Neuronal Mapping of the Heart with 6[18F]Fluorometaraminol

Donald M. Wieland, Karen C. Rosenspire, Gary D. Hutchins, Marcian Van Dort, Jill M. Rothley, Suresh G. Mislankar, Christopher C. Massin, David L. Gildersleeve, Philip S. Sherman, Markus Schwaiger, Helen T. Lee

Research output: Contribution to journalArticle

54 Scopus citations

Abstract

The false neurotransmitter metaraminol labeled with fluorine-18 has been used to noninvasively assess regional adrenergic nerve density in the canine heart. Intravenous administration of 6-[18F]fluorometaraminol (FMR) results in high, selective accumulation of radioactivity in the heart; drug blocking studies with desipramine and reserpine confirm the neuronal locus of FMR. Iodine-125 labeled metaraminol, however, shows no selective accumulation in the canine heart. Positron emission tomography (PET) analyses with FMR of closed-chest dogs bearing left ventricular neuronal defects clearly delineate the region of neuronal impairment; blood perfusion in the left ventricle wall was homogeneous as determined by [13N]NH3tomograms. The accumulation of FMR in regionally denervated dog heart correlates closely (r = 0.88) with endogenous norepinephrine concentrations. PET-generated 18F time-activity curves demonstrate marked kinetic differences between normal and denervated myocardium. FMR/PET analysis could be used to assess the heterogeneity of sympathetic innervation in human heart disease contingent on the development of FMR with sufficiently high specific activity to clearly avoid pressor activity.

Original languageEnglish (US)
Pages (from-to)956-964
Number of pages9
JournalJournal of Medicinal Chemistry
Volume33
Issue number3
DOIs
StatePublished - Mar 1990
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Wieland, D. M., Rosenspire, K. C., Hutchins, G. D., Van Dort, M., Rothley, J. M., Mislankar, S. G., Massin, C. C., Gildersleeve, D. L., Sherman, P. S., Schwaiger, M., & Lee, H. T. (1990). Neuronal Mapping of the Heart with 6[18F]Fluorometaraminol. Journal of Medicinal Chemistry, 33(3), 956-964. https://doi.org/10.1021/jm00165a012