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.
Original language | English |
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Pages (from-to) | 239-243 |
Number of pages | 5 |
Journal | Nuclear Medicine and Biology |
Volume | 33 |
Issue number | 2 |
DOIs | |
Publication status | Published - Feb 2006 |
Keywords
- 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