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

• Published in: Journal of Nuclear Medicine Vol. 58; no. 8; pp. 1330 - 1333
• Main Authors: van der Aart, Jasper, van der Doef, Thalia F., Horstman, Paul, Huisman, Marc C., Schuit, Robert C., van Lingen, Arthur, Windhorst, Albert D., van Berckel, Bart N.M., Lammertsma, Adriaan A.
• Format: Journal Article
• Language: English
• Published: United States 01.08.2017
• Subjects: 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; NMDA; 11C; dosimetry; PET
• ISSN: 0161-5505; 2159-662X; 1535-5667
• DOI: 10.2967/jnumed.116.188250

The methylguanidine derivative C-GMOM ( C-labeled -(2-chloro-3-thiomethylphenyl)- '-(3-methoxyphenyl)- '-methylguanidine) has been used successfully to quantify -methyl-d-aspartate (NMDA) receptor binding in humans. The purpose of the present study was to estimate the C-GMOM radiation dose in healthy humans. After C-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. The mean absorbed radiation doses in source organs ranged from 7.7 μGy·MBq in the brain to 12.7 μGy·MBq in the spleen. The effective dose (±SD) was 4.5 ± 0.5 μSv·MBq The effective dose of C-GMOM is at the lower end of the range seen for other C-labeled ligands, allowing for serial PET scanning in a single subject.