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

James M Stone, Kjell Erlandsson, Erik Arstad, Rodrigo Affonseca Bressan, Lisa Squassante, Vincenza Teneggi, Peter J Ell, Lyn S Pilowsky

Research output: Contribution to journalArticlepeer-review

30 Citations (Scopus)


[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.
Original languageEnglish
Pages (from-to)239-243
Number of pages5
JournalNuclear Medicine and Biology
Issue number2
Publication statusPublished - Feb 2006


  • Adult
  • Brain
  • Cross-Over Studies
  • Guanidines
  • Humans
  • Iodine Radioisotopes
  • Ketamine
  • Male
  • Metabolic Clearance Rate
  • Molecular Probe Techniques
  • Placebo Effect
  • Radiopharmaceuticals
  • Receptors, N-Methyl-D-Aspartate
  • Single-Blind Method
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon


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