Skip to main content
SpringerLink
Log in

Labelled sigma receptor ligands: can their role in neurology and oncology be extended?

  • Editorial
  • Published:
European Journal of Nuclear Medicine Aims and scope Submit manuscript

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

References

  1. Ferris CD, Hirsh DJ, Brooks BP, Snyder SH. σ receptors: from molecule to man. J Neurochem 1991; 57: 729–737.

    Article  CAS  PubMed  Google Scholar 

  2. Su T-P. σ receptors. Putative links between nervous, endocrine and immune systems. Eur J Biochem 1991; 200: 633–642.

    Article  CAS  PubMed  Google Scholar 

  3. Hellewell SB, Bruce A, Feinstein G, et al. Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors. Eur J Pharmacol 1994; 268: 9–18.

    Article  CAS  PubMed  Google Scholar 

  4. Hellewell SB, Bowen WD. A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain. Brain Res 1990; 527: 244–253.

    Article  CAS  PubMed  Google Scholar 

  5. Quirion R, Bowen WD, Itzhak Y, Junien JL, Musacchio JM, Rothman RB, Su TP, Tam SW, Taylor TW. A proposal for the classification of σ binding sites. Trends Pharmacol Sci 1992; 13: 85–86.

    Article  CAS  PubMed  Google Scholar 

  6. Nguyen V, Mardon K, Kassiou M, Christie MJ. In vitro and in vivo characterisation of [3H]ANSTO-14 binding to the σ1 binding sites. Nucl Med Biol 1999; 26: 209–215.

    Article  CAS  PubMed  Google Scholar 

  7. Hanner M, Moebius F, Flandorfer A, Knaus HG, Striessnig J, Kempner E, Glossmann H. Purification, molecular cloning, and expression of the mammalian sigma1-binding site. Proc Natl Acad Sci U S A 1996; 93: 8072–8077.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  8. Bowen WD, Hellewell SB, McGarry KA. Evidence for a multi-site model of the rat brain sigma receptor. Eur J Pharmacol 1989; 163: 309–318.

    Article  CAS  PubMed  Google Scholar 

  9. Bowen WD. Sigma receptors: recent advances and new clinical potentials. Pharm Acta Helv 2000; 74: 211–218.

    Article  CAS  PubMed  Google Scholar 

  10. Jansen KL, Faull RL, Storey P, Leslie RA. Loss of sigma binding sites in the CA1 area of the anterior hippocampus in Alzheimer’s disease correlates with CA1 pyramidal cell loss. Brain Res 1993; 623: 299–302.

    Article  CAS  PubMed  Google Scholar 

  11. Thurgur C, Church J. The anticonvulsant actions of sigma receptor ligands in the Mg2+-free model of epileptiform activity in rat hippocampal slices. Br J Pharmacol 1998; 124: 917–929.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  12. Helmeste DM, Tang SW, Bunney WE Jr, Potkin SG, Jones EG. Decrease in sigma but no increase in striatal dopamine D4 sites in schizophrenic brains. Eur J Pharmacol 1996; 314: R3–R5.

    Article  CAS  PubMed  Google Scholar 

  13. Shibuja H, Mori H Toru M. Sigma receptors in schizophrenic cerebral cortices. Neurochem Res 1992; 17: 983–990.

    Article  Google Scholar 

  14. Kawamura K, Ishiwata K, Tajima H, et al. Synthesis and in vivo evaluation of [11C]SA6298 as a PET sigma1 receptor ligand. Nucl Med Biol 1999; 26: 915–922.

    Article  CAS  PubMed  Google Scholar 

  15. Vilner BJ, John CS, Bowen WD. Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines. Cancer Res 1995; 55: 408–413.

    CAS  PubMed  Google Scholar 

  16. Bem WT, Thomas GE, Mamone JY, Homan SM, Levy BK, Johnson FE, Coscia CJ. Overexpression of σ receptors in nonneural human tumours. Cancer Res 1991; 51: 6558–6562.

    CAS  PubMed  Google Scholar 

  17. Mach RH, Smith CR, Al-Nabulsi I, Whirrett BR, Childers SR, Wheeler KT. σ2 receptors as potential biomarkers of proliferation in breast cancer. Cancer Res 1997; 57: 156–161.

