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Synthesis and evaluation of potential tumor localizing radiopharmaceuticals: Technetium‐99m iminodiacetic acid derivatives of sulfanilamides
Author(s) -
Hunt F. C.,
Maddalena D. J.,
McLaren A. B.,
Wilson J. G.
Publication year - 1982
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580190206
Subject(s) - iminodiacetic acid , chemistry , biodistribution , chelation , technetium 99m , technetium , lipophilicity , radiochemistry , nuclear chemistry , stereochemistry , organic chemistry , biochemistry , in vitro , nuclear medicine , scintigraphy , medicine
To exploit the tissue affinity of compounds for radiopharmaceutical purposes, attachment of chelating groups is usually necessary to facilitate technetium‐99m binding and transport. The chelating group, iminodiacetic acid, previously used to modify lidocaine for hepatobiliary radiopharmaceuticals, was attached to several antibiotic sulfanilamides known to concentrate in certain transplanted animal tumors. These iminodiacetic acid derivatives were labelled with technetium‐99m by the stannous chloride reduction method. Biodistribution of the 99m Tc labelled compounds in tumor bearing rats revealed no specific concentration in the tumors and localization mainly in the excretory organs. The results indicate that, as in the case of lidocaine, conversion of the sulfanilamides into iminodiacetic acid derivatives and chelation with technetium leads to an altered biodistribution and loss of biological specificity.