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((E)-1-( STI)Iodo-1-penten-5-yl)triphenylphosphonium iodide: convenient preparation of a potentially useful myocardial perfusion agent

Journal Article · · J. Med. Chem.; (United States)
DOI:https://doi.org/10.1021/jm00374a007· OSTI ID:6233542
;

A rapid iodination method has been developed for the synthesis of the new STI-labeled phosphonium cation ((E)-1-iodo-1-penten-5-yl)triphenylphosphonium iodide by I treatment of the corresponding trans-vinylboronic acid. This new model myocardial perfusion agent is obtained after purification in 25-50% yield in <1 h. High myocardial uptake (5 min, 2.38% dose/g) with prolonged retention (3 h, 2.21% dose/g) was observed in rats. In addition, heart/blood ratios were high and continued to increase over a 1-day period (5 min, 17:1; 60 min, 23:1; 3 h, 27:1, 1 day, 158:1). In rats, the liver uptake was moderate (5 min, 1.40% dose/g; 60 min; 0.25% dose/g). Excellent myocardial images were obtained in a dog. 22 references, 1 figure, 2 tables.

Research Organization:
Oak Ridge National Lab., TN
DOE Contract Number:
AC05-84OR21400
OSTI ID:
6233542
Journal Information:
J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 27:8; ISSN JMCMA
Country of Publication:
United States
Language:
English

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Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMAL TISSUES
ANIMALS
AROMATICS
BETA DECAY RADIOISOTOPES
BODY
CARDIOVASCULAR SYSTEM
CHEMICAL REACTIONS
DATA
DIGESTIVE SYSTEM
DOGS
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
GLANDS
HALOGENATION
HEART
HOURS LIVING RADIOISOTOPES
IMAGES
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINATION
IODINE 123
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
LIVER
MAMMALS
MUSCLES
MYOCARDIUM
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
ORGANIC PHOSPHORUS COMPOUNDS
ORGANS
PERFUSED TISSUES
RADIOISOTOPES
RATS
RODENTS
TISSUES
TRACER TECHNIQUES
UPTAKE
VERTEBRATES