Quantification of the novel N-methyl-D-aspartate receptor ligand [C-11] GMOM in man

Thalia F. van der Doef, Sandeep S. V. Golla, Pieter J. Klein, Gisela M. Oropeza-Seguias, Robert C. Schuit, Athanasios Metaxas, Ellen Jobse, Lothar A. Schwarte, Albert D. Windhorst, Adriaan A. Lammertsma, Bart N. M. van Berckel, Ronald Boellaard

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18 Citations (Scopus)


[11C]GMOM (carbon-11 labeled N-(2-chloro-5-thiomethylphenyl)-N′-(3-[11C]methoxy-phenyl)-N′-methylguanidine) is a PET ligand that binds to the N-methyl-d-aspartate receptor with high specificity and affinity. The purpose of this first in human study was to evaluate kinetics of [11C]GMOM in the healthy human brain and to identify the optimal pharmacokinetic model for quantifying these kinetics, both before and after a pharmacological dose of S-ketamine. Dynamic 90 min [11C]GMOM PET scans were obtained from 10 subjects. In six of the 10 subjects, a second PET scan was performed following an S-ketamine challenge. Metabolite corrected plasma input functions were obtained for all scans. Regional time activity curves were fitted to various single- and two-tissue compartment models. Best fits were obtained using a two-tissue irreversible model with blood volume parameter. The highest net influx rate (Ki) of [11C]GMOM was observed in regions with high N-methyl-d-aspartate receptor density, such as hippocampus and thalamus. A significant reduction in the Ki was observed for the entire brain after administration of ketamine, suggesting specific binding to the N-methyl-d-aspartate receptors. This initial study suggests that the [11C]GMOM could be used for quantification of N-methyl-d-aspartate receptors.
Original languageEnglish
Pages (from-to)1111-1121
JournalJournal of cerebral blood flow and metabolism
Issue number6
Publication statusPublished - Jun 2016


  • Glutamate
  • N-methyl-D-aspartate receptor
  • [C-11] GMOM
  • kinetic modeling
  • positron emission tomography
  • quantitative imaging

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