Neuronal mapping of the heart with 6-[18F]fluorometaraminol

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

Research output: Contribution to journalArticle

54 Citations (Scopus)

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]NH3 tomograms. 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
StatePublished - 1990
Externally publishedYes

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Metaraminol
Positron emission tomography
Positron-Emission Tomography
Canidae
Dogs
Bearings (structural)
Desipramine
Fluorine
Reserpine
Iodine
Intravenous Administration
Adrenergic Agents
Radioactivity
Heart Ventricles
Neurotransmitter Agents
Heart Diseases
Myocardium
Norepinephrine
Thorax
Perfusion

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Wieland, D. M., Rosenspire, K. C., Hutchins, G., Van Dort, M., Rothley, J. M., Mislankar, S. G., ... Schwaiger, M. (1990). Neuronal mapping of the heart with 6-[18F]fluorometaraminol. Journal of Medicinal Chemistry, 33(3), 956-964.

Neuronal mapping of the heart with 6-[18F]fluorometaraminol. / Wieland, Donald M.; Rosenspire, Karen C.; Hutchins, Gary; Van Dort, Marcian; Rothley, Jill M.; Mislankar, Suresh G.; Lee, Helen T.; Massin, Christopher C.; Gildersleeve, David L.; Sherman, Philip S.; Schwaiger, Markus.

In: Journal of Medicinal Chemistry, Vol. 33, No. 3, 1990, p. 956-964.

Research output: Contribution to journalArticle

Wieland, DM, Rosenspire, KC, Hutchins, G, Van Dort, M, Rothley, JM, Mislankar, SG, Lee, HT, Massin, CC, Gildersleeve, DL, Sherman, PS & Schwaiger, M 1990, 'Neuronal mapping of the heart with 6-[18F]fluorometaraminol', Journal of Medicinal Chemistry, vol. 33, no. 3, pp. 956-964.
Wieland DM, Rosenspire KC, Hutchins G, Van Dort M, Rothley JM, Mislankar SG et al. Neuronal mapping of the heart with 6-[18F]fluorometaraminol. Journal of Medicinal Chemistry. 1990;33(3):956-964.
Wieland, Donald M. ; Rosenspire, Karen C. ; Hutchins, Gary ; Van Dort, Marcian ; Rothley, Jill M. ; Mislankar, Suresh G. ; Lee, Helen T. ; Massin, Christopher C. ; Gildersleeve, David L. ; Sherman, Philip S. ; Schwaiger, Markus. / Neuronal mapping of the heart with 6-[18F]fluorometaraminol. In: Journal of Medicinal Chemistry. 1990 ; Vol. 33, No. 3. pp. 956-964.
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