title: A potential melanoma tracer: synthesis, radiolabeling, and biodistribution in mice of a new nitridotechnetium bis(aminothiol) derivative pharmacomodulated by a N-(diethylaminoethyl)benzamide.
abstract: Radioiodobenzamides are the best-known agents under study for the diagnosis of cutaneous melanoma and its metastases. We report the synthesis of a new BAT derivative radiopharmaceutical in which radioiodine is replaced by 99m-technetium. The cyclic intermediary methyl 4-[3-(4,4,7,7-tetramethyl-5,6-dithia-2, 9-diazacyclodecyl)-2-oxapropyl]benzoate (5) occurred in two different conformations identified by spectroscopic analysis. The final BAT ligand was radiolabeled using the nitridotechnetium core by a ligand-exchange reaction. Two different complexes were purified. After macroscopic 99-technetium synthesis, syn and anti isomers were identified. The global radiochemical yield was over 80%. The biodistribution of these two complexes was evaluated in mice bearing murine B16 melanoma. Extensive liver and kidney uptake was observed, but the benzamide tropism for the tumor was partially preserved.
authors.affiliation: INSERM Unité 484, rue Montalembert, BP 184, 63005 Clermont-Ferrand, France.
authors.forename: P
authors.initials: P
authors.lastname: Auzeloux
authors.forename: J
authors.initials: J
authors.lastname: Papon
authors.forename: E M
authors.initials: EM
authors.lastname: Azim
authors.forename: M
authors.initials: M
authors.lastname: Borel
authors.forename: R
authors.initials: R
authors.lastname: Pasqualini
authors.forename: A
authors.initials: A
authors.lastname: Veyre
authors.forename: J C
authors.initials: JC
authors.lastname: Madelmont
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D001812:Blood-Brain Barrier; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008546:Melanoma, Experimental / Q000378:metabolism*; D051379:Mice; D008810:Mice, Inbred C57BL; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D001549:Benzamides; D015609:Organotechnetium Compounds