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

J Cereb Blood Flow Metab. 2016 Jun;36(6):1111-21. doi: 10.1177/0271678X15608391. Epub 2015 Oct 5.


[(11)C]GMOM (carbon-11 labeled N-(2-chloro-5-thiomethylphenyl)-N'-(3-[(11)C]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 [(11)C]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 [(11)C]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 [(11)C]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 [(11)C]GMOM could be used for quantification of N-methyl-d-aspartate receptors.

Keywords: Glutamate; N-methyl-d-aspartate receptor; [11C]GMOM; kinetic modeling; positron emission tomography; quantitative imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Brain / metabolism*
  • Carbon Radioisotopes / pharmacokinetics
  • Female
  • Humans
  • Kinetics
  • Ligands
  • Male
  • Positron-Emission Tomography / methods*
  • Protein Binding
  • Radiopharmaceuticals / pharmacokinetics
  • Receptors, N-Methyl-D-Aspartate / analysis
  • Receptors, N-Methyl-D-Aspartate / metabolism*
  • Young Adult


  • Carbon Radioisotopes
  • Ligands
  • Radiopharmaceuticals
  • Receptors, N-Methyl-D-Aspartate