Synthesis and evaluation of radioiodinated terminal-substituted 5-iodo-(2-thienyl) fatty acids as new myocardial imaging agents
In order to evaluate the stability of radioiodide attached to the 5 position of thiophenes substituted at the 2-position with tissue-specific groups as new radiopharmaceuticals, two (/sup 125/I)iodothienyl-substituted long-chain fatty acids have been prepared and evaluated in rats. Radioiodide was introduced into the 5 position of 17-(2-thienyl)heptadecanoic acid and 13-(2-thienyl)tridecanoic acid by K-/sup 125/I treatment of their corresponding 5-(bis-(trifluoroacetoxyl))thallium derivatives. Tissue distribution studies in rats with 17-(5-(/sup 125/I)iodo(2-thienyl)heptadecanoic acid shows significant heart uptake and prolonged retention accompanied by in vivo deiodination and moderate blood levels. A comparison of the heart uptake of the 17 carbon fatty acid with a 13 carbon analogue, 13-(5-(/sup 135/I)iodo(2-thienyl))tridecanoic acid, demonstrated a significantly greater myocardial uptake for the 17 carbon fatty acid than the 13 carbon analogue. These results suggest that the 5-iodothienyl moiety substituted at the terminal position of long chain fatty acids does not interfere with myocardial uptake and that such compounds may be of value as a new class of myocardial imaging agents. 17 references, 2 tables.
- Research Organization:
- Oak Ridge National Lab., TN
- DOE Contract Number:
- AC05-84OR21400
- OSTI ID:
- 5965242
- Journal Information:
- J. Heterocycl. Chem.; (United States), Journal Name: J. Heterocycl. Chem.; (United States) Vol. 21; ISSN JHTCA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Synthesis and evaluation of radioiodinated (E)-18-iodo-17-octadecenoic acid as a model iodoalkenyl fatty acid for myocardial imaging
New myocardial imaging agents: stabilization of radioiodine as a terminal vinyl iodide moiety on tellurium fatty acids
Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
CARBOXYLIC ACIDS
CARDIOVASCULAR SYSTEM
COUNTING TECHNIQUES
DATA
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EVALUATION
EXPERIMENTAL DATA
HEART
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MEDICINE
MUSCLES
MYOCARDIUM
NUCLEAR MEDICINE
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
VERTEBRATES