期刊
NUCLEAR MEDICINE AND BIOLOGY
卷 35, 期 8, 页码 869-874出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.nucmedbio.2008.09.002
关键词
[(18)F]FDDNP; Amyloid; Metabolism; BBB transport; PET
资金
- DiMI [LSHB-CT-2005-512146]
[(18)F]FDDNP is a positron emission tomography (PET) tracer for determining amyloid plaques and neurofibrillary tangles in the brain in vivo. in order to quantify binding of this tracer properly, a metabolite-corrected plasma input function is required. The purpose of the present Study was to develop a sensitive method for measuring [(18)F]FDDNP and its radiolabelled metabolites in plasma. The second aim was to assess whether these radiolabelled metabolites enter the brain. In humans, there was extensive metabolism of [(18)F]FDDNP. After 10 min, more than 90% of plasma radioactivity was identified as polar (18)F-labelled fragments, probably formed from N-dealkylation of [(18)F]FDDNP. These labelled metabolites were reproduced in vitro using human hepatocytes. PET studies in rats showed that these polar metabolites can penetrate the blood-brain barrier and result in uniform brain uptake. (c) 2008 Elsevier Inc. All rights reserved.
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