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PET studies of 18 F-memantine in healthy volunteers

2002; Elsevier BV; Volume: 29; Issue: 2 Linguagem: Inglês

10.1016/s0969-8051(01)00293-1

1872-9614

S.M. Ametamey, Matthias Bruehlmeier, Stefan Kneifel, M. Kokic, M. Honer, Michele Arigoni, Andreas K. Buck, Corinna Bürger, Samuel Samnick, G. Quack, P. A. Schubiger,

Advanced MRI Techniques and Applications

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.