Nuclear Medicine and Biology
Volume 33, Issue 2 , Pages 211-215 , February 2006

In vivo evaluation in rats of [18F]1-(2-fluoroethyl)-4-[(4-cyanophenoxy)methyl]piperidine as a potential radiotracer for PET assessment of CNS sigma-1 receptors

  • Rikki N. Waterhouse

      Affiliations

    • Department of Psychiatry, Columbia University, New York, NY 10032, USA
    • Department of Radiology, Columbia University, New York, NY 10032, USA
    • Neurobiology and Imaging Program, Department of Biological Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA
    • Corresponding Author InformationCorresponding author. Neurobiology and Imaging Program, Department of Biological Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA. Tel.: +1 212 543 6630; fax: +1 212 543 6030.
    • ,
  • Raymond C. Chang

      Affiliations

    • Department of Psychiatry, Columbia University, New York, NY 10032, USA
    • Neurobiology and Imaging Program, Department of Biological Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA
    • ,
  • Jun Zhao

      Affiliations

    • Department of Psychiatry, Columbia University, New York, NY 10032, USA
    • Neurobiology and Imaging Program, Department of Biological Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA
    • ,
  • Patty E. Carambot

      Affiliations

    • Department of Psychiatry, Columbia University, New York, NY 10032, USA
    • Neurobiology and Imaging Program, Department of Biological Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA

Received 22 June 2005 ,Revised 19 October 2005 ,Accepted 19 October 2005.

