Annals of Nuclear Medicine

, 19:701 | Cite as

Evaluation of [11C]SA5845 and [11C]SA4503 for imaging of sigma receptors in tumors by animal PET

  • Kiichi Ishiwata
  • Kazunori Kawamura
  • Kazuo Kubota
  • Tadayuki Kobayashi
  • Philip H. Elsinga
  • Mayumi Ono
  • Minoru Maeda
Original Article


Sigma receptors are expressed in a wide variety of tumor cell lines, and are expressed in proliferating cells. A radioligand for the visualization of sigma receptors could be useful for selective detection of primary tumors and their metastases, and for non-invasive assessment of tumor proliferative status. To this end we evaluated two sigma receptor ligands, [11C]SA5845 and [11C]SA4503. In an in vitro study, AH109A hepatoma showed moderate densities of sigma1 and sigma2 receptors, and VX-2 carcinoma showed a high density of sigma2 receptors: Bmax (fmol/mg protein) for sigma1 vs. sigma2, 1,700 vs. 1,200 for AH109A hepatoma and 800 vs. 10,000 for VX-2 carcinoma. In a cell growth assay in vitro, neither SA5845 nor SA4503 (<10 μM) showed any inhibitory effect on proliferation of the AH109A hepatoma cells. In rats, the uptake of [11C]SA5845 and [11C]SA4503 in AH109A tissues was accumulated over the first 60 minutes; however, the uptake of both tracers increased by co-injection with haloperidol as a sigma receptor ligand. On the other hand, in the PET studies of rabbits, the uptake of [11C]SA5845 in the VX-2 carcinoma was relatively higher than that of [11C]SA4503, because of a much higher density of sigma2 receptors compared to sigma1 receptors in the VX-2 tissue, and the uptake of both tracers in the VX-2 tissue was decreased by carrier-loading and pre-treatment with haloperidol ([11C]SA5845, 53% and 26%, respectively; [11C]SA4503, 41% and 22%, respectively at 30 minutes after injection). Therefore, [11C]SA5845 and [11C]SA4503 may be potential ligands for PET imaging of sigma receptor-rich tumors.

Key words

sigma receptor PET SA5845 SA4503 tumor imaging 


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Copyright information

© Springer 2005

Authors and Affiliations

  • Kiichi Ishiwata
    • 1
  • Kazunori Kawamura
    • 1
    • 2
  • Kazuo Kubota
    • 3
  • Tadayuki Kobayashi
    • 4
  • Philip H. Elsinga
    • 5
  • Mayumi Ono
    • 6
  • Minoru Maeda
    • 7
  1. 1.Positron Medical CenterTokyo Metropolitan Institute of GerontologyItabashi-ku, TokyoJAPAN
  2. 2.SHI Accelerator ServiceTokyoJapan
  3. 3.Department of RadiologyInternational Medical Center of JapanTokyoJapan
  4. 4.M’s Science Co., Ltd.KobeJapan
  5. 5.PET-centerCroningen University HospitalGroningenThe Netherlands
  6. 6.Department of Medical Biochemistry, Graduate School of Medical SciencesKyushu UniversityFukuokaJapan
  7. 7.Graduate School of Pharmaceutical SciencesKyushu UniversityFukuokaJapan

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