Abstract
(1R,2S)-4-[18F]fluorometaraminol (4-[18F]FMR), a tracer for cardiac sympathetic innervation, was synthesized by electrophilic aromatic substitution. A trimethylstannyl precursor, protected with tert-butoxycarbonyl protecting groups, was radiofluorinated with high specific radioactivity [18F]F2. Specific radioactivity of 4-[18F]FMR, in average 11.8 +/-3.3 GBq/micromol, was improved 40-800-fold in comparison to the previous electrophilic fluorinations. The biodistribution of 4-[18F]FMR in rat was in accordance with the known distribution of sympathetic innervation. 4-[18F]FMR showed no metabolic degradation in left ventricle of rat heart, where the uptake was high, rapid and specific.
MeSH terms
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Animals
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Biotransformation
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Body Burden
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Electrochemistry / methods
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Heart Ventricles / diagnostic imaging*
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Heart Ventricles / innervation
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Heart Ventricles / metabolism*
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Isotope Labeling / methods
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Male
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Metaraminol / analogs & derivatives*
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Metaraminol / chemical synthesis
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Metaraminol / pharmacokinetics*
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Norepinephrine / metabolism*
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Organ Specificity
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Radiation Dosage
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Rats, Sprague-Dawley
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Sympathetic Nervous System / diagnostic imaging*
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Sympathetic Nervous System / metabolism*
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Tissue Distribution
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Tomography, Emission-Computed / methods
Substances
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4-fluorometaraminol
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Radiopharmaceuticals
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Metaraminol
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Norepinephrine