Synthesis and biological evaluation of 17-(/sup 131/I)iodo-9-telluraheptadecanoic acid, a potential imaging agent

Journal Article · Tue Jun 01 00:00:00 EDT 1982 · J. Med. Chem.; (United States)

DOI:https://doi.org/10.1021/jm00348a001· OSTI ID:6710647

Goodman, M M; Knapp, Jr, F F; Callahan, A P; Ferren, L A

A method has been developed for the preparation of terminal halogenated tellurium fatty acids (X-R-Te-R'-COOH). The synthesis and physical properties of 17-bromo- and 17-iodo-9-telluraheptadecanoic acid (17-iodo-9-THDA) are described. The radiohalogenated agents are of interest as a result of their expected pronounced and prolonged heart uptake and potential use for evaluation of regional myocardial fatty acid metabolism. Evaluation in rats indicates that the myocardial uptake of 17-(/sup 131/I)iodo-9-telluraheptadecanoic acid (17-(/sup 131/I)iodo-9-THDA) is accompanied by significant in vivo deiodination. A comparison of the heart uptake and deiodination of 17-(/sup 131/I)iodo-9-THDA and 16-(/sup 131/I)iodopalmitic acid has demonstrated a close similarity in blood levels of radioactivity and thyroid uptake of radioiodide after administration of these agents to rats. These data suggest that the mechanism of deiodination of terminal radioiodinated alkanoic acids primarily results from direct cleavage of the carbon-iodine bond and not from loss of radioiodine from the final catabolite.

• Research Organization: Nuclear Medicine Technology Group, Health and Safety Research Division, Oak Ridge National Laboratory, Tennessee
• OSTI ID: 6710647
• Journal Information: J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 25:6; ISSN JMCMA
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL PATHWAYS
BODY
CARBOXYLIC ACIDS
CARDIOVASCULAR SYSTEM
CHEMICAL PREPARATION
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DIAGNOSTIC USES
DRUGS
HEART
INTERMEDIATE MASS NUCLEI
IODINE 131
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
METABOLISM
MUSCLES
MYOCARDIUM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SCINTISCANNING
SYNTHESIS
USES
VERTEBRATES