Nuclear medicine progress report for quarter ending September 30, 1984
The preparation and animal testing of a new radio-iodinated p-iodophenylamine-linked dihydropyridine system is described. The model agent, 1-methyl-3-(N-(..beta..-(4-(/sup 125/I)iodophenyl)ethyl)carbamoyl)-1,4-dihydropyridine, was prepared by coupling 4-(/sup 125/I)iodoaniline with the methiodide salt succinimidyl ester of nicotinic acid followed by dithionite reduction to the lipid soluble product. The dihydropyridine agent showed good brain uptake in rats (5 min, 1.14% injected dose/gm; 60 min, 1.12% dose/gm) and good brain to blood ratios (5 min 3.9:1, 60 min, 3.5:1). In contrast the quaternary ammonium compound, prior to reduction, showed only moderate brain uptake (5 min, 0.63; 60 min, 0.46) and low brain to blood ratios (5 min, 0.05; 60 min, 0.06). Also described is further investigation of the effects of fasting on the relative myocardial retention of straight-chain iodovinyl fatty acids. 18-(/sup 125/)Iodo-17-octadecenoic acid showed good retention in unfasted rats. Studies have now been reported for fasted rats where this agent showed rapid myocardial wash-out. In fasted rats, approx. 70% wash-out at 30 min, and in unfasted rats, approx. 15% wash-out at 30 min was observed. During this period several shipments were made to Medical Cooperative investigators including three samples of /sup 191/Os-potassium osmate (Children's Hospital, Boston, and the University of Liege, Belgium) and 15-(p-(/sup 131/I)iodophenyl)-3-R,S-methylpentadecanoic acid (University of Massachusetts and Brookhaven National Laboratory).
- Research Organization:
- Oak Ridge National Lab., TN (USA)
- DOE Contract Number:
- AC05-84OR21400
- OSTI ID:
- 6241427
- Report Number(s):
- ORNL/TM-9394; ON: DE85004766
- Country of Publication:
- United States
- Language:
- English
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Nuclear Medicine progress report for quarter ending March 31, 1986
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Related Subjects
CARBOXYLIC ACIDS
RETENTION
NUCLEAR MEDICINE
RESEARCH PROGRAMS
PYRIDINES
UPTAKE
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
AMINES
BRAIN
IODINE 125
IODINE 131
MYOCARDIUM
OSMIUM 191
RATS
ANIMALS
AZINES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CARDIOVASCULAR SYSTEM
CENTRAL NERVOUS SYSTEM
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EVEN-ODD NUCLEI
HEART
HEAVY NUCLEI
HETEROCYCLIC COMPOUNDS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MEDICINE
MINUTES LIVING RADIOISOTOPES
MUSCLES
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
OSMIUM ISOTOPES
RADIOISOTOPES
RODENTS
SYNTHESIS
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics