Nuclear Medicine and Biology
Volume 36, Issue 2 , Pages 155-162 , February 2009

Preparation and evaluation of ethyl [18F]fluoroacetate as a proradiotracer of [18F]fluoroacetate for the measurement of glial metabolism by PET

  • Tetsuya Mori

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
  • ,
  • Li-Quan Sun

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
    • School of Life Science and Technology, Beijing Institute of Technology, Beijing 100081, China
  • ,
  • Masato Kobayashi

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
  • ,
  • Yasushi Kiyono

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
    • Corresponding Author InformationCorresponding author. Tel.: +81 776 61 8420; fax: +81 776 61 8170.
  • ,
  • Hidehiko Okazawa

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
  • ,
  • Takako Furukawa

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan
  • ,
  • Hidekazu Kawashima

      Affiliations

    • Graduate School of Medicine, Kyoto University, Kyoto 606-8501, Japan
  • ,
  • Michael J. Welch

      Affiliations

    • Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA
  • ,
  • Yasuhisa Fujibayashi

      Affiliations

    • Biomedical Imaging Research Center, University of Fukui, Fukui 910-1193, Japan

Received 3 October 2008 ,Revised 5 November 2008 ,Accepted 11 November 2008.

References 

  1. Bains JS, Oliet SH. Glia: they make your memories stick!. Trends Neurosci. 2007;30:417–424
  2. Haydon PG, Carmignoto G. Astrocyte control of synaptic transmission and neurovascular coupling. Physiol Rev. 2006;86:1009–1031
  3. Nedergaard M, Ransom B, Goldman SA. New roles for astrocytes: redefining the functional architecture of the brain. Trends Neurosci. 2003;26:523–530
  4. Volterra A, Meldolesi J. Astrocytes, from brain glue to communication elements: the revolution continues. Nat Rev Neurosci. 2005;6:626–640
  5. Haberg A, Qu H, Sonnewald U. Glutamate and GABA metabolism in transient and permanent middle cerebral artery occlusion in rat: importance of astrocytes for neuronal survival. Neurochem Int. 2006;48:531–540
  6. Hosoi R, Kashiwagi Y, Tokumura M, Abe K, Hatazawa J, Inoue O. Sensitive reduction in 14C-acetate uptake in a short-term ischemic rat brain. J Stroke Cerebrovasc Dis. 2007;16:77–81
  7. Anezaki T, Yanagisawa K, Takahashi H, Nakajima T, Miyashita K, Ishikawa A, et al. Remote astrocytic response of prefrontal cortex is caused by the lesions in the nucleus basalis of Meynert, but not in the ventral tegmental area. Brain Res. 1992;574:63–69
  8. Hundal O. Major depressive disorder viewed as a dysfunction in astroglial bioenergetics. Med Hypotheses. 2007;68:370–377
  9. Kondziella D, Brenner E, Eyjolfsson EM, Markinhuhta KR, Carlsson ML, Sonnewald U. Glial–neuronal interactions are impaired in the schizophrenia model of repeated MK801 exposure. Neuropsychopharmacology. 2006;31:1880–1887
  10. Qu H, Eloqayli H, Muller B, Aasly J, Sonnewald U. Glial–neuronal interactions following kainate injection in rats. Neurochem Int. 2003;42:101–106
  11. Zwingmann C, Leibfritz D, Hazell AS. Brain energy metabolism in a sub-acute rat model of manganese neurotoxicity: an ex vivo nuclear magnetic resonance study using [1-13C]glucose. Neurotoxicology. 2004;25:573–587
  12. Muir D, Berl S, Clarke DD. Acetate and fluoroacetate as possible markers for glial metabolism in vivo. Brain Res. 1986;380:336–340
  13. Waniewski RA, Martin DL. Preferential utilization of acetate by astrocytes is attributable to transport. J Neurosci. 1998;18:5225–5233
