Radiotracers for cardiac sympathetic innervation: Transport kinetics and binding affinities for the human norepinephrine transporter

Nuclear Medicine and Biology

Volumn 40, Issue 3, 2013, Pages 331-337

  Raffel, David M ^a   Chen, Wei ^a   Jung, Yong Woon ^a   Jang, Keun Sam ^a   Gu, Guie ^a   Cozzi, Nicholas V ^b  

^a UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

^b UNIVERSITY OF WISCONSIN SCHOOL OF MEDICINE AND PUBLIC HEALTH   (United States)

Author keywords

Biogenic amines; C6 glioma cells; Hydroxyephedrine; Isolated rat heart; Positron emission tomography

Indexed keywords

CARBON 3 HYDROXYEPHEDRINE C 11; CARBON 3 HYDROXYPHENETHYLGUANIDINE C 11; CARBON 4 FLUORO 3 HYDROXYPHENETHYLGUANIDINE C 11; CARBON 4 HYDROXYPHENETHYLGUANIDINE C 11; CARBON 6 FLUORO 3 HYDROXYPHENETHYLGUANIDINE C 11; CARBON EPINEPHRINE C 11; CARBON N GUANYL 3 OCTOPAMINE C 11; NORADRENALIN TRANSPORTER; TRACER; TRITIUM DOPAMINE H 3; TRITIUM NOREPINEPHRINE H 3; UNCLASSIFIED DRUG;

ACCURACY; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING ASSAY; COMPETITIVE INHIBITION; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DISSOCIATION CONSTANT; GENETIC TRANSFECTION; GLIOMA CELL; HEART INNERVATION; HUMAN; HUMAN CELL; IN VITRO STUDY; MICHAELIS MENTEN KINETICS; NONHUMAN; RAT; REPRODUCIBILITY; STRUCTURE ACTIVITY RELATION; SYMPATHETIC INNERVATION; TRANSPORT KINETICS;

ANIMALS; BIOLOGICAL TRANSPORT; CELL LINE, TUMOR; EPHEDRINE; EPINEPHRINE; HEART; HUMANS; KINETICS; NOREPINEPHRINE PLASMA MEMBRANE TRANSPORT PROTEINS; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; RADIOACTIVE TRACERS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SYMPATHETIC NERVOUS SYSTEM;

EID: 84875265595     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2012.11.014     Document Type: Article

References (26)

1. Bengel F.M. Imaging targets of the sympathetic nervous system of the heart: translational considerations. J Nucl Med 2011, 52:1167-1170.
2. DeGrado T.R., Hutchins G.D., Toorongian S.A., Wieland D.M., Schwaiger M. Myocardial kinetics of carbon-11-meta-hydroxyephedrine: retention mechanisms and effects of norepinephrine. J Nucl Med 1993, 34:1287-1293.
3. Nguyen N.T.B., DeGrado T.R., Chakraborty P., Wieland D.M., Schwaiger M. Myocardial kinetics of C-11 epinephrine in the isolated working rat heart. J Nucl Med 1997, 38:780-785.
4. Raffel D.M., Wieland D.M. Assessment of cardiac sympathetic nerve integrity with positron emission tomography. Nucl Med Biol 2001, 28:541-559.
5. Raffel D.M., Jung Y.W., Gildersleeve D.L., Sherman P.S., Moskwa J.J., Tluczek L.J., et al. Radiolabeled phenethylguanidines: novel imaging agents for cardiac sympathetic neurons and adrenergic tumors. J Med Chem 2007, 50:2078-2088.
6. Rosenspire K.C., Haka M.S., Van Dort M.E., Jewett D.M., Gildersleeve D.L., Schwaiger M., et al. Synthesis and preliminary evaluation of carbon-11-meta-hydroxyephedrine: a false transmitter agent for heart neuronal imaging. J Nucl Med 1990, 31:1328-1334.
7. 11C]epinephrine for routine PET studies in humans. Nucl Med Biol 1993, 20:939-944.
8. Lowry O.H., Rosebrough N.J., Farr A.L., Randall R.J. Protein measurments with the folin phenol reagent. J Biol Chem 1951, 193:265-275.
9. 3H]mazindol to cardiac norepinephrine transporters: kinetic and equilibrium studies. Naunyn-Schmiedeberg's Arch Pharmacol 2004, 370:9-16.
10. Iversen L.L. The uptake and storage of noradrenaline in sympathetic nerves 1967, Cambridge University Press, Cambridge.
11. Hellmann G., Hertting G., Peskar B. Uptake kinetics and metabolism of 7-3H-dopamine in the isolated perfused rat heart. Br J Pharmacol 1971, 41:256-269.
12. Iversen L.L. The uptake of noradrenaline by the isolated perfused rat heart. Brit J Pharmacol 1963, 21:523-537.
13. Iversen L.L. The uptake of catechol amines at high perfusion concentrations in the rat isolated heart: a novel catechol amine uptake process. Br J Pharmacol 1965, 25:18-33.
14. Iversen L.L. Role of transmitter uptake mechanisms in synaptic neurotransmission. Br J Pharmacol 1971, 41:571-591.
15. 131I]iodobenzylguanidine kinetics in isolated rat heart. Nucl Med Biol 1998, 25:59-64.
16. Raffel D., Loc'h C., Mardon K., Mazière B., Syrota A. Kinetics of the norepinephrine analog [Br-76]-meta-bromobenzylguanidine in isolated working rat heart. Nucl Med Biol 1998, 25:1-16.
17. Kim C.H., Kim H.S., Cubells J.F., Kim K.S. A previously undescribed intron and extensive 5' upstream sequence, but not Phox2a-mediated transactivation, are necessary for high level cell type-specific expression of the human norepinephrine transporter gene. J Biol Chem 1999, 274:6507-6518.
18. Eshleman A.J., Neve R.L., Janowsky A., Neve K.A. Characterization of a recombinant human dopamine transporter in multiple cell lines. J Pharmacol Exp Ther 1995, 274:276-283.
19. 3H]Substrate- and cell-specific effects of uptake inhibitors on human dopamine and serotonin transporter-mediated efflux. Synapse 1998, 30:97-106.
20. Foley K.F., Van Dort M.E., Sievert M.K., Ruoho A.E., Cozzi N.V. Stereospecific inhibition of monoamine uptake transporters by meta-hydroxyephedrine isomers. J Neur Transm 2002, 109:1229-1240.
21. Stein W.D. Transport and diffusion across cell membranes 1986, Academic Press, London.
22. Schömig E., Korber M., Bönisch H. Kinetic evidence for a common binding site for substrates and inhibitors of the neuronal noradrenaline carrier. Naunyn-Schmiedeberg's Arch Pharmacol 1988, 337:626-632.
23. Sung U., Apparsundaram S., Galli A., Kahlig K.M., Savchenko V., Schroeter S., et al. A regulated interaction of syntaxin 1A with the antidepressant-sensitive norepinephrine transporter establishes catecholamine clearance capacity. J Neurosci 2003, 23:1697-1709.
24. Bennett M.K., Garcia-Arraras J.E., Elferink L.A., Peterson K., Fleming A.M., Hazuka C.D., et al. The syntaxin family of vesicular transport receptors. Cell 1993, 74:863-873.
25. Fournier K.M., Robinson M.B. A dominant-negative variant of SNAP-23 decreases the cell surface expression of the neuronal glutamate transporter EAAC1 by slowing constitutive delivery. Neurochem Int 2006, 48:596-603.
26. Sager J.J., Torres G.E. Proteins interacting with monoamine transporters: current state and future challenges. Biochemistry 2011, 50:7295-7310.