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Synthesis, characterization and comparative biodistribution study of a new series of p-iodine-125 benzamides as potential melanoma imaging agents.

Authors
  • Moins, N
  • Papon, J
  • Seguin, H
  • Gardette, D
  • Moreau, M F
  • Labarre, P
  • Bayle, M
  • Michelot, J
  • Gramain, J C
  • Madelmont, J C
  • Veyre, A
Type
Published Article
Journal
Nuclear Medicine and Biology
Publisher
Elsevier
Publication Date
Oct 01, 2001
Volume
28
Issue
7
Pages
799–808
Identifiers
PMID: 11578901
Source
Medline
License
Unknown

Abstract

Iodobenzamides are reported to possess some affinity for melanoma. In order to identify the compound having the most appropriate pharmacokinetic properties as a potential melanoma imaging agent, thirteen new [125I]radioiodobenzamides with a butylene amide-amine spacer and various substituents on the terminal amino group were investigated. Their synthesis, radioiodination and biodistribution in B16 melanoma bearing C57BL6 mice are described and compared to [125I] labeled N-(2-diethylaminoethyl)-4-iodobenzamide ([125I]BZA), our reference compound. Changes in the terminal amino constituents induced modifications of lipophilicity, tumor uptake and organ distribution. The dimethylaminobutyl iodobenzamide appeared to be the most promising radiopharmaceutical imaging agent for the detection of melanoma and its metastases.

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