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

doi:10.1021/jm00165a012

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

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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 language	English
Pages (from-to)	956-964
Number of pages	9
Journal	Journal of Medicinal Chemistry
Volume	33
Issue number	3
DOIs	https://doi.org/10.1021/jm00165a012
State	Published - Mar 1990
Externally published	Yes

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@article{8058ec52e2bb40cfb4d062be8067c8dc,

title = "Neuronal Mapping of the Heart with 6[18F]Fluorometaraminol",

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.",

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

year = "1990",

month = mar,

doi = "10.1021/jm00165a012",

language = "English",

volume = "33",

pages = "956--964",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "3",

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T1 - Neuronal Mapping of the Heart with 6[18F]Fluorometaraminol

AU - Wieland, Donald M.

AU - Rosenspire, Karen C.

AU - Hutchins, Gary D.

AU - Van Dort, Marcian

AU - Rothley, Jill M.

AU - Mislankar, Suresh G.

AU - Massin, Christopher C.

AU - Gildersleeve, David L.

AU - Sherman, Philip S.

AU - Schwaiger, Markus

AU - Lee, Helen T.

PY - 1990/3

Y1 - 1990/3

N2 - 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.

AB - 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.

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JO - Journal of Medicinal Chemistry

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

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