References 

  1. Guitart X, Codony X, Monroy X. Sigma receptors: biology and therapeutic potential. Psychopharmacology. 2004;174:301–319
  2. Maurice T, Urani A, Phan VL, Romieu P. The interaction between neuroactive steroids and the sigma1 receptor function: behavioral consequences and therapeutic opportunities. Brain Res Brain Res Rev. 2001;37:116–132
  3. Maurice T, Martin-Fardon R, Romieu P, Matsumoto RR. Sigma(1) (sigma(1)) receptor antagonists represent a new strategy against cocaine addiction and toxicity. Neurosci Biobehav Rev. 2002;26:499–527
  4. Maurice T. Neurosteroids and sigma1 receptors, biochemical and behavioral relevance. Pharmacopsychiatry. 2004;37:S171–S182
  5. Takebayashi M, Hayashi T, Su TP. A perspective on the new mechanism of antidepressants: neuritogenesis through sigma-1 receptors. Pharmacopsychiatry. 2004;37(Suppl 3):S208–S213
  6. Su TP, Hayashi T. Understanding the molecular mechanism of sigma-1 receptors: towards a hypothesis that sigma-1 receptors are intracellular amplifiers for signal transduction. Curr Med Chem. 2003;10:2073–2080
  7. Nuwayhid SJ, Werling LL. Sigma1 receptor agonist-mediated regulation of N-methyl-d-aspartate-stimulated [3H]dopamine release is dependent upon protein kinase C. J Pharmacol Exp Ther. 2003;304:364–369
  8. Chaki S, Okuyama S, Ogawa S, Tomisawa K. Regulation of NMDA-induced [3H]dopamine release from rat hippocampal slices through sigma-1 binding sites. Neurochem Int. 1998;33:29–34
  9. Ault DT, Werling LL. Neuropeptide Y-mediated enhancement of NMDA-stimulated [3H]dopamine release from rat prefrontal cortex is reversed by sigma1 receptor antagonists. Schizophr Res. 1998;31:27–36
  10. Gudelsky GA. Effects of sigma receptor ligands on the extracellular concentration of dopamine in the striatum and prefrontal cortex of the rat. Eur J Pharmacol. 1995;286:223–228
  11. Gonzalez-Alvear GM, Werling LL. sigma1 receptors in rat striatum regulate NMDA-stimulated [3H]dopamine release via a presynaptic mechanism. Eur J Pharmacol. 1995;294:713–719
  12. Weatherspoon JK, Gonzalez-Alvear GM, Werling LL. Regulation of [3H]norepinephrine release from guinea pig hippocampus by sigma2 receptors. Eur J Pharmacol. 1997;326:133–138
  13. Gonzalez-Alvear GM, Werling LL. Sigma receptor regulation of norepinephrine release from rat hippocampal slices. Brain Res. 1995;673:61–69
  14. Nakagawara M, Sato Y. Neuropeptide Y: psychopharmacological and clinical aspects. Yakubutsu Seishin Kodo. 1994;14:117–127
  15. Hayashi T, Su T. Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs. 2004;18:269–284
  16. Bowen W. Sigma receptors: recent advances and new clinical potentials. Pharm Acta Helv. 2000;74:211–218
  17. Collier TL, Lecomte R, McCarthy TJ, Meikle S, Ruth TJ, Scopinaro F, et al. Assessment of cancer-associated biomarkers by positron emission tomography: advances and challenges. Dis Markers. 2002;18:211–247
  18. John CS, Bowen WD, Saga T, Kinuya S, Vilner BJ, Baumgold J, et al. A malignant melanoma imaging agent: synthesis, characterization, in vitro binding and biodistribution of iodine-125-(2-piperidinylaminoethyl)4-iodobenzamide. J Nucl Med. 1993;34:2169–2175
  19. Musacchio JM. The psychotomimetic effects of opiates and the sigma receptor. Neuropsychopharmacology. 1990;3:191–200
  20. Skuza G, Wedzony K. Behavioral pharmacology of sigma-ligands. Pharmacopsychiatry. 2004;37:S183–S188
  21. Debonnel G. Current hypotheses on sigma receptors and their physiological role: possible implications in psychiatry. J Psychiatr Neurosci. 1993;18:157–172
  22. Wang B, Rouzier R, Albarracin CT, Sahin A, Wagner P, Yang Y, et al. Expression of sigma 1 receptor in human breast cancer. Breast Cancer Res Treat. 2004;87:205–214
  23. Ding Y-W, Fowler FS, Dewey SL, Wolf AP, Logan J, Gatley SJ, et al. Synthesis and PET studies of fluorine-18-BMY 14802: a potential antipsychotic drug. J Nucl Med. 1993;34:246–254
  24. Jung YW, Frey KA, Mulholland GK, del Rosario R, Sherman PS, Raffel DM, et al. Vesamicol receptor mapping of brain cholinergic neurons with radioiodine-labeled positional isomers of benzovesamicol. J Med Chem. 1996;39:3331–3342
  25. Kimes AS, Wilson AA, Scheffel U, Campbell BG, London ED. Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites. J Med Chem. 1992;35:4683–4689
  26. Schlyer DJ, Volkow ND, Fowler JS, Wolf AP, Shiue C-Y, Dewey SL, et al. Regional distribution and kinetics of haloperidol binding in human brain: a pet study with [18F]haloperidol. Synapse. 1992;11:10–19
  27. Musachio J, Scheffel U, Stathis M, Ravert H, Mathews W, Dannals R. (+)-[C-11]-cis-N-benzyl-normetazocine: a selective ligand for sigma receptors in vivo. Life Sci. 1994;55:225
  28. Ametamey SM, Samnick S, Leenders KL, Vontobel P, Quack G, Parsons CG, et al. Fluorine-18 radiolabelling, biodistribution studies and preliminary PET evaluation of a new memantine derivative for imaging the NMDA receptor. J Recep Signal Transduct Res. 1999;19:129–141
  29. Ishiwata K, Senda M. In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum. Nucl Med Biol. 1999;26:627–631
  30. Ishiwata K, Noguchi J, Ishii S, Hatano K, Ito K, Nabeshima T, et al. Synthesis and preliminary evaluation of [11C]NE-100 labeled in two different positions as a PET sigma receptor ligand. Nucl Med Biol. 1998;25:195–202
  31. Elsinga P, Kawamura K, Kobayashi T, Tsukada H, Senda M, Vaalburg W, et al. Synthesis and evaluation of [18F]fluoroethyl SA4503 as a PET ligand for the sigma receptor. Synapse. 2002;43:259–267
  32. Kawamura K, Ishiwata K, Tajima H, Ishii S, Matsuno K, Homma Y, et al. In vivo evaluation of [(11)C]SA4503 as a PET ligand for mapping CNS sigma(1) receptors. Nucl Med Biol. 2000;27:255–261
  33. Waterhouse RN, Collier TL. In vivo evaluation of [18F]1-(3-fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine: a selective sigma-1 receptor radioligand for PET. Nucl Med Biol. 1997;24:127–134
  34. Waterhouse RN, Stabin MG, Page JG. Preclinical acute toxicity studies and rodent-based dosimetry estimates of the novel sigma-1 receptor radiotracer [(18)F]FPS. Nucl Med Biol. 2003;30:555–563
  35. Waterhouse RN, Slifstein M, Talbot P, Dumont F, Sultana A, Sudo Y, et al. Development of [18F]1-(3-fluoropropyl)-4-[(4-cyanomethoxy)methyl]piperidine ([18F]FPS): an effective PET tracer for imaging sigma-1 receptors in the primate CNS. Mol Imaging Biol. 2002;4:S35–S36
  36. Zhao J, Chang R, Carambot P, Waterhouse RN. Radiosynthesis and in vivo study of [18F]1-(2-flouroethyl)-4-[(4-cyanophenoxy)methyl]piperidine as a novel sigma-1 receptor ligand. J Label Compd Radiopharm. 2005;48:547–555
  37. van Waarde A, Buursma AR, Hospers GA, Kawamura K, Kobayashi T, Ishii K, et al. Tumor imaging with 2 sigma-receptor ligands, 18F-FE-SA5845 and 11C-SA4503: a feasibility study. J Nucl Med. 1939;45:1939–1945
  38. Leitner ML, Hohmann AG, Patrick SL, Walker JM. Regional variation in the ratio of sigma 1 to sigma 2 binding in rat brain. Eur J Pharmacol. 1994;259:65–69

PII: S0969-8051(05)00270-2

doi: 10.1016/j.nucmedbio.2005.10.007

Nuclear Medicine and Biology
Volume 33, Issue 2 , Pages 211-215 , February 2006

Article Tools

* Image Usage & Resolution