| Literature DB >> 19026948 |
Gert Luurtsema1, Robert C Schuit, Kevin Takkenkamp, Mark Lubberink, N Harry Hendrikse, Albert D Windhorst, Carla F M Molthoff, Nelleke Tolboom, Bart N M van Berckel, Adriaan A Lammertsma.
Abstract
[(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 80% 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.Entities:
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Year: 2008 PMID： 19026948 DOI： 10.1016/j.nucmedbio.2008.09.002
Source DB: PubMed Journal: Nucl Med Biol ISSN： 0969-8051 Impact factor: 2.408