Abstract
(−)-Norepinephrine is the predominant neurotransmitter of the sympathetic innervation of the heart. Racemic norepinephrine was labelled with carbon-11 and injected i.v. into Cynomolgus monkeys. Five minutes after injection there was a more than tenfold higher radioactivity in the heart than in adjacent tissue. Pretreatment with the norepinephrine reuptake inhibitor desipramine reduced the uptake by more than 80%. The high specific uptake of racemic [11C]norepinephrine indicates that enatiomerically pure (−)-[11C]norepinephrine has promising potential for detailed mapping of the sympathetic innervation of the human myocardium.
Article PDF
Avoid common mistakes on your manuscript.
References
Axelrod J. The fate of adrenaline and noradrenaline. In: Vane J, Wolstenholme G, O'Connor M, eds.Adrenergic mechanisms. Boston: Little, Brown & Co; 1960:28–39.
Goldstein D, Brush J, Eisenhofer G, Stull R, Esler M. In vivo measurement of neuronal uptake of norepinephrine in the human heart.Circulation 1988;78:41–48.
Melon P, Schwaiger M. Imaging of metabolism and autonomic innervation of the heart by positron emission tomography.Eur J Nucl Med 1992;19:453–464.
Fowler J, MacGregor R, Ansari A, Atkins H, Wolf A. A new rapid synthesis of carbon-11 labeled norepinephrine hydrochloride.J Med Chem 1974;17:246–248.
Schwaiger M, Hutchins G, Wieland D. PET measurements of presynaptic sympathetic nerve terminals in the heart. In: Kuhl D, ed.In vivo imaging of neurotransmitter functions in brain, heart and tumors. Washington: American College of Nuclear Physicians; 1991:329–347.
Iversen L, Jarrot B, Simmonds M. Differences in the uptake, storage and metabolism of (+)- and (−)-noradrenaline.Br J Pharmacol 1971;43:845–855.
Garg B, Krell R, Sokolski T, Patil P. Steric aspects of adrenergic drugs XXII: retention of (+)- and (−)-norepinephrine by mouse heart.J Pharm Sci 1973;62:1126–1129.
Ding Y, Fowler J, Dewey S, et al. Comparison of high specific activity (−) and (+)-6-[18F]fluoronorepinephrine and 6-[18F]fluorodopamine in baboons: heart uptake, metabolism and the effect of desipramine.J Nucl Med 1993;34:619–629.
Någren K, Schoeps K, Halldin C, Swahn C, Farde L. Selective synthesis of racemic 1-11C-labelled norepinephrine, octopamine and phenylethanolamine using [11C]nitromethane.Appl Radiat Isot 1994;45 (in press).
Swahn C, Halldin C, Farde L. HPLC-method for determination of ligand metabolism during PET-studies.Ann Univ Turkuensis 1992;88:65–66.
Raismann R, Sette M, Pimoule C, Kanger S. High affinity3H-desipramine binding in the periphal and central nervous system: a specific site associated with the neuronal uptake of noradrenaline.Eur J Pharmacol 1982;78:345–351.
Author information
Authors and Affiliations
Additional information
Correspondence to: L. Farde
Rights and permissions
About this article
Cite this article
Farde, L., Halldin, C., Någren, K. et al. Positron emission tomography shows high specific uptake of racemic carbon-11 labelled norepinephrine in the primate heart. Eur J Nucl Med 21, 345–347 (1994). https://doi.org/10.1007/BF00947971
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF00947971