Nuclear Medicine and Biology
Volume 33, Issue 2 , Pages 239-243, February 2006

Ketamine displaces the novel NMDA receptor SPET probe [123I]CNS-1261 in humans in vivo☆

  • James M. Stone

      Affiliations

    • Institute of Psychiatry, King's College London, De Crespigny Park London, SE5 8AF UK
    • Corresponding Author InformationCorresponding author. Tel.: +44 020 7848 0531.
    • ,
  • Kjell Erlandsson

      Affiliations

    • Institute of Nuclear Medicine, University College London, London, W1N 8AA UK
    • ,
  • Erik Årstad

      Affiliations

    • Institute of Psychiatry, King's College London, De Crespigny Park London, SE5 8AF UK
    • ,
  • Rodrigo A. Bressan

      Affiliations

    • Institute of Psychiatry, King's College London, De Crespigny Park London, SE5 8AF UK
    • ,
  • Lisa Squassante

      Affiliations

    • GlaxoSmithKline (GSK), Verona 37135, Italy
    • ,
  • Vincenza Teneggi

      Affiliations

    • GlaxoSmithKline (GSK), Verona 37135, Italy
    • ,
  • Peter J. Ell

      Affiliations

    • Institute of Nuclear Medicine, University College London, London, W1N 8AA UK
    • ,
  • Lyn S. Pilowsky

      Affiliations

    • Institute of Psychiatry, King's College London, De Crespigny Park London, SE5 8AF UK
    • Institute of Nuclear Medicine, University College London, London, W1N 8AA UK

Received 3 October 2005; received in revised form 2 December 2005; accepted 4 December 2005.

Abstract 

[123I]CNS-1261 [N-(1-naphthyl)-N′-(3-iodophenyl)-N-methylguanidine] is a high-affinity SPET ligand with selectivity for the intrachannel PCP/ketamine/MK-801 site of the N-methyl-d-aspartate (NMDA) receptor. This study evaluated the effects of ketamine (a specific competitor for the intrachannel PCP/ketamine/MK-801 site) on [123I]CNS-1261 binding to NMDA receptors in vivo. Ten healthy volunteers underwent 2 bolus-plus-infusion [123I]CNS-1261 scans, one during placebo and the other during a ketamine challenge. Ketamine administration led to a significant decrease in [123I]CNS-1261 VT in most of the brain regions examined (P<.05). [123I]CNS-1261 appears to be a specific ligand in vivo for the intrachannel PCP/ketamine/MK-801 NMDA binding site.

Keywords: NMDA ion channel, Ketamine, [123I]CNS-1261, Single photon emission tomography

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☆ There are no conflicts of interest to report. LSP, EA, and KE were supported by a UK Medical Research Council Senior Clinical Research Fellowship to LSP. JS and RAB were supported by a research grant from GSK.

PII: S0969-8051(05)00294-5

doi:10.1016/j.nucmedbio.2005.12.001

Nuclear Medicine and Biology
Volume 33, Issue 2 , Pages 239-243, February 2006

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