Synthesis and preliminary evaluation of carbon-11-meta-hydroxyephedrine: A false transmitter agent for heart neuronal imaging

Journal Article · Wed Aug 01 00:00:00 EDT 1990 · Journal of Nuclear Medicine; (USA)

OSTI ID:6528939

Rosenspire, K C; Haka, M S; Van Dort, M E; Jewett, D M; Gildersleeve, D L; Schwaiger, M; Wieland, D M ^[1]

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1. Univ. of Michigan Medical Center, Ann Arbor (USA)

Carbon-11-meta-hydroxyephedrine is a new radiotracer developed for mapping the sympathetic nerves of the heart. Carbon-11-meta-hydroxyephedrine is synthesized by direct N-methylation of metaraminol with ({sup 11}C)methyl iodide in dimethyl formamide/dimethyl sulfoxide and purified by semi-preparative reversed-phase HPLC. Total synthesis time is 45 min from end-of-bombardment. Carbon-11-meta-hydroxyephedrine is produced in 40%-50% corrected radiochemical yield with a specific activity of 900 Ci/mmol. Routine radiochemical and chemical purity are 95% and 98%, respectively. Biodistribution studies in rats show high myocardial uptake. Pretreatment with desipramine, a drug known to selectively block neuronal uptake, results in a 92% decrease in tracer accumulation in the myocardium. Metabolic studies in guinea pigs show less than 5% metabolites in heart tissue 30 min after intravenous injection suggesting that ({sup 11}C)meta-hydroxyephedrine is suitable for kinetic modeling. These preliminary results support this new tracer as a clinical agent for neuronal imaging of the heart.

• OSTI ID: 6528939
• Journal Information: Journal of Nuclear Medicine; (USA), Journal Name: Journal of Nuclear Medicine; (USA) Vol. 31:8; ISSN 0161-5505; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AUTONOMIC NERVOUS SYSTEM
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CARBON 11
CARBON ISOTOPES
CARDIOVASCULAR SYSTEM
CHEMICAL PREPARATION
CHEMICAL REACTIONS
CHROMATOGRAPHY
DISTRIBUTION
DRUGS
EVEN-ODD NUCLEI
GUINEA PIGS
HEART
IMAGE PROCESSING
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
METABOLISM
METHYLATION
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NUCLEI
ORGANS
PROCESSING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SEPARATION PROCESSES
SYNTHESIS
TISSUE DISTRIBUTION
VERTEBRATES