    CAS  PubMed  Google Scholar 

  18. Wheeler KT, Wang LM, Wallen CA, Childers SR, Cline JM, Keng PC, Mach RH. Sigma-2 receptors as a biomarker of proliferation in solid tumours. Br J Cancer 2000; 82: 1223–1232.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  19. Al-Nabulsi I, Mach RH, Wang LM, Wallen CA, Keng PC, Sten K, Childers SR, Wheeler KT. Effect of ploidy, recruitment, environmental factors, and tamoxifen treatment on the expression of sigma-2 receptors in proliferating and quiescent tumour cells. Br J Cancer 1999; 81: 925–933.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  20. John CS, Lim B, Vilner BJ, Geyer BC, Bowen WD. Substituted halogenated arylsulfonamides: a new class of σ receptor binding tumor imaging agents. J Med Chem 1998; 41: 2445–2450.

    Article  CAS  PubMed  Google Scholar 

  21. Yang B, Wu L, Day CS, Wheeler SR, Choi SR, Kung HF, Mach RH. A sigma-2 selective 99mTc compound as a potential tumor imaging agent [abstract]. J Nucl Med 2000; 41: 121P.

    Google Scholar 

  22. Mach RH, Huang Y, Buchheimer et al. [F18]N-4′-fluorobenzyl-4-(3-bromophenyl)acetamide for imaging the receptor status of tumors. J Labelled Comp Radiopharm 1999; 42: S258.

    Google Scholar 

  23. John CS, Lim BB, Geyer BC, Vilner BJ, Bowen WD. 99mTc-labeled sigma-receptor-binding complex: synthesis, characterization, and specific binding to human ductal breast carcinoma (T47D) cells. Bioconjug Chem 1997; 8: 304–309.

    Article  CAS  PubMed  Google Scholar 

  24. John CS, Bowen WD, Fisher SJ, Lim BB, Geyer BC, Vilner BJ, Wahl- RL. Synthesis, in vitro pharmacologic characterization, and preclinical evaluation of N-[2-(1′-piperidinyl)ethyl]-3-[125I]iodo-4-methoxy-benzamide (P[125I]MBA) for imaging breast cancer. Nucl Med Biol 1999; 26: 377–382.

    Article  CAS  PubMed  Google Scholar 

  25. Michelot JM, Moreau MF, Veyre AJ, et al. Phase II scintigraphic clinical trial of malignant melanoma and metastases with iodine-123-N-(2-diethyl-aminoethyl-4-iodobenzamide). J Nucl Med 1993; 34: 1260–1266.

    CAS  PubMed  Google Scholar 

  26. Everaert H, Flamen P, Franken PR, Verhaege W, Bossuyt A. Sigma receptor imaging by means of 123-IDAB scintigraphy; clinical application in melanoma and non-small cell lung cancer. Anticancer Res 1997; 17: 1577–1582.

    CAS  PubMed  Google Scholar 

  27. Everaert H, Bossuyt A, Flamen P, Mertens J, Franken PR. Visualizing ocular melanoma using iodine-123-N-(diethylaminoethyl) 4-iodobenzamide SPECT. J Nucl Med 1997; 38: 870–873.

    CAS  PubMed  Google Scholar 

  28. Nicholl C, Mohammed A, Hull WE, Bubeck B, Eisenhut M. Pharmacokinetics of iodine-123-IMBA for melanoma imaging. J Nucl Med 1997; 38: 127–133.

    CAS  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Nuclear Medicine, University Hospital, Free University Brussels (AZ-VUB), 101 Laarbeeklaan, 1090, Brussels, Belgium

    Vicky Caveliers, Hendrik Everaert, Tony Lahoutte, Lawrence O. Dierickx & Axel Bossuyt

  2. Department of Radiology, George Washington University, Washington DC, USA

    Christy S. John

Authors
  1. Vicky Caveliers
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Hendrik Everaert
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Tony Lahoutte
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Lawrence O. Dierickx
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Christy S. John
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Axel Bossuyt
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Caveliers, V., Everaert, H., Lahoutte, T. et al. Labelled sigma receptor ligands: can their role in neurology and oncology be extended?. Eur J Nucl Med 28, 133–135 (2001). https://doi.org/10.1007/s002590000368

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s002590000368

Search

Navigation