Synthesis, metal complexation and biological evaluation of a novel semi-rigid bifunctional chelating agent for 99mTc labelling

Julien Le Gal (1) , Sandra Michaud (1) , Marie Gressier (1) , Yvon Coulais , Eric Benoist (1)

1 CIRIMAT - Centre interuniversitaire de recherche et d'ingenierie des matériaux

A novel bifunctional chelating agent bearing an aromatic ring has been synthesised and characterised. This ligand formed well-defined oxorhenium complexes. The analogous 99mTcO-complex was obtained in an excellent yield with high radiochemical purity (>95%). The biodistribution of the 99mTo-complex after intravenous injection studied in normal rats showed that the activity was excreted mainly via renal-urinary pathway indicating its use for labelling peptides with 99mTc.

Mots clés: Radiopharmaceuticals; Technetium-99m; Rhenium; Bifunctional chelating agent; Metallic complexes

Domaines: Matériaux; Chimie thérapeutique

Julien Le Gal, Sandra Michaud, Marie Gressier, Yvon Coulais, Eric Benoist. Synthesis, metal complexation and biological evaluation of a novel semi-rigid bifunctional chelating agent for 99mTc labelling. Bioorganic and Medicinal Chemistry, 2006, 14 (9), pp.2904-2909. ⟨10.1016/j.bmc.2005.12.005⟩. ⟨hal-03598118⟩