The Tohoku Journal of Experimental Medicine
Online ISSN : 1349-3329
Print ISSN : 0040-8727
ISSN-L : 0040-8727
Regular Contributions
Analysis of Plasma Metabolites during Human PET Studies with Three Receptor Ligands, [11C] YM-09151-2, [11C] doxepin and [11C] pyrilamine
Kiichi Ishiwata, Kazuhiko Yanai, Ren Iwata, Toshihiro Takahashi, Jun Hatazawa, Masatoshi Itoh, Koji Watabe, Takehiko Watanabe, Tatsuo Ido
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Keywords: receptor ligand, human plasma metabolites, carbon-11, positron emission tomography (PET)
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1996 Volume 178 Issue 2 Pages 129-136

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Abstract

Carbon-11 labeled metabolites in human plasma were analyzed by high- performance liquid chromatography during positron emission tomography (PET) studies using the dopamine D2 ligand [11C]YM-09151-2 as well as the histamine H1, ligands [11C] doxepin and [11C] pyrilamine. For all the three tracers, blood clearance of the radioactivity was extremely rapid after an i.v. injection. The plasma protein-binding of [11C]YM-09151-2 and [11C] doxepin had protective effects upon the metabolic alteration of the ligands, whereas [11C] pyrilamine was free from the protein-binding and immediately degraded. The degradation of [11C] doxepin was more rapid in epileptic patients on medication than in normal subjects. These results indicate that analysis of metabolites in the plasma is necessary to determine the accurate arterial input function for quantitative PET measurement.

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© 1996 Tohoku University Medical Press
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