Biological Distribution of Chemical Analogs of Fatty Acids and Long Chain Hydrocarbons Containing a Strong Chelating Agent

The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaaeetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30min after intravenou...

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Veröffentlicht in:Journal of pharmaceutical sciences 1977-02, Vol.66 (2), p.225-228
Hauptverfasser: Karesh, Stephen M., Eckelman, William C., Reba, Richard C.
Format: Artikel
Sprache:eng
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Zusammenfassung:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaaeetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30min after intravenous administration of these 99mTc-labeled and 57Co-labeled derivatives was compared to the biological distribution of the parent compound, 3H-palmitic acid. The average myocardial uptake for these compounds was 0.04%/g, compared to 0.15%/g for palmitic acid. The heart to blood ratio at 30min reached a maximum of 3:1 for the best physiological analog of palmitic acid, compared to an average of 30:1 for palmitic acid. Although none of these analogs appears to be clinically useful, their production methods might be applicable to the synthesis of new compounds that might increase the specificity of radiopharmaceuticals.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600660223