Modification of lypophilic groups and replacement of phosphorus by arsenic to study the effect on myocardial specificity of radioiodinated phosphonium cations
Conference
·
· J. Nucl. Med.; (United States)
OSTI ID:6590991
The organic cation, (E-1-iodo-1-penten-5-yl)triphenylphosphonium iodide (I), shows attractive myocardial uptake and retention in rats and dogs. The effect of modification of lypophilic groups attached to phosphorus and replacement of phosphorus by arsenic on myocardial specificity and retention of radioiodinated cations has now been evaluated. Triphenylarsonium (II, M=As), dicyclohexylphenylphosphonium (III, M=P) and dimethyl-n-octylphosphonium (IV, M=P) cations ((R/sub 3/M/sup +/-(CH/sub 2/)/sub 3/-CH=CH*I)I/sup -/) attached to the E-1-(/sup 125/I)iodo-1-pentenyl group were prepared via NaI-chloramine T iodination of the corresponding vinylboronic acid cation substrates. Compounds I-IV and the respective precursors were analyzed (TLC, NMR, and CandH) and /sup 125/I analogs I-IV were evaluated in rats (5/group). All four agents showed good uptake and retention demonstrating that these structural alterations do not greatly affect the myocardial specificity of these interesting new agents.
- Research Organization:
- Nuclear Medicine Group, Oak Ridge National Lab., Oak Ridge, TN
- DOE Contract Number:
- W-7405-ENG-26
- OSTI ID:
- 6590991
- Report Number(s):
- CONF-840619-
- Conference Information:
- Journal Name: J. Nucl. Med.; (United States) Journal Volume: 25:5
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550501* -- Metabolism-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINES
AMMONIUM COMPOUNDS
ANIMALS
ARSENIC COMPOUNDS
BIOCHEMISTRY
BODY
CARDIOVASCULAR SYSTEM
CHEMICAL PREPARATION
CHEMISTRY
DISTRIBUTION
DOGS
DRUGS
EVALUATION
FUNCTIONS
HEART
HYDROGEN COMPOUNDS
INORGANIC ACIDS
LABELLED COMPOUNDS
MAMMALS
METABOLISM
MUSCLES
MYOCARDIUM
ORGANIC ARSENIC COMPOUNDS
ORGANIC COMPOUNDS
ORGANS
PHOSPHORIC ACID
QUATERNARY COMPOUNDS
RADIOPHARMACEUTICALS
RATS
RETENTION FUNCTIONS
RODENTS
STRUCTURE-ACTIVITY RELATIONSHIPS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
AMINES
AMMONIUM COMPOUNDS
ANIMALS
ARSENIC COMPOUNDS
BIOCHEMISTRY
BODY
CARDIOVASCULAR SYSTEM
CHEMICAL PREPARATION
CHEMISTRY
DISTRIBUTION
DOGS
DRUGS
EVALUATION
FUNCTIONS
HEART
HYDROGEN COMPOUNDS
INORGANIC ACIDS
LABELLED COMPOUNDS
MAMMALS
METABOLISM
MUSCLES
MYOCARDIUM
ORGANIC ARSENIC COMPOUNDS
ORGANIC COMPOUNDS
ORGANS
PHOSPHORIC ACID
QUATERNARY COMPOUNDS
RADIOPHARMACEUTICALS
RATS
RETENTION FUNCTIONS
RODENTS
STRUCTURE-ACTIVITY RELATIONSHIPS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
VERTEBRATES