Fluorine-18 radiolabelling, biodistribution studies and preliminary PET evaluation of a new memantine derivative for imaging the NMDA receptor |
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Authors: | Ametamey S M Samnick S Leenders K L Vontobel P Quack G Parsons C G Schubiger P A |
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Institution: | Center for Radiopharmaceutical Science of ETH, Paul Scherrer Institute, Villigen-PSI, Switzerland. |
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Abstract: | A synthetic method has been established for preparing 18F]1-amino-3-fluoromethyl-5-methyl-adamantane (18F]AFA). Biodistribution of the radiotracer in mice showed high brain uptake. The peak uptake (3.7% I.D/g organ) for the brain occurred at 30 min after injection. Accumulation of radioactivity in mouse brain was consistent with the known distribution of the NMDA receptors. The binding of 18F]AFA to the phencyclidine (PCP) binding sites of the NMDA receptor complex and the sigma recognition sites in a Rhesus monkey was also examined using positron emission tomography (PET). The regional brain distribution of 18F]AFA was changed by memantine and by (+)-MK-801, indicating competition for the same binding sites. Treatment with haloperidol caused a marked reduction of radioactivity uptake in all the brain regions examined. (-)-Butaclamol, which has pharmacological specificity for sigma sites, did not have any significant effects. |
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