Design, synthesis and evaluation of redox radiopharmaceuticals: a potential new approach for the development of brain imaging agents
Conference
·
OSTI ID:5887031
The fabrication and complete evaluation are described of a dihydropyridine in equilibrium pyridinium salt type redox system for the delivery of radioiodinated agents to the brain. The pivotal intermediate, N-succinimidyl (1-methylpyridinium iodide)-3-carboxylate was prepared by condensation of nicotinic acid and N-hydroxysuccinimide in the presence of dicyclohexylcarbodimide, followed by quaternization of III with methyl iodide. Tissue distribution studies of /sup 125/I-labeled 4-iodoaniline and the redox agents were performed in rats. (/sup 125/I)Iodoaniline initially showed moderate (0.58% dose/gm) brain uptake with subsequent release of the radioactivity from the brain. (/sup 125/I)Iodoaniline, when coupled to a dihydropyridine carrier showed higher uptake and retention in the brain. The (/sup 125/I)iodophenylethyl analogue showed uptake and retention in the brain to be very similar. Apparently the lipophilic agents cross the blood-brain barrier and are oxidized (quaternized) within the brain. The blood-brain barrier then prevents their release resulting in high uptake and retention in the brain and high brain:blood ratios. 11 refs., 3 figs.
- Research Organization:
- Oak Ridge National Lab., TN (USA)
- DOE Contract Number:
- AC05-84OR21400
- OSTI ID:
- 5887031
- Report Number(s):
- CONF-8606111-2; ON: DE86009462
- Country of Publication:
- United States
- Language:
- English
Similar Records
Nuclear medicine progress report for quarter ending September 30, 1984
Evaluation of the brain-specific delivery of radioiodinated (iodophenyl)alkyl-substituted amines coupled to a dihydropyridine carrier
Nuclear medicine progress report for quarter ending March 31, 1984
Technical Report
·
Fri Nov 30 23:00:00 EST 1984
·
OSTI ID:6241427
Evaluation of the brain-specific delivery of radioiodinated (iodophenyl)alkyl-substituted amines coupled to a dihydropyridine carrier
Journal Article
·
Thu Oct 31 23:00:00 EST 1985
· J. Med. Chem.; (United States)
·
OSTI ID:5721893
Nuclear medicine progress report for quarter ending March 31, 1984
Technical Report
·
Wed Aug 01 00:00:00 EDT 1984
·
OSTI ID:6595807
Related Subjects
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
400303 -- Organic Chemistry-- Isotope Exchange & Isotope Separation-- (-1987)
550501* -- Metabolism-- Tracer Techniques
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
BETA DECAY RADIOISOTOPES
BLOOD-BRAIN BARRIER
CHEMICAL PREPARATION
DATA
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLING
MAMMALS
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
RADIOISOTOPES
RATS
RODENTS
SYNTHESIS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
VERTEBRATES
400303 -- Organic Chemistry-- Isotope Exchange & Isotope Separation-- (-1987)
550501* -- Metabolism-- Tracer Techniques
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMALS
BETA DECAY RADIOISOTOPES
BLOOD-BRAIN BARRIER
CHEMICAL PREPARATION
DATA
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
INFORMATION
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLING
MAMMALS
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC IODINE COMPOUNDS
RADIOISOTOPES
RATS
RODENTS
SYNTHESIS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
VERTEBRATES