Document Report Card

ID: ALA1146219

Journal: J Med Chem

Title: Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.

Authors: Pham TQ, Greguric I, Liu X, Berghofer P, Ballantyne P, Chapman J, Mattner F, Dikic B, Jackson T, Loc'h C, Katsifis A.

Abstract: The imaging potential of a series of [123I]benzamides was studied in mice bearing B16F0 melanoma tumors. Compound [123I]25 exhibited tumor uptake >8 %ID/g at 1 h, while that of [123I]14d and [123I]25 reached a maximum of 9-12 %ID/g at 6 h. Standardized uptake values of [123I]14d were higher than 100 between 24 and 72 h after injection. In haloperidol treated animals, the tumor uptake of [123I]14d was not significantly different to controls, while significant reduction of [123I]25 uptake was observed, supporting that [123I]14d uptake relates to melanin interaction, whereas part of the mechanism of [123I]25 uptake is related to its sigma 1-receptor affinity. Benzamides 14d and 25, which display rapid and high tumor uptake, appear to be promising imaging agents for melanoma detection, while 14d, which displays a long lasting and high melanoma/nontarget ratio, is more suitable for evaluation as a potential radiotherapeutic.

CiteXplore: 17602544

DOI: 10.1021/jm0701627