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

18Citations
Citations of this article
30Readers
Mendeley users who have this article in their library.

This article is free to access.

Abstract

[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 (K i) 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 K i 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.

Cite

CITATION STYLE

APA

Van Der Doef, T. F., Golla, S. S. V., Klein, P. J., Oropeza-Seguias, G. M., Schuit, R. C., Metaxas, A., … Boellaard, R. (2016). Quantification of the novel N-methyl-d-aspartate receptor ligand [11°C]GMOM in man. Journal of Cerebral Blood Flow and Metabolism, 36(6), 1111–1121. https://doi.org/10.1177/0271678X15608391

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free