864462-59-9Relevant articles and documents
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma
Pham, Tien Q.,Greguric, Ivan,Liu, Xiang,Berghofer, Paula,Ballantyne, Patrice,Chapman, Janette,Mattner, Filomena,Dikic, Branko,Jackson, Timothy,Loc'h, Christian,Katsifis, Andrew
, p. 3561 - 3572 (2008/02/09)
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 σ1-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.
RADIOHALOGENATED BENZAMIDE DERIVATIVES AND THEIR USE IN TUMOR DIAGNOSIS AND TUMOR THERAPY
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Page/Page column 36-37, (2008/06/13)
This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.