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

doi:10.1016/j.nucmedbio.2005.12.001

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 journal › Article › peer-review

30 Citations (Scopus)

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
Pages (from-to)	239-243
Number of pages	5
Journal	Nuclear Medicine and Biology
Volume	33
Issue number	2
DOIs	https://doi.org/10.1016/j.nucmedbio.2005.12.001
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

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10.1016/j.nucmedbio.2005.12.001

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@article{9d004811e40c465091df3ae493edc337,

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

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 = "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",

author = "Stone, {James M} and Kjell Erlandsson and Erik Arstad and Bressan, {Rodrigo Affonseca} and Lisa Squassante and Vincenza Teneggi and Ell, {Peter J} and Pilowsky, {Lyn S}",

year = "2006",

month = feb,

doi = "10.1016/j.nucmedbio.2005.12.001",

language = "English",

volume = "33",

pages = "239--243",

journal = "Nuclear Medicine and Biology",

issn = "0969-8051",

publisher = "Elsevier Inc.",

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T1 - Ketamine displaces the novel NMDA receptor SPET probe [(123)I]CNS-1261 in humans in vivo

AU - Stone, James M

AU - Erlandsson, Kjell

AU - Arstad, Erik

AU - Bressan, Rodrigo Affonseca

AU - Squassante, Lisa

AU - Teneggi, Vincenza

AU - Ell, Peter J

AU - Pilowsky, Lyn S

PY - 2006/2

Y1 - 2006/2

N2 - [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.

AB - [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.

KW - Adult

KW - Brain

KW - Cross-Over Studies

KW - Guanidines

KW - Humans

KW - Iodine Radioisotopes

KW - Ketamine

KW - Male

KW - Metabolic Clearance Rate

KW - Molecular Probe Techniques

KW - Placebo Effect

KW - Radiopharmaceuticals

KW - Receptors, N-Methyl-D-Aspartate

KW - Single-Blind Method

KW - Tissue Distribution

KW - Tomography, Emission-Computed, Single-Photon

U2 - 10.1016/j.nucmedbio.2005.12.001

DO - 10.1016/j.nucmedbio.2005.12.001

M3 - Article

C2 - 16546678

SN - 0969-8051

VL - 33

SP - 239

EP - 243

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

IS - 2

ER -

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

Abstract

Keywords

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