  14. Kuge Y, Hikosaka K, Seki K, Ohkura K, Nishijima K, Tsukamoto E, et al. In vitro uptake of [1-14C]octanoate in brain slices of rats: basic studies for assessing [1-11C]octanoate as a PET tracer of glial functions. Nucl Med Biol. 2002;29:303–306
  15. Kuge Y, Kawashima H, Yamazaki S, Hashimoto N, Miyake Y. [1-11C]octanoate as a potential PET tracer for studying glial functions: PET evaluation in rats and cats. Nucl Med Biol. 1996;23:1009–1012
  16. Yamazaki S, Fukui K, Kawashima H, Kuge Y, Miyake Y, Kangawa K. Uptake of radioactive octanoate in astrocytoma cells: basic studies for application of [11C]octanoate as a PET tracer. Ann Nucl Med. 1996;10:395–399
  17. Inoue O, Hosoi R, Momosaki S, Yamamoto K, Amitani M, Yamaguchi M, et al. Evaluation of [14C]phenylacetate as a prototype tracer for the measurement of glial metabolism in the rat brain. Nucl Med Biol. 2006;33:985–989
  18. Momosaki S, Hosoi R, Sanuki T, Todoroki K, Yamaguchi M, Gee A, et al. [14C]Benzyl acetate is a potential radiotracer for the measurement of glial metabolism in the rat brain. Nucl Med Biol. 2007;34:939–944
  19. Fonnum F, Johnsen A, Hassel B. Use of fluorocitrate and fluoroacetate in the study of brain metabolism. Glia. 1997;21:106–113
  20. Lear JL, Ackermann RF. Evaluation of radiolabeled acetate and fluoroacetate as potential tracers of cerebral oxidative metabolism. Metab Brain Dis. 1990;5:45–56
  21. Hassel B, Bachelard H, Jones P, Fonnum F, Sonnewald U. Trafficking of amino acids between neurons and glia in vivo. Effects of inhibition of glial metabolism by fluoroacetate. J Cereb Blood Flow Metab. 1997;17:1230–1238
  22. Morrison JF, Peters RA. Biochemistry of fluoroacetate poisoning: the effect of fluorocitrate on purified aconitase. Biochem J. 1954;58:473–479
  23. Sun LQ, Mori T, Dence CS, Ponde DE, Welch MJ, Furukawa T, et al. New approach to fully automated synthesis of sodium [18F]fluoroacetate — a simple and fast method using a commercial synthesizer. Nucl Med Biol. 2006;33:153–158
  24. Oldendorf WH. Measurement of brain uptake of radiolabeled substances using a tritiated water internal standard. Brain Res. 1970;24:372–376
  25. DeGrado TR, Turkington TG, Williams JJ, Stearns CW, Hoffman JM, Coleman RE. Performance characteristics of a whole-body PET scanner. J Nucl Med. 1994;35:1398–1406
  26. Saji H, Iida Y, Kawashima H, Ogawa M, Kitamura Y, Mukai T, et al. In vivo imaging of brain dopaminergic neurotransmission system in small animals with high-resolution single photon emission computed tomography. Anal Sci. 2003;19:67–71
  27. Buchwald P. Structure–metabolism relationships: steric effects and the enzymatic hydrolysis of carboxylic esters. Mini Rev Med Chem. 2001;1:101–111
  28. Ericsson H, Tholander B, Regardh CG. In vitro hydrolysis rate and protein binding of clevidipine, a new ultrashort-acting calcium antagonist metabolised by esterases, in different animal species and man. Eur J Pharm Sci. 1999;8:29–37
  29. Morikawa M, Inoue M, Tsuboi M. Substrate specificity of carboxylesterase (E.C.3.1.1.1) from several animals. Chem Pharm Bull (Tokyo). 1976;24:1661–1664
  30. Quon CY, Mai K, Patil G, Stampfli HF. Species differences in the stereoselective hydrolysis of esmolol by blood esterases. Drug Metab Dispos. 1988;16:425–428
  31. Ponde DE, Dence CS, Oyama N, Kim J, Tai YC, Laforest R, et al. F-Fluoroacetate: a potential acetate analog for prostate tumor imaging — in vivo evaluation of 18F-fluoroacetate versus 11C-acetate. J Nucl Med. 2007;48:420–428
  32. Clarke DD. Fluoroacetate and fluorocitrate: mechanism of action. Neurochem Res. 1991;16:1055–1058

PII: S0969-8051(08)00244-8

doi: 10.1016/j.nucmedbio.2008.11.006

Nuclear Medicine and Biology
Volume 36, Issue 2 , Pages 155-162 , February 2009