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J Nucl Med. 2008; 49 (Supplement 1):47P
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Radiopharmaceutical Chemistry: New Chemistry-Other

Novel Radiolabeling Approaches

Investigation of novel 11C-guanidines as cardiac sympathetic nerve imaging agents

David Raffel1, Yong-Woon Jung1, Guie Gu1, Phillip Sherman1 and Carole Quesada1

1 Department of Radiology, University of Michigan, Ann Arbor, Michigan

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Objectives: Several 11C-phenethylguanidines have been found to possess favorable kinetic properties for quantifying cardiac sympathetic nerve density with PET, including long neuronal retention times due to trapping in vesicles. We sought to extend these findings by investigating other N-guanyl structures with known adrenergic activity as platforms for developing new 11C- and 18F-labeled sympathetic nerve tracers. Guanoxan (GOX) is a potent adrenergic neuron blocking agent and 2-(2-pyridinyl)ethylguanidine (2PYG) is an antihypertensive.

Methods: We prepared 11C-GOX, 11C-6-hydroxy-GOX (6H-GOX), 11C-7-hydroxy-GOX (7H-GOX), 11C-2PYG and 11C-5-hydroxy-2PYG (5H-2PYG) with 11CNBr (J Med Chem 50:2078, 2007). Neuronal uptake rates (Kup) and retention times (T1/2) were measured in isolated rat heart. Biodistribution studies were performed in rats at T = 30 min.

Results: GOX and 2PYG had similar neuronal uptake rates and retention times (see Table). 7H-GOX had more rapid uptake and much longer retention than GOX and 6H-GOX. 5H-2PYG had similar neuronal uptake to 2PYG, but much longer retention, consistent with efficient vesicular storage. Rat biodistribution data showed that GOX, 7H-GOX, 2PYG and 5H-2PYG all had low uptake in liver and lungs, suggesting good imaging properties in humans.

Conclusions: These findings demonstrate that ring hydroxylation of N-guanyl compounds with potent adrenergic activity frequently leads to agents with favorable kinetics and biodistribution for PET studies of cardiac sympathetic innervation.

Research Support: NIH R01-HL079540


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This Article
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Right arrow Articles by Quesada, C.