PET studies of 18F-memantine in healthy volunteers

Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In hu...

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Veröffentlicht in:Nuclear medicine and biology 2002-02, Vol.29 (2), p.227-231
Hauptverfasser: AMETAMEY, S. M, BRUEHLMEIER, M, SCHUBIGER, P. A, KNEIFEL, S, KOKIC, M, HONER, M, ARIGONI, M, BUCK, A, BURGER, C, SAMNICK, S, QUACK, G
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container_end_page 231
container_issue 2
container_start_page 227
container_title Nuclear medicine and biology
container_volume 29
creator AMETAMEY, S. M
BRUEHLMEIER, M
SCHUBIGER, P. A
KNEIFEL, S
KOKIC, M
HONER, M
ARIGONI, M
BUCK, A
BURGER, C
SAMNICK, S
QUACK, G
description Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of 18F-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of 18F-memantine was examined in five healthy volunteers. In humans, 18F-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of 18F-memantine in receptor-rich regions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that 18F-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors.
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The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. 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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects Adult
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
Humans
Investigative techniques, diagnostic techniques (general aspects)
Male
Medical sciences
Memantine - analogs & derivatives
Memantine - blood
Memantine - pharmacokinetics
Nervous system
Radioligand Assay
Radionuclide investigations
Radiopharmaceuticals - blood
Radiopharmaceuticals - pharmacokinetics
Receptors, N-Methyl-D-Aspartate - analysis
Receptors, N-Methyl-D-Aspartate - metabolism
Reference Values
Tomography, Emission-Computed
title PET studies of 18F-memantine in healthy volunteers
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