clinical and Experimental Medicine

Elisabeth Blom¹  Sergio Estrada¹  Manoj Nair¹  Chenmin Ding¹  Taj Muhammad¹  Håkan Hall¹  Irina Velikyan¹  Bengt Långström¹ 

关键词: 68Ga;    RGD;    biodistribution;   

DOI  :  

学科分类：医学（综合）

来源: e-Century Publishing Corporation

【 摘 要 】

Several peptides comprising Arg-Gly-Asp (RGD) domain and macrocyclic chelator were labeled with ⁶⁸Ga for the imaging of angiogenesis. The analogues varied in peptide constitution, linker and chelator type. The labeling efficiency did not vary with the peptide constitution and linker type, but depended on the chelator type. Four of the compounds containing 2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (DOTA) chelator were labeled at 90 ± 5°C using conventional or microwave heating reaching 90% of ⁶⁸Ga incorporation after 5 and 2 min respectively, when the concentration of the precursor was 2.5 μM. The compound having 2,2',2''-(1,4,7-triazonane-1,4,7-triyl)triacetic acid (NOTA) as the chelator could be labeled at room temperature within 5 min using 2.5 μM peptide precursor. Two of the compounds contained a poly (ethylene glycol) (PEG) linker to the chelator. The biodistribution of the analogues was studied in male rats.

【 授权许可】

Unknown