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Acyclic Chelate with Ideal Properties for 68Ga PET Imaging Agent Elaboration.

TitleAcyclic Chelate with Ideal Properties for 68Ga PET Imaging Agent Elaboration.
Publication TypeJournal Article
Year of Publication2010
AuthorsBoros, E, Ferreira, CL, Cawthray, JF, Price, EW, Patrick, BO, Wester, DW, Adam, MJ, Orvig, C
JournalJournal of the American Chemical Society
Volume132
Pagination15726 - 15733
Date Published2010///
ISBN Number0002-7863
KeywordsPET imaging agent synthesis acyclic gallium isotope diagnosis
Abstract

We have investigated novel bifunctional chelate alternatives to the aminocarboxylate macrocycles NOTA (N3O3) or DOTA (N4O4) for application of radioisotopes of Ga to diagnostic nuclear medicine and have found that the linear N4O2 chelate H2dedpa coordinates 67Ga quant. to form [67Ga(dedpa)]+ after 10 min at RT. Concn.-dependent coordination to H2dedpa of either 68Ga or 67Ga showed quant. conversion to the desired products with ligand concns. as low as 10-7 M. With 68Ga, specific activities as high as 9.8 mCi nmol-1 were obtained without purifn. In a 2 h competition expt. against human apo-transferrin, [67Ga(dedpa)]+ showed no decompn. Two bifunctional versions of H2dedpa are also described, and these both coordinate to 67Ga at RT within 10 min. Complete syntheses, characterizations, labeling studies, and biodistribution profiles of the 67Ga complexes are presented for the new platform chelates. The stability of these platform chelates is higher than that of DOTA. [on SciFinder(R)]