title: Synthesis and evaluation of new iodine-125 radiopharmaceuticals as potential tracers for malignant melanoma.
abstract: The synthesis, labeling, and biodistribution of four 125I radiopharmaceuticals designed to localize in melanoma were tested. Uptake in tumors was demonstrated by autoradiography of whole-body sections and quantitated by measurement of radioactivity of selected tissues and tumors using melanoma-bearing mice. N-(2-diethylaminoethyl)-4-iodobenzamide was selected for its highest melanoma uptake: 60 min after IV injection of 6.5% and 4% ID/g, respectively for murine B16 and human melanotic melanoma. Tumor uptake showed the highest values of all analyzed tissues from 6 to 24 hr after injection. High uptake in melanotic tumor tissue with relatively low uptake in blood, muscle, brain, lung, and liver tissue resulted in high tumor/nontumor ratios (at 24 hr for B16, tumor/blood = 37, tumor/brain = 147, tumor/muscle = 95). This agent was compared with iodoamphetamine. Scintigraphic images of the tumor confirmed that external detection of melanoma is possible with this new radiopharmaceutical.
authors.affiliation: INSERM U 71, B.P. 184, Clermont-Ferrand, France.
authors.forename: J M
authors.initials: JM
authors.lastname: Michelot
authors.forename: M F
authors.initials: MF
authors.lastname: Moreau
authors.forename: P G
authors.initials: PG
authors.lastname: Labarre
authors.forename: J C
authors.initials: JC
authors.lastname: Madelmont
authors.forename: A J
authors.initials: AJ
authors.lastname: Veyre
authors.forename: J M
authors.initials: JM
authors.lastname: Papon
authors.forename: D F
authors.initials: DF
authors.lastname: Parry
authors.forename: J F
authors.initials: JF
authors.lastname: Bonafous
authors.forename: J Y
authors.initials: JY
authors.lastname: Boire
authors.forename: G G
authors.initials: GG
authors.lastname: Desplanches
mesh_terms: D000662:Amphetamines; D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis; D007457:Iodine Radioisotopes; D020367:Iofetamine; D008297:Male; D008546:Melanoma, Experimental / Q000000981:diagnostic imaging*; D051379:Mice; D008815:Mice, Inbred Strains; D011877:Radionuclide Imaging; D014018:Tissue Distribution
chemical_list: D000662:Amphetamines; D001549:Benzamides; D007457:Iodine Radioisotopes; C066918:N-(2-(diethylamino)ethyl)-4-iodobenzamide; D020367:Iofetamine