Synthesis and Evaluation of Novel Radioiodinated Benzamides for Malignant Melanoma
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- 作者：Tien Q. Pham ; Ivan Greguric ; Xiang Liu ; Paula Berghofer ; Patrice Ballantyne ; Janette Chapman ; Filomena Mattner ; Branko Dikic ; Timothy Jackson ; Christian Loc'h ; Andrew Katsifis
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：July 26, 2007
- 年：2007
- 卷：50
- 期：15
- 页码：3561 - 3572
- 全文大小：201K
- 年卷期：v.50,no.15(July 26, 2007)
- ISSN：1520-4804
文摘
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 amaximum of 9-12 %ID/g at 6 h. Standardized uptake values of [123I]14d were higher than 100 between 24and 72 h after injection. In haloperidol treated animals, the tumor uptake of [123I]14d was not significantlydifferent to controls, while significant reduction of [123I]25 uptake was observed, supporting that [123I]14duptake relates to melanin interaction, whereas part of the mechanism of [123I]25 uptake is related to its
1-receptor affinity. Benzamides 14d and 25, which display rapid and high tumor uptake, appear to bepromising imaging agents for melanoma detection, while 14d, which displays a long lasting and highmelanoma/nontarget ratio, is more suitable for evaluation as a potential radiotherapeutic.
1-receptor affinity. Benzamides 14d and 25, which display rapid and high tumor uptake, appear to bepromising imaging agents for melanoma detection, while 14d, which displays a long lasting and highmelanoma/nontarget ratio, is more suitable for evaluation as a potential radiotherapeutic.