Human Dosimetry of the N-Methyl-d-Aspartate Receptor Ligand 11C-GMOM

Jasper van der Aart; Thalia F van der Doef; Paul Horstman; Marc C Huisman; Robert C Schuit; Arthur van Lingen; Albert D Windhorst; Bart N M van Berckel; Adriaan A Lammertsma

doi:10.2967/jnumed.116.188250

Human Dosimetry of the N-Methyl-d-Aspartate Receptor Ligand ¹¹C-GMOM

J Nucl Med. 2017 Aug;58(8):1330-1333. doi: 10.2967/jnumed.116.188250. Epub 2017 Feb 9.

Authors

Jasper van der Aart¹, Thalia F van der Doef², Paul Horstman², Marc C Huisman², Robert C Schuit², Arthur van Lingen², Albert D Windhorst², Bart N M van Berckel², Adriaan A Lammertsma²

Affiliations

¹ Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands jaspervanderaart@gmail.com.
² Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands.

PMID: 28183990
DOI: 10.2967/jnumed.116.188250

Abstract

The methylguanidine derivative ¹¹C-GMOM (¹¹C-labeled N-(2-chloro-3-thiomethylphenyl)-N'-(3-methoxyphenyl)-N'-methylguanidine) has been used successfully to quantify N-methyl-d-aspartate (NMDA) receptor binding in humans. The purpose of the present study was to estimate the ¹¹C-GMOM radiation dose in healthy humans. Methods: After ¹¹C-GMOM injection, 3 female and 2 male subjects underwent 10 consecutive whole-body PET scans in approximately 77 min. Seven source organs were defined manually, scaled to a sex-specific reference, and residence times were calculated for input into OLINDA/EXM software. Accepted tissue-weighting factors were used to calculate the effective dose. Results: The mean absorbed radiation doses in source organs ranged from 7.7 μGy·MBq^-1 in the brain to 12.7 μGy·MBq^-1 in the spleen. The effective dose (±SD) was 4.5 ± 0.5 μSv·MBq^-1Conclusion: The effective dose of ¹¹C-GMOM is at the lower end of the range seen for other ¹¹C-labeled ligands, allowing for serial PET scanning in a single subject.

Keywords: 11C; NMDA; PET; dosimetry.

Publication types

Clinical Trial
Research Support, Non-U.S. Gov't

MeSH terms

Adult
Carbon Radioisotopes*
Female
Guanidines / metabolism*
Guanidines / pharmacokinetics
Healthy Volunteers
Humans
Ligands
Male
Positron-Emission Tomography
Radiometry
Receptors, N-Methyl-D-Aspartate / metabolism*
Tissue Distribution

Substances

Carbon Radioisotopes
Guanidines
Ligands
N-(2-chloro-5-thiomethylphenyl)-N'-(3-methoxyphenyl)-N'-methylguanidine
Receptors, N-Methyl-D-Aspartate