6-[18F]fluorometaraminol: a radiotracer for in vivo mapping of adrenergic nerves of the heart.
The false neurotransmitter metaraminol has been 18F labeled and evaluated as a possible heart imaging agent on the basis of its selective accumulation in adrenergic nerves. Reaction of 6-(acetoxymercurio)-N-t-BOC-metaraminol with acetyl hypofluorite followed by removal of the BOC group provides a regiospecific synthesis of 6-fluorometaraminol (4). Use of acetyl hypo[18F]fluorite gives [18F]-4 in 60 min in 20-42% radiochemical yield. Systemic blockade of the neuronal uptake-1 carrier with desmethylimipramine or systemic destruction of the adrenergic nerves with 6-hydroxydopamine lowers [18F]-4 accumulation greater than or equal to 85% in all four regions of the rat heart. These preliminary findings suggest that [18F]-4 could be used to assess neuronal damage in various heart diseases by positron emission tomography.
Mislankar
S G
SG
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.
Gildersleeve
D L
DL
Wieland
D M
DM
Massin
C C
CC
Mulholland
G K
GK
Toorongian
S A
SA
D000818:Animals; D004285:Dogs; D005260:Female; D005462:Fluorine Radioisotopes; D006321:Heart / Q000000981:diagnostic imaging / Q000294:innervation*; D008297:Male; D008680:Metaraminol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D013564:Sympathetic Nervous System / Q000000981:diagnostic imaging*
D005462:Fluorine Radioisotopes; C054817:6-fluorometaraminol; D008680:Metaraminol