A novel electrophilic synthesis and evaluation of medium specific radioactivity (1R,2S)-4-[18F]fluorometaraminol, a tracer for the assessment of cardiac sympathetic nerve integrity with PET



: Eskola O, Grönroos T, Bergman J, Haaparanta M, Marjamäki P, Lehikoinen P, Forsback S, Langer O, Hinnen F, Dollé F, Halldin C, Solin O

: 2004

: Nuclear Medicine and Biology

: Nuclear medicine and biology

: Nucl Med Biol

: 31

: 1

: 103

: 110

: 0969-8051

DOI: https://doi.org/10.1016/s0969-8051(03)00098-2


(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